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5-HT2Areceptor agonist-1 is a 5-HT2Areceptor agonist with the EC50 of 5.54 nM. 5-HT2Areceptor agonist-1 can be used for the research of mood disorders .
5-HT2Areceptor agonist-3 is the most selective agonist for the human 5-HT2Areceptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor .
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
Lumateperone (ITI-007) tosylate is a 5-HT2Areceptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .
Lumateperone (ITI-007) is an orally active 5-HT2Areceptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2Areceptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction .
5-HT2Areceptor agonist-2 is a highly potent serotonin 5-HT2 receptor agonists. 5-HT2Areceptor agonist-2 inspires 5-HT2A, 5-HT2B, and 5-HT2C with EC50 values of 1.7, 0.58, and 0.50 nM, respectively .
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2Areceptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2Areceptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .
LY320954 is a selective 5-HT2Areceptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+ influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
5-HT6/5-HT2Areceptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2Areceptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2Areceptor ligand-1 has the potential for neurological and psychiatric disorders research .
5-HT6/5-HT2Areceptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2Areceptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2Areceptor ligand-2 shows pro-cognitive properties .
5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2Creceptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .
LPH-5 is a selective 5-HT2Areceptor agonist (EC50=190 nM). LPH-5 works by selectively activating the 5-HT2Areceptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the 5-HT2Areceptor. LPH-5 can be used to further explore the 5-HT2Areceptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders .
cis-Urocanic acid is a 5-HT2Areceptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2Areceptor .
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2Areceptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2Areceptor in humans, respectively, and has potent antidepressant activity.
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2Areceptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2Areceptor[1].
Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2Areceptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2Areceptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2Areceptor. Iferanserin has the potential for internal hemorrhoid disease treatment .
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
Risperidone is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2Areceptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2Areceptor-mediated current response with an IC50 of 72.4 μM.
Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Pipamperone (Floropipamide; McN-JR 3345) dihydrochloride is a high-affinity antagonist of 5-HT2Areceptor (pKi=8.2) and D4receptor (pKi=8.0) and a low-affinity antagonist of D2receptor (pKi=6.7) .
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
Deramciclane has a high affinity for 5-HT2A and 5-HT2Creceptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2Creceptors without direct stimulatory agonist.
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2Areceptor (pKi=8.2) and D4receptor (pKi=8.0) and a low-affinity antagonist of D2receptor (pKi=6.7) .
Flumexadol is a selective and affinity 5-HT2Creceptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2Areceptor. Flumexadol is an orally active non-narcotic analgesic .
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2Areceptor with pIC50 and pKd of 8.73 and 9.3, respectively.
(+)-OSU6162 is an stabilizer on dopaminergic and serotonergic brain signaling. (+)-OSU6162 is a partial agonist of 5-HT2Areceptor. (+)-OSU6162 can be used for neurological research .
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2)receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2Areceptor. Fananserin also is a selective dopamine D4receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor .
Pruvanserin (EMD 281014 free acid) is a selective 5-HT2Areceptor antagonist. Pruvanserin alleviates tactile allodynia in diabetic rats. Pruvanserin can also be used for research of insomnia .
Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT2Areceptor antagonist, extracted from patent WO 2005/002578 A1 .
ZINC866533340 is a ligand for 5-HT receptor5-HT2A with Ki of 1.6 nM. ZINC866533340 is used in AlphaFold2 technology to determines three-dimensional structure of proteins .
Cyproheptadine hydrochloride is a potent and orally active 5-HT2Areceptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders .
Cyproheptadine is a potent and orally active 5-HT2Areceptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders .
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
(R)-Fluoxetine hydrochloride, an antidepressant, is serotonin reuptake inhibitor (SSRI). (R)-Fluoxetine hydrochloride has modest affinity at the 5-HT2A and 5-HT2Creceptors .
Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
Risperidone (Standard) is the analytical standard of Risperidone. This product is intended for research and analytical applications. Risperidone is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2Areceptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
Pimavanserin (Standard) is the analytical standard of Pimavanserin. This product is intended for research and analytical applications. Pimavanserin is a selective inverse agonist of the 5-HT2Areceptor with pIC50 and pKd of 8.73 and 9.3, respectively.
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2Areceptor-mediated contraction of guinea pig trachea .
Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2Areceptor (Ki of 0.6 nM) and dopamine D2receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1Areceptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2Areceptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2Areceptor with a pA2 of 8.32 in a rat tail artery assay .
Pipamperone (Standard) is the analytical standard of Pipamperone. This product is intended for research and analytical applications. Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2Areceptor (pKi=8.2) and D4receptor (pKi=8.0) and a low-affinity antagonist of D2receptor (pKi=6.7) .
Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
Renzapride hydrochloride is a benzamide that inhibits irritable bowel syndrome and has antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors. Renzapride hydrochloride also exhibits antagonistic activity at 5-HT(2B) receptors and has a certain affinity for 5-HT(2A) and 5-HT(2C) receptors .
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2Areceptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergicreceptors and H1-histaminergicreceptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2Areceptor (Ki=0.6 nM) and dopamine D2receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1Areceptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2Areceptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively .
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2Areceptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
SB-200646 is the first selective 5-HT2B/2C over 5-HT2Areceptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo .
SB-200646A is the first selective 5-HT2B/2C over 5-HT2Areceptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo .
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2Areceptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
1-1-Naphthylpiperazine hydrochloride (1-NP hydrochloride; 1-Naphthylpiperazine hydrochloride) is a serotonergic derivative of quipazine, which is both an agonist for 5-HT1Areceptor and an antagonist for 5-HT2Areceptor. 1-1-Naphthylpiperazine hydrochloride induces cell apoptosis. 1-1-Naphthylpiperazine hydrochloride prevents the immunosuppression and photocarcinogenesis .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].
Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation .
Zicronapine is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2Areceptors.
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2Areceptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension .
Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2Areceptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3receptors .
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2Areceptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
Perospirone (hydrochloride) (Standard) is the analytical standard of Perospirone (hydrochloride). This product is intended for research and analytical applications. Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2Areceptor (Ki of 0.6 nM) and dopamine D2receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1Areceptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
Risperidone E-oxime (Standard) is the analytical standard of Risperidone E-oxime. This product is intended for research and analytical applications. Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Cyproheptadine (Standard) is the analytical standard of Cyproheptadine. This product is intended for research and analytical applications. Cyproheptadine is a potent and orally active 5-HT2Areceptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders .
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Cyproheptadine (hydrochloride) (Standard) is the analytical standard of Cyproheptadine (hydrochloride). This product is intended for research and analytical applications. Cyproheptadine hydrochloride is a potent and orally active 5-HT2Areceptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders .
1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
Brexpiprazole-d8 is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2Areceptor antagonist (Ki=0.47 nM)[1][2].
BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptorKi values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent .
Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergicreceptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells .
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].
SB 221284 is a selective 5-HT2C/2Breceptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2Creceptors, respectively. SB 221284 can be used for the research of neurological disease .
LY266097 hydrochloride is a selective 5-HT2Breceptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
Promethazine (hydrochloride) (Standard) is the analytical standard of Promethazine (hydrochloride). This product is intended for research and analytical applications. Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2Areceptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine . Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .
Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity .
Tedatioxetine (Lu AA24530) acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist .
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM .
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2Areceptor-mediated signaling .
CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration .
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergicreceptors and H1-histaminergicreceptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist .
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Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2Areceptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2Lreceptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM) .
A-381393 is a potent, selective, brain penetrate dopamine D4receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM) .
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2Areceptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19 .
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2Lreceptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM) .
Perphenazine (Standard) is the analytical standard of Perphenazine. This product is intended for research and analytical applications. Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2Breceptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2Breceptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
PF-03246799 (PF-3246799) is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research .
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2Areceptors, respectively. BL-1020 mesylate is agonist for GABAAreceptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1][2].
Quetiapine (Standard) is the analytical standard of Quetiapine. This product is intended for research and analytical applications. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2Areceptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopaminereceptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopaminereceptor antagonist . Ziprasidone hydrochloride has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopaminereceptor antagonist . Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
Zicronapine (Lu 31-130) fumarate is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine (Lu 31-130) fumarate has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2Areceptors .
Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats .
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats .
Flibanserin (Standard) is the analytical standard of Flibanserin. This product is intended for research and analytical applications. Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2Areceptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopaminereceptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2Areceptor with pIC50 and pKd of 8.73 and 9.3, respectively .
Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2Creceptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2Breceptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects .
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2Breceptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility .
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT2Creceptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2Breceptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .
Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopaminereceptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
Cyamemazine-d6 is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
Flibanserin (hydrochloride) (propan-2-ol) (hydrate) (BIMT-17 (hydrochloride) (propan-2-ol) (hydrate); BIMT-17BS (hydrochloride) (propan-2-ol) (hydrate))is an orally active serotonin 5-HT1A receptor agonist and 5-HT2Areceptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin hydrochloride shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2Areceptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM[1][2][3].
RS-64459-193 is a 5-HT1A receptor partial agonist with a Ki of 24.9 nM. RS-64459-193 also shows high affinity for 5-HT2C, 5-HT2A and 5-HT7 with pKi values of 6.87, 7.02, and 7.18, respectively. RS-64459-193 is almost devoid of activity at the m 5-HT3 receptor .
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2Lreceptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM) .
SB-215505 is a potent and subtype-selective 5-HT2Breceptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively . SB-215505 increases wakefulness and motor activity in rats .
AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent .
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
CP-809101 hydrochloride is a potent and highly selective 5-HT2Creceptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2Areceptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
CP-809101 is a potent and highly selective 5-HT2Creceptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2Areceptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
SB228357 is a selective, potent and orall active 5-HT2C/2Breceptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects .
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model .
Ziprasidone (hydrochloride monohydrate) (Standard) is the analytical standard of Ziprasidone (hydrochloride monohydrate). This product is intended for research and analytical applications. Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopaminereceptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
Ziprasidone (hydrochloride) (Standard) is the analytical standard of Ziprasidone (hydrochloride). This product is intended for research and analytical applications. Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability .
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2Creceptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2Areceptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2Creceptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2Areceptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
Zotepine (Standard) is the analytical standard of Zotepine. This product is intended for research and analytical applications. Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
SB 242084 monohydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2Creceptor antagonist (crosses the blood-brain barrier). SB 242084 monohydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2Areceptor. SB 242084 monohydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
AVN-101 free base is a multi-target drug candidate with the potential to inhibit central nervous system (CNS) diseases. AVN-101 free base exhibits high inhibitory activity on 5-HT7 receptors and also has certain activity on 5-HT6, 5-HT2A and 5-HT2C receptors. Due to its anxiolytic and antidepressant activities, AVN-101 free base is also expected to be used in diseases such as general anxiety disorder, depression, schizophrenia and multiple sclerosis .
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
Org37684 is a highly potent 5-HT2Creceptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC50=7.96) and ten times for the 5-HT2A (pEC50=7.11) receptor .
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2Creceptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects .
LY314228 is an aminoguanidine 5-HT2 antagonist with relative selectivity for 5-HT2A receptors (IC50: 147.9 nM). The Ki values ??of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2Creceptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2Creceptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
JPC0323 is a dual 5-HT2C/5-HT2Areceptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values ??for 5-HT2receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research .
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2Creceptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
Methiothepin maleate is a potent and non-selective 5-HT2receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Pimethixene maleate (Standard) is the analytical standard of Pimethixene maleate. This product is intended for research and analytical applications. Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
Methiothepin is a potent and non-selective 5-HT2receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV (Kis=6.6 and 8.9 nM, respectively). It is also an antagonist of the 5-HT2Areceptor and the α2B-adrenergic receptor (Ki=5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gαq and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2CINI receptors (EC50s=38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s=38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2Areceptor-mediated current response with an IC50 of 72.4 μM.
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Cyproheptadine is a potent and orally active 5-HT2Areceptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders .
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergicreceptors and H1-histaminergicreceptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergicreceptors and H1-histaminergicreceptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
5HT2A Protein, Human (Sf9, Flag, His, H70-A265, S162K, M164W, Q313-K403) is the recombinant human-derived 5HT2A, expressed by Sf9 insect cells , with His, Flag labeled tag. ,
5HT2A Protein, Human (Sf9, Flag, His, L66-A265, T311-P405, L247A, L371A) is the recombinant human-derived 5HT2A, expressed by Sf9 insect cells , with His, Flag labeled tag. ,
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2Areceptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2Areceptor[1].
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
Brexpiprazole-d8 is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2Areceptor antagonist (Ki=0.47 nM)[1][2].
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively .
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].
Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine . Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .
Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1][2].
Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2Areceptor with pIC50 and pKd of 8.73 and 9.3, respectively .
Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Cyamemazine-d6 is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM[1][2][3].
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2Areceptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2Creceptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
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