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Results for "

5-HT2A agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (89) Adrenergic Receptor (10) Androgen Receptor (1) Apoptosis (4) Dopamine Receptor (33) Drug Metabolite (1) GABA Receptor (1) Histamine Receptor (1) Isotope-Labeled Compounds (7) mAChR (3) Parasite (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (2) Infection (3) Inflammation/Immunology (12) Metabolic Disease (7) Neurological Disease (78)

Inhibitors & Agonists

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153912

5-HT2A receptor agonist-3	5-HT Receptor	Others
5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a K_i of 2.5 nM, and with 124-fold selectivity for *5-HT2A* over the structurally similar 5-HT2C receptor .

HY-145393

5-HT2A receptor agonist-1	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-1 is a *5-HT2A* receptor agonist with the EC₅₀ of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders .

HY-103102

TCB2	5-HT Receptor	Neurological Disease
TCB2 is an agonist of serotonin *5-HT_2A* receptor.

HY-162176

5-HT2A agonist 2	5-HT Receptor	Others
5-HT2A agonist 2 (Compound 5) is a *5-HT_2A* agonist .

HY-145841

5-HT2A receptor agonist-2	5-HT Receptor	Cardiovascular Disease
5-HT2A receptor agonist-2 is a highly potent serotonin 5-HT2 receptor agonists. 5-HT2A receptor agonist-2 inspires 5-HT_2A, 5-HT_2B, and 5-HT_2C with EC₅₀ values of 1.7, 0.58, and 0.50 nM, respectively .

HY-156534

5-HT2A&5-HT2C agonist-1	5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC₅₀s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .

HY-169001

5-HT2A/5-HT2C inverse agonist 1	5-HT Receptor	Neurological Disease
5-HT2A/5-HT2C inverse agonist 1 is a potent and dual *5-HT2A* and 5-HT2C receptor 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 .

HY-163205

VU6067416	5-HT Receptor	Neurological Disease
VU6067416 is a potent and brain-penetrant *5-HT2A* agonist with an EC₅₀ of 189 nM .

HY-161511

LPH-5	5-HT Receptor	Neurological Disease
LPH-5 is a selective *5-HT2A* receptor agonist (EC₅₀=190 nM). LPH-5 works by selectively activating the *5-HT2A* receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the *5-HT2A* receptor. LPH-5 can be used to further explore the *5-HT2A* receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders .

HY-159831

Remlifanserin	5-HT Receptor	Others
Remlifanserin is a potent serotonin receptor (5-HT2A) inverse agonist .

HY-14557

Pimavanserin Maximum Cited Publications 12 Publications Verification ACP-103	5-HT Receptor	Neurological Disease
Pimavanserin is a selective inverse agonist of the *5-HT2A* receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-113008A

cis-Urocanic acid (Z)-Urocanic acid; cis-UCA	5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (K_d=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .

HY-10559

Nelotanserin 2 Publications Verification APD125	5-HT Receptor	Neurological Disease Cancer
Nelotanserin is a potent *5-HT_2A* inverse agonist, a moderately potent 5-HT_2C partial inverse agonist and a weak 5-HT_2B inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

HY-103145

PNU-22394 hydrochloride	5-HT Receptor	Neurological Disease
PNU-22394 hydrochloride is an agonist for 5-HT, with K_i of 6.1 and 10 nM, for 5-HT_2C and 5-HT_2A, respectively .

HY-135392

N-Desmethyl Pimavanserin AC-279	Drug Metabolite	Neurological Disease
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-155206

(+)-OSU6162	5-HT Receptor	Neurological Disease
(+)-OSU6162 is an stabilizer on dopaminergic and serotonergic brain signaling. (+)-OSU6162 is a partial agonist of 5-HT2A receptor. (+)-OSU6162 can be used for neurological research .

HY-117118A

AC-90179	5-HT Receptor	Neurological Disease
AC-90179 is a selective *5-HT2A* receptor inverse agonist (K_i = 2.1 nM) and 5-HT2C antagonist, a potential antipsychotic compound .

HY-101630

Deramciclane EGIS-3886	5-HT Receptor	Neurological Disease
Deramciclane has a high affinity for *5-HT_2A* and 5-HT_2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT_2C receptors without direct stimulatory agonist.

HY-113008AS

cis-Urocanic acid-13C3 (Z)-Urocanic acid-¹³C₃; cis-UCA-¹³C₃	Isotope-Labeled Compounds 5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid- ¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor 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-HT2A receptor[1].

HY-14557R

Pimavanserin (Standard)	5-HT Receptor	Neurological Disease
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-HT2A* receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-103403

(-)-OSU6162 hydrochloride PNU96391 hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
(-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at *5-HT2A* and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability .

HY-133024

Flumexadol	5-HT Receptor	Neurological Disease
Flumexadol is a selective and affinity 5-HT_2C receptor agonist with a K_i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT_2A receptor. Flumexadol is an orally active non-narcotic analgesic .

HY-156533A

5-HT2 agonist-1 free base	5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
5-HT2 agonist-1 (Compound 24) free base is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC₅₀s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .

HY-156533

5-HT2 agonist-1	5-HT Receptor	Cancer
5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC₅₀s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .

HY-156532C

(-)-5-HT2C agonist-3	5-HT Receptor	Neurological Disease
(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT_2C selective agonist with G_q signaling preference, with EC₅₀ values ??for 5-HT₂ receptors of 5-HT_2C: 103 nM; 5-HT_2B: 570 nM; *5-HT_2A: 72 nM. (-)-5-HT2C agonist*-3 can be used in antipsychotic research .

HY-A0095S

Flibanserin-d4 BIMT-17-d₄; BIMT-17BS-d₄	5-HT Receptor	Neurological Disease
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].

HY-128386

Cinitapride monotartrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Cinitapride monotartrate is a 5-HT_1A and 5-HT₄ agonist. Cinitapride monotartrate is also a *5-HT_2A* and D₂ antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia .

HY-103144

WAY 629 hydrochloride	5-HT Receptor	Neurological Disease
WAY 629 hydrochloride is a potent and selective 5-HT_2C agonist with EC₅₀s of 426, 260000 nM for 5-HT_2C and 5-HT_2A, respectively. WAY 629 hydrochloride decreases feeding behavior .

HY-103144A

WAY 629	5-HT Receptor	Neurological Disease
WAY 629 is a potent and selective 5-HT_2C agonist with EC₅₀s of 426, 260000 nM for 5-HT_2C and 5-HT_2A, respectively. WAY 629 decreases feeding behavior .

HY-14546

Aripiprazole 5+ Cited Publications OPC-14597	5-HT Receptor Dopamine Receptor	Infection Neurological Disease Inflammation/Immunology
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-HT2A* receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .

HY-14546A

Aripiprazole monohydrate OPC-14597 monohydrate	5-HT Receptor Dopamine Receptor	Infection Neurological Disease Inflammation/Immunology
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-HT2A* receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19 .

HY-19733

Lumateperone tosylate ITI-007 tosylate	5-HT Receptor Dopamine Receptor	Neurological Disease
Lumateperone (ITI-007) tosylate is a *5-HT2A* receptor 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 .

HY-157429

25N-N1-Nap	5-HT Receptor	Neurological Disease
25N-N1-Nap (compound 16) is a β-arrestin-biased *5-HT2A* agonist. 25N-N1-Nap antagonizes phencyclidine induced hyperactivity in Male C57BL/6 J mice .

HY-14546R

Aripiprazole (Standard) OPC-14597 (Standard)	5-HT Receptor Dopamine Receptor	Infection Neurological Disease Inflammation/Immunology
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-HT2A* receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .

HY-B0731

Perospirone hydrochloride SM-9018	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone hydrochloride (SM-9018) is an orally active antagonist of *5-HT_2A* receptor (K_i of 0.6 nM) and dopamine D₂ receptor (K_i of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT_1A receptor (K_i of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-17637

Lumateperone ITI-007	Dopamine Receptor 5-HT Receptor	Neurological Disease Cancer
Lumateperone (ITI-007) is an orally active *5-HT2A* receptor 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 .

HY-103105A

LP 12 hydrochloride hydrate	5-HT Receptor	Neurological Disease
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively) .

HY-112538

1-(1-Naphthyl)piperazine hydrochloride 1-NP hydrochloride; 1-NapHThylpiperazine hydrochloride	5-HT Receptor Apoptosis	Inflammation/Immunology Cancer
1-1-Naphthylpiperazine hydrochloride (1-NP hydrochloride; 1-Naphthylpiperazine hydrochloride) is a serotonergic derivative of quipazine, which is both an agonist for 5-HT1A receptor and an antagonist for *5-HT2A* receptor. 1-1-Naphthylpiperazine hydrochloride induces cell apoptosis. 1-1-Naphthylpiperazine hydrochloride prevents the immunosuppression and photocarcinogenesis .

HY-135392S

N-Desmethyl Pimavanserin-d9 hydrochloride AC-279-d₉ hydrochloride	Isotope-Labeled Compounds	Neurological Disease
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-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively .

HY-103105

LP 12 hydrochloride	5-HT Receptor	Neurological Disease
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively) .

HY-15780S

Brexpiprazole-d8 OPC-34712-d₈	5-HT Receptor Dopamine Receptor	Neurological Disease
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-HT2A receptor antagonist (Ki=0.47 nM)[1][2].

HY-B0731A

Perospirone SM-9018 free base	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone (SM-9018 free base) is an orally active antagonist of *5-HT_2A* receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of 5-HT_1A receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-14539

Clozapine 5+ Cited Publications HF 1854	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
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 K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and *serotonin 5HT2A* receptor with K_i*s of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist* at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-125641

AL-34662	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease
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 .

HY-14539A

Clozapine hydrochloride HF 1854 hydrochloride	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
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 K_i of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and *serotonin 5HT2A* receptor with K_i*s 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) .

HY-162423

CYB210010	5-HT Receptor Androgen Receptor	Neurological Disease
CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor 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 .

HY-133152

Brexpiprazole S-oxide DM-3411	5-HT Receptor Dopamine Receptor	Neurological Disease
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-HT_1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a *5-HT_2A* receptor antagonist with a K_i of 0.47 nM .

HY-21994

Org-12962 hydrochloride	5-HT Receptor	Neurological Disease
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT_2C receptor agonist and exhibits pEC₅₀ values of 7.01, 6.38 and 6.28 for 5-HT_2C, 5-HT_2A and 5-HT_2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model .

HY-B0731R

Perospirone hydrochloride (Standard)	5-HT Receptor Dopamine Receptor	Neurological 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-HT_2A* receptor (K_i of 0.6 nM) and dopamine D₂ receptor (K_i of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT_1A receptor (K_i of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-A0095

Flibanserin 2 Publications Verification BIMT-17; BIMT-17BS	5-HT Receptor	Neurological Disease Cancer
Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K_i values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research ^- .

Cat. No.	Product Name	Type

HY-15401A

WAY 163909 hydrochloride

Biochemical Assay Reagents

WAY-163909 hydrochloride is a potent 5-hydroxytryptamine receptor 2C (5-HT2C) agonist with an EC50 of 8 nM and a maximum efficacy of 90%, while displaying minimal activity at 5-HT2A receptors. Its selectivity is further demonstrated by Ki values of 10.5 nM for 5-HT2C, alongside higher Ki values for 5-HT2A (212 nM), 5-HT7 (343 nM), and 5-HT2B (485 nM), and it lacks significant activity at various other receptors.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0049

Nuciferine 4 Publications Verification	Structural Classification Alkaloids Aporphine Alkaloids other families Source classification Plants Isoquinoline Alkaloids	Parasite 5-HT Receptor Dopamine Receptor
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (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-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-N0049R

Nuciferine (Standard)	Structural Classification Alkaloids other families Source classification Plants	5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (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-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Cat. No.	Product Name	Chemical Structure

HY-113008AS

cis-Urocanic acid-13C3
cis-Urocanic acid- ¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor 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-HT2A receptor[1].

HY-15780S

Brexpiprazole-d8
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-HT2A receptor antagonist (Ki=0.47 nM)[1][2].

HY-A0095S1

Flibanserin-d4-1

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].

HY-133152S

Brexpiprazole S-oxide-d8

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-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].

HY-15780S1

Brexpiprazole-d8-1

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-HT2A receptor 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].

HY-A0095S

Flibanserin-d4
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].

HY-135392S

N-Desmethyl Pimavanserin-d9 hydrochloride
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-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively .

HY-32329S

Setiptiline-d3

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].

HY-B0031S2

Quetiapine-d8 fumarate

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].

HY-B0031S3

Quetiapine-d8 hemifumarate

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].

HY-B0031S4

Quetiapine hemifumarate-d8

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].

HY-B0031S5

Quetiapine-d4-1 fumarate

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 pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-14153S

Tegaserod-d11

Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, 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 .

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