Search Result
Results for "
5-HT2B
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-147203
-
|
5-HT Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease .
|
-
-
- HY-126057S
-
|
Parasite
5-HT Receptor
|
Infection
|
(R)-Praziquantel-d11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].
|
-
-
- HY-103129
-
|
5-HT Receptor
|
Neurological Disease
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor 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 .
|
-
-
- HY-100851A
-
|
5-HT Receptor
|
Cardiovascular Disease
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
-
- HY-103094
-
|
5-HT Receptor
|
Inflammation/Immunology
|
LY266097 hydrochloride is a selective 5-HT2B receptor 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 .
|
-
-
- HY-14153
-
|
5-HT Receptor
Apoptosis
|
Metabolic Disease
Cancer
|
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C 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 .
|
-
-
- HY-14153A
-
SDZ-HTF-919; HTF-919
|
5-HT Receptor
Apoptosis
|
Neurological Disease
Metabolic Disease
|
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, 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 .
|
-
-
- HY-126057
-
|
Parasite
5-HT Receptor
|
Infection
|
(R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer .
|
-
-
- HY-103129A
-
|
5-HT Receptor
|
Neurological Disease
|
SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor 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 .
|
-
-
- HY-14153S
-
|
5-HT Receptor
Apoptosis
Isotope-Labeled Compounds
|
Metabolic Disease
Cancer
|
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C 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 .
|
-
-
- HY-103153
-
-
-
- HY-18596
-
|
5-HT Receptor
|
Neurological Disease
|
SB-215505 is a potent and subtype-selective 5-HT2B receptor 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 .
|
-
-
- HY-103135
-
|
5-HT Receptor
|
Neurological Disease
|
SB 206553 hydrochloride is a high affinity, selective and orally active 5-HT2B / 5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92) . SB 206553 possesses anxiolytic-like properties .
|
-
-
- HY-123480
-
|
5-HT Receptor
|
Neurological Disease
|
EGIS-7625 is a selective and competitive 5-HT2B inhibitor with pKi values of 9.0, 6.2, 7.7 for 5-HT2B, 5-HT2A, 5-HT2C, respective. EGIS-7625 partially attenuates m-chlorophenylpiperazine-induced hypomotility and hypophagia .
|
-
-
- HY-119946
-
-
-
- HY-W380450
-
Viloxazin; Emovit
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Viloxazine (Viloxazin) is a norepinephrine reuptake inhibitor, also a potent 5-HT2C agonist and 5-HT2B antagonist with an EC50 of 32 μM and an IC50 of 27 μM for 5-HT2C and 5-HT2B, respectively. The mechanism of action of Viloxazine predominantly involves serotonergic and noradrenergic pathways. Viloxazine can be used for researching depression .
|
-
-
- HY-125784
-
Viloxazin hydrochloride; Emovit hydrochloride
|
Others
|
Neurological Disease
|
Viloxazine hydrochloride is the hydrochloride salt form of Viloxazine (HY-W380450). Viloxazine (Viloxazin) hydrochloride is a norepinephrine reuptake inhibitor and a potent 5-HT2C agonist agent and 5-HT2B antagonist, EC50 for 5-HT2C b> is 32 μM, and the IC50 for 5-HT2B is 27 μM. Viloxazine hydrochloride's mechanism of action primarily involves serotonergic and noradrenergic pathways. Viloxazine hydrochloride is used in antidepressant research .
|
-
-
- HY-125784B
-
(S)-Viloxazin hydrochloride; (S)-Emovit hydrochloride
|
Others
|
Neurological Disease
|
(S)-Viloxazine hydrochloride is the isomer of Viloxazine hydrochloride (HY-125784). Viloxazine hydrochloride is the hydrochloride salt form of Viloxazine (HY-W380450). Viloxazine (Viloxazin) hydrochloride is a norepinephrine reuptake inhibitor and a potent 5-HT2C agonist agent and 5-HT2B antagonist,EC50 for 5-HT2C b> is 32 μM,and the IC50 for 5-HT2B is 27 μM. Viloxazine hydrochloride's mechanism of action primarily involves serotonergic and noradrenergic pathways. Viloxazine hydrochloride is used in antidepressant research .
|
-
-
- HY-153027
-
Methylergonovine; Ryegonovin free base; Spametrin F free base
|
5-HT Receptor
|
Endocrinology
|
Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. The distribution half-life of Methylergometrine is only 1-2 min. Methylergometrine can be used as an oxytocin to treat uterine atony .
|
-
-
- HY-15296
-
-
-
- HY-15419
-
|
5-HT Receptor
|
Neurological Disease
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
-
- HY-15419A
-
|
5-HT Receptor
|
Neurological Disease
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
-
- HY-15296A
-
FCE-21336 diphosphate
|
Dopamine Receptor
Autophagy
|
Endocrinology
Cancer
|
Cabergoline diphosphate is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
|
-
-
- HY-118010A
-
|
5-HT Receptor
|
Cardiovascular Disease
|
(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca 2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease .
|
-
-
- HY-W131725
-
|
5-HT Receptor
|
Cardiovascular Disease
|
(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca 2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease .
|
-
-
- HY-10559
-
APD125
|
5-HT Receptor
|
Neurological Disease
Cancer
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
-
- HY-14153AS
-
SDZ-HTF-919-13C,d3; HTF-919-13C,d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
|
-
-
- HY-15296S1
-
-
-
- HY-15296S
-
-
-
- HY-101369
-
|
5-HT Receptor
|
Neurological Disease
|
BW-723C86 is a potent and a selective 5-HT2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats .
|
-
-
- HY-15296R
-
|
Dopamine Receptor
Autophagy
|
Endocrinology
Cancer
|
Cabergoline (Standard) is the analytical standard of Cabergoline. This product is intended for research and analytical applications. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
|
-
-
- HY-W014208
-
AF-267B
|
Others
|
Others
|
NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors .
|
-
-
- HY-103110
-
ST1936
1 Publications Verification
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
-
- HY-103110A
-
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
-
- HY-103155
-
|
5-HT Receptor
|
Neurological Disease
|
SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease .
|
-
-
- HY-10792
-
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor 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 .
|
-
-
- HY-103154
-
|
5-HT Receptor
|
Neurological Disease
|
SB228357 is a selective, potent and orall active 5-HT2C/2B receptor 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 .
|
-
-
- HY-14148
-
|
Others
|
Neurological Disease
|
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 .
|
-
-
- HY-103120
-
|
5-HT Receptor
|
Neurological Disease
|
Org37684 is a highly potent 5-HT2C receptor 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 .
|
-
-
- HY-10457A
-
TD-5108 hydrochloride
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
|
-
-
- HY-110129
-
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor 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 .
|
-
-
- HY-10457
-
TD-5108
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
|
-
-
- HY-119103
-
|
5-HT Receptor
|
Neurological 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 .
|
-
-
- HY-103138A
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor 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-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects .
|
-
-
- HY-16729A
-
YKP10811 hydrochloride
|
5-HT Receptor
|
Inflammation/Immunology
|
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility .
|
-
-
- HY-103138
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT2C receptor 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-HT2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .
|
-
-
- HY-14546
-
Aripiprazole
Maximum Cited Publications
8 Publications Verification
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-18099A
-
E-52862 hydrochloride
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
|
-
-
- HY-118152
-
|
5-HT Receptor
|
Neurological Disease
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety .
|
-
-
- HY-145841
-
|
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-HT2A, 5-HT2B, and 5-HT2C with EC50 values of 1.7, 0.58, and 0.50 nM, respectively .
|
-
- HY-14546A
-
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-14147
-
BRL 24924
|
5-HT Receptor
|
Metabolic Disease
|
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist . Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study .
|
-
- HY-10895
-
SB 334867A
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
|
-
- HY-B1033
-
|
5-HT Receptor
Dopamine Receptor
Sodium Channel
|
Neurological Disease
|
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-HT7 receptor, 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 .
|
-
- HY-101365
-
|
5-HT Receptor
|
Neurological Disease
|
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 .
|
-
- HY-101365A
-
|
5-HT Receptor
|
Neurological Disease
|
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 .
|
-
- HY-156533A
-
|
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-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-HT Receptor
|
Neurological Disease
|
(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values ??for 5-HT2 receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research .
|
-
- HY-10895A
-
SB334867A free base
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
|
-
- HY-B1101
-
Pimetixene
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
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 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 .
|
-
- HY-B1101A
-
Pimetixene maleate
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
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 .
|
-
- HY-18099
-
S1RA
1 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
|
-
- HY-14546R
-
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-14147A
-
(S)-BRL 24924
|
5-HT Receptor
|
Metabolic Disease
|
(S)-Renzapride ((S)-BRL 24924) is the isomer of HY-14147 Renzapride. Renzapride is a 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride also is a 5HT2b and 5HT3 receptor antagonist. Renzapride can be used for constipation predominant irritable bowel syndrome (C-IBS) study .
|
-
- HY-105285
-
Neu-P11
|
Melatonin Receptor
5-HT Receptor
P2X Receptor
TRP Channel
Sodium Channel
|
Neurological Disease
|
Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities .
|
-
- HY-106136
-
PD-6735; LY-156735
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment .
|
-
- HY-132225
-
|
5-HT Receptor
|
Inflammation/Immunology
|
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 .
|
-
- HY-B1101AR
-
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
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 .
|
-
- HY-10564
-
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
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 .
|
-
- HY-N0049
-
|
Parasite
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
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.
|
-
- HY-109112
-
RP5063
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
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 .
|
-
- HY-10564S
-
MCI-9042-d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
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].
|
-
- HY-N0049R
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
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.
|
-
- HY-109112R
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
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 .
|
-
- HY-15543A
-
|
5-HT Receptor
|
Neurological Disease
|
CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. 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 .
|
-
- HY-15543
-
|
5-HT Receptor
|
Neurological Disease
|
CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. 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 .
|
-
- HY-134807
-
|
P2X Receptor
5-HT Receptor
Autophagy
|
Cancer
|
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
|
-
- HY-101009
-
Metitepine maleate; Ro-8-6837 maleate
|
5-HT Receptor
|
Neurological Disease
|
Methiothepin maleate is a potent and non-selective 5-HT2 receptor 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).
|
-
- HY-111491
-
Metitepine; Ro 8-6837
|
5-HT Receptor
|
Neurological Disease
|
Methiothepin is a potent and non-selective 5-HT2 receptor 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).
|
-
- HY-107836
-
Metitepine mesylate; Ro 8-6837 mesylate
|
5-HT Receptor
|
Neurological Disease
|
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor 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).
|
-
- HY-103124
-
|
5-HT Receptor
|
Neurological Disease
|
DOI hydrochloride is a serotonin 5-HT2A/2C receptor agonist with Ki values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A, h5-HT2C and h5-HT2B receptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice .
|
-
- HY-155117
-
-
- HY-145699
-
|
5-HT Receptor
|
Others
|
UCSF686 is a probe with which to study the function of the 5-HT5AR. UCSF686 loses affinity at 5-HT5AR (>10 000 nM) but not at 5-HT1AR, 5-HT2BR, and 5-HT7R. UCSF686 controls for off-target effects .
|
-
- HY-134494
-
|
GPR68
|
Neurological Disease
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .
|
-
- HY-117792
-
|
5-HT Receptor
|
Inflammation/Immunology
|
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. .
|
-
- HY-107624
-
ATC0175
1 Publications Verification
|
MCHR1 (GPR24)
|
Neurological Disease
|
ATC0175 is a potent, selective and orally active melanin-concentrating hormone 1 recepter antagonist with IC50s of 13.5, >10000 nM for MCH1R, MCH2R, respectively. ATC0175 shows antidepressant effects and anxiolytic effects in animal models. ATC0175 has the potential for the research of depression and/or anxiety disorders .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-15401A
-
|
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 |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-126057S
-
|
(R)-Praziquantel-d11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].
|
-
-
- HY-14153S
-
|
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C 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 .
|
-
-
- HY-14153AS
-
|
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
|
-
-
- HY-15296S1
-
|
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
|
-
-
- HY-15296S
-
|
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
|
-
-
- HY-10564S
-
|
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].
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: