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Home > Inhibitors & Agonists > GPCR > 5-HT Receptor

5-HT Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC49608 RS 67333 hydrochloride Featured
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.
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DC29051 Perospirone Featured
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic drug and has the potential for schizophrenic disease treatment.
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DC48644 Zacopride hydrochloride Featured
Zacopride hydrochloride is a potent antagonist of 5-HT3 receptor with a Ki of 0.38 nM. Zacopride hydrochloride is also a agonist of 5-HT4 receptor with a Ki of 373 nM. Zacopride hydrochloride has anxiolytic activity. Zacopride hydrochloride has the potential for the research of Schizophrenia.
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DC71747 Aripiprazole monohydrate Featured
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.
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DC70176 AGH-107 Featured
AGH-107 is a potent, selective 5-HT7 receptor agonist with Ki of 6 nM and EC50 of 19 nM, 176-fold selectivity over 5-HT1AR.AGH-107 exhibited high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.
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DC8755 WAY 100635 Hydrochloride Featured
DC72326 Tabernanthalog Featured
Tabernanthalog is a water-soluble, non-hallucinogenic and non-toxic analogue of ibogaine. Tabernanthalog is a 5-HT2A agonist. Tabernanthalog is found to promote structural neural plasticity, reduce alcohol- and heroin-seeking behaviour, and produce antidepressant-like effects in rodents.
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DC73369 VU6047534
VU6047534 is a selective, peripherally restricted 5-HT2B partial agonist with IC50 of 480 nM in radioligand binding assays.
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DC73368 TZB-30878
TZB-30878 is a potent, selective, orally bioavailable 5-HT1A agonist and 5-HT3 antagonist, selectively binds to human 5-HT1A and 5-HT) receptors with Kd values of 0.68 and 8.90 nM, respectively.
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DC73367 PZ-1922
PZ-1922 is a potent, triple-acting 5-HT6R/5-HT3R antagonist and MAO-B reversible inhibitor with Ki of 17/0.45 nM (5-HT6R/5-HT3R), and pIC50 of 8.93 for MAO-B.
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DC73366 NU-1223
NU-1223 is a β carboline analog of alstonine and serotonin 5-HT2C receptor agonist, blocks phencyclidine and amphetamine-induced hyperactivity in subchronic phencyclidine mice.
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DC73365 NH300094
NH300094 is a potent antagonist of 5-HT receptors and dopamine receptors with IC50 of 0.47 nM, 1.04 nM, 11.71 nM and 31.55 nM for 5-HT2A, D2L, D2S and D3 receptors, respectively.
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DC73364 E-6801
E-6801 is a potent, selective 5-HT6 receptor partial agonist of 5-HT6 receptor with pKi of 8.46, cAMP formation EC50 of 8.02.
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DC73363 CSTI-300
CSTI-300 (SMP-100) is a potent, selective 5-HT3 receptor partial agonist with high affinity for human and rat 5-HT3 receptor (Ki=2.0 nM).
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DC73362 ASP5736
AS5736 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 3.6, 1.7 and 4.4 nM against human, rat, mouse 5-HT5A receptors, respectively.
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DC73361 AS2674723
AS2674723 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.75, 0.67 and 1.9 nM against human, rat, mouse 5-HT5A receptors, respectively.
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DC73360 AS2030680
AS2030680 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.58, 1.1 and 2.6 nM against human, rat, mouse 5-HT5A receptors, respectively.
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DC73359 25B-NBOMe
25B-NBOMe is a highly selective 5-HT2A receptor agonist with Ki of 0.05 nM, 100-fold selective over 5-HT2C (Ki=4.6 nM).
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DC9915 PF04995274,PF 04995274 Featured
PF-04995274 is a 5-HT4 receptor partial agonist. It thought to act centrally as a pro-cognitive agent that being developed for the treatment of Alzheimer's disease (AD).
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DC4102 SB-269970,SB 269970 Featured
SB269970 is a potent and selective 5-HT7 receptor antagonist.
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DC70441 GR-127935 Featured
GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor; displays >100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types; blocks porcine carotid vascular response to sumatriptan in vivo; orally bioavailable and centrally active.
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DC11422 Lumateperone Tosylate Featured
Lumateperone 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 SERT blocker (Ki = 61 nM).
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DC71510 Ansofaxine hydrochloride Featured
Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
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DC7583 Idalopirdine(Lu-AE-58054) Featured
Lu AE58054 is an in-vitro potency and selectivity, in-vivo binding affinity and effect of the 5-HT(6)R antagonist with a Ki value of 0.83 nM.
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DC72614 SB-699551
SB699551 is a potent, selective 5-HT5A receptor antagonist with pKi of 8.3, >100-fold selectivity over 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors. SB699551 also is a novel PSMD4/Rpn10 inhibitor, decreases cell viability in MM cell lines.
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DC72613 3-AQC
3-AQC, a piperazinylquinoxaline derivative, is a potent and competitive 5-HT3 receptor antagonist.
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DC72612 RS-102221
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.
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DC72611 CP-135807
CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research.
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DC9150 Tianeptine sodium salt Featured
Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.
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DC8354 Intepirdine (SB-742457, RVT-101) Featured
SB-742457(RVT-101) is a selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects.
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