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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
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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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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DC9313 Sarpogrelate (hydrochloride) Featured
Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.
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DC8334 RS-127445 Featured
RS-127445 is a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.
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DC7268 Risperidone(R 64 766)
Risperidone(R 64 766) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM).
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DC8795 Pimavanserin(ACP-103) Featured
Pimavanserin(ACP-103) is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.
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DC9059 Olanzapine Featured
Olanzapine(LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
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DC7884 LY310762 Featured
LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
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DC7710 Lasmiditan (COL-144; LY573144) Featured
Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.
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DC9260 Eptapirone Featured
Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family.
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DC11399 AVN-492 Featured
AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
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DC7494 SB-242084 HCl Featured
5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2Breceptors respectively. Also displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.
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DC72327 Tetrahydro-β-carboline
Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 µM.
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DC72181 Oxetorone fumarate
Oxetorone fumarate is a non-selective, orally active serotonin antagonist. Oxetorone fumarate is an antimigraine agent.
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DC72180 Nefazodone
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of drug-drug interaction. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice.
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DC41002 5-HT1A modulator 2 hydrochloride
5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT, is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding.
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DC72031 GR-46611
GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia.
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DC71751 SB 258741 hydrochloride
SB 258741 hydrochloride is a specific 5-HT7 receptor antagonist and can be used for the research of schizophrenia.
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DC71750 Sarpogrelate
Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate (MCI-9042) increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease.
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DC71749 EMD386088
EMD386088 is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 induces cell death. EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.
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DC71748 Brexpiprazole hydrochloride
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
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DC71509 Ziprasidone mesylate
Ziprasidone (CP-88059) mesylate, an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor 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).
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DC71508 Ziprasidone mesylate trihydrate
Ziprasidone (CP-88059) mesylate trihydrate, an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor 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).
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