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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
DC76397 W-2451
W-2451 (NSC 294839) is a selective serotonin 5-HT2 receptor antagonist. W-2451 is promising for research of neurological disorders.
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DC76396 VU0631019
VU0631019 is a potent antagonist of 5-HT2B, with the IC50 of 29 nM. VU0631019 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans.
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DC76395 VU0530244
VU0530244 is a potent antagonist of 5-HT2B, with the IC50 of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans.
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DC76394 Trelanserin
Trelanserin (SL-650472) is a 5-HT receptor antagonist and also an effective in vitro smooth muscle contraction antagonist, competing against the contractions induced by sumatriptan with a pA2 of 8.17±0.36.
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DC76393 THRX-194556
THRX-194556 is a 5-HT4 receptor agonist. THRX-194556 can be used to study gastrointestinal functional disorders and Alzheimer’s disease.
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DC76392 Tenilapine
Tenilapine displays potent inverse agonist activity at rat and human 5-HT(2C) receptors.
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DC76391 Serotonin maleate
Serotonin hydrogen maleate is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrogen maleate is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
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DC76390 SAM-315
SAM-315 (WAY-255315) is a potent antagonist of 5-Hydroxytryptamine-6, with Ki and IC50 of 1.1 nM and 4.6 nM, respectively. SAM-315 significantly increases acetylcholine and glutamate release in hippocampus of the brain.
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DC76389 RS 67506 hydrochloride
RS 67506 hydrochloride is a 5-HT4 receptor agonist. The pKi value of RS 67506 hydrochloride for 5-HT4 in guinea pig striatum is 8.8. RS 67506 hydrochloride can be used in neuro-related research.
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DC76388 Ro4368554
Ro4368554 is a brain-penetrant and selective 5-HT6 antagonist that reverses memory deficits induced by scopolamine and tryptophan depletion. Ro4368554 can be utilized in research related to memory deficits.
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DC76387 Quetiapine sulfone
Quetiapine sulfone is a main metabolite of Quetiapine, and through the 15-lipoxygenase-1 pathway.
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DC76386 PUC-55
PUC-55 is a 5-HT6R antagonist with a Ki of 37.5 nM that induces neuronal autophagy by inhibiting the mTOR pathway. It holds potential for research in the field of neurological disorders.
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DC76385 PUC-10
PUC-10 is a 5-HT6 receptor antagonist with a Ki of 14.6 nM and an IC50 of 32 nM. In silico predictions suggest that PUC-10 is orally active and can cross the blood-brain barrier. PUC-10 can induce autophagy in SH-SY5Y cells by inhibiting the mTOR pathway. PUC-10 can be used in the research of neurological disorders.
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DC76384 p-MPPF
p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT. Aripiprazole N-oxide is formed from aripiprazole by the cytochrome P450 (CYP) isoforms CYP2D6 and CYP3A4.
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DC76383 Pellotine
Pellotine is an alkaloid that can be isolated from Lophophora. Pellotine is the inverse agonist for 5-HT7 receptor with an EC50 of 291 nM. Pellotine exhibits good affinity to 5-HT1DR and 5-HT6R with Ki of 117 nM and 170 nM. Pellotine reduces intracellular cAMP levels, thereby reducing neuronal excitability and neurotransmitter release.
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DC76382 Paynantheine
Paynantheine is an alkaloid with antinociceptive activity, which is found in Mitragyna speciosa. Paynantheine is also a 5-HT1AR and 5-HT2BR agonist that induces lower lip retraction and antinociception in rats.
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DC76381 Olanzapine ketolactam
Olanzapine ketolactam (compound 1) is the impurity of Olanzapine. Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT
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DC76380 NLX-266
NLX-266 is an orally active ERK1/2-biased 5-HT1A receptor agonist. NLX-266 can be used in the study of Parkinson's disease.
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DC76379 N-Desmethyl asenapine
N-Desmethyl asenapine is a metabolite of Asenapine.
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DC76378 MRS8209
MRS8209 is the antagonist for serotonin receptor with a Ki of 4.27 nM for 5-HT2BR. MRS8209 exhibits protective effect on pressure at airway opening (PAO), and can be used in research of pulmonary fibrosis.
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DC76377 Mirtazapine N-oxide
Mirtazapine N-oxide is a metabolite of Mirtazapine.
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DC76376 Methamnetamine hydrochloride
Methamnetamine (PAL-1046) hydrochloride is an amphetamine-based psychoactive substance. Methamnetamine hydrochloride causes excessive release of serotonin.
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DC76375 LY-272015
LY-272015 is an orally active, specific 5-HT2B receptor antagonist. LY-272015 completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
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DC76374 Jimscaline
Jimscaline (compound R-(-)2) is a 5-HT2A agonist and mescaline analogue that can be utilized in neurological research.
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DC76373 IHCH-7086
IHCH-7086 is a β-arrestin-biased 5-HT2A serotonin receptor agonist (Ki: 12.59 nM). IHCH-7086 recruits β-arrestin through activation of 5-HT2A receptors, thereby removing hallucinogenic activity. IHCH-7086 improves depression-like behavior in mice without hallucinogenic effects.
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DC76372 Hydrodolasetron
Hydrodolasetron is a metabolite of Dolasetron. Hydrodolasetron is more potent than Dolasetron in inhibiting nAChR. Hydrodolasetron is a 5-HT(3A)R blocker with an IC50 of 0.29 nM. Hydrodolasetron has antiemetic activity.
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DC76371 Flibanserin hydrochloride
Flibanserin hydrochloride (BIMT-17 hydrochloride) is an orally active 5-HT1A receptor agonist and 5-HT2A receptor antagonist with binding affinities Ki of 1 nM and 49 nM, respectively. Flibanserin hydrochloride also binds to dopamine D4 receptors with a Ki of 4-24 nM. Flibanserin hydrochloride has antidepressant and anxiolytic effects and can be used in the study of hypoactive sexual desire disorder (HSDD).
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DC76370 Etoperidone
Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively.
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DC76369 Ethylpropyltryptamine
Ethylpropyltryptamine (EPT) is a novel orally active psychoactive substance. Ethylpropyltryptamine (EPT) is predicted to be a partial agonist of the 5-HT2A receptor.
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DC76368 ECPLA
ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors.
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