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5-HT Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC78554 F-14258
F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.
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DC78550 TGF-8027
TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression).
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DC78543 Y-36912
Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (Ki = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.
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DC78507 MW073
MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].
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DC78504 Elzasonan
Elzasonan (CP-448187) is a 5-hydroxytryptamine1B receptor antagonist. Elzasonan is used in research on depression.
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DC78493 rel-Asenapine hydrochloride
rel-Asenapine (rel-Org 5222) hydrochloride is a relative configuration of Asenapine hydrochloride. Asenapine (Org 5222) hydrochloride, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine hydrochloride can be used in the research of schizophrenia and bipolar disorder.
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DC78442 SDZ 208-912
SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia.
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DC78397 SEP-4199
SEP-4199 is a nonracemic 85:15 ratio of Aramisulpride and Esamisulpride. SEP-4199 exhibits significant differences in relative potency at two different receptors (5-HT7R and D2R) compared to the racemate. SEP-4199 exhibits antidepressant effects.
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DC78322 GSK-958108
GSK-958108 is a highly selective 5-HT1A receptor antagonist. GSK-958108 is commonly used in the study of neurological conditions.
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DC78317 MCI-225 hydrate hydrochloride
MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder.
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DC78216 EMD 386088 free base
EMD386088 free base is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 free base induces cell death. EMD386088 free base regulates the activity of ERK1/2. EMD386088 free base has the potential for the research of alzheimer's disease (AD) and schizophrenia.
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DC78186 (S)-Ebalzotan
(S)-Ebalzotan is the S-form of Ebalzotan. Ebalzotan is a 5-HT1A receptor agonist with activity in the study of depression. Ebalzotan can serve as a precursor to important active pharmaceutical ingredients. The synthesis of Ebalzotan involves a multi-enzyme catalyzed reduction reaction to obtain saturated primary or secondary alcohols in high yields and high enantioselectivity.
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DC78144 Ifoxetine
Ifoxetine (CGP 15210G) is an inhibitor of 5-HT reuptake. Ifoxetine specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine has antidepressant properties.
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DC78134 S-14489
S-14489 is an orally active selective postsynaptic 5-HT1A receptor antagonist with a pKi of 9.2. S-14489 can act as a 5-HT1A autoreceptor agonist and inhibit striatal 5-hydroxytryptophan accumulation. S-14489 can be used for the research of neurological disease.
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DC78029 RS130-180
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression.
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DC77912 Org 6582
Org 6582 is a competitive, selective, and long-acting 5-HT (Ki = 89 nM) uptake inhibitor. Org 6582’s inhibitory effect on 5-HT uptake can last for more than 48 hours. Org 6582 can be used for research on depressive disorders.
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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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