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5-HT Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC71160 Lerisetron
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats.
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DC71084 ML 10302
ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.
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DC71022 CP 93129 dihydrochloride
CP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.
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DC9322 Ramosetron (Hydrochloride) Featured
Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.
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DC45564 F13714 fumarate Featured
F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress.
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DC8483 SB-399885 HCl Featured
Potent, brain penetrant, orally active 5-HT6 antagonist. Displays > 200-fold selectivity for 5-HT6 over other 5-HT receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human 5-HT6 receptors respectively).
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DC8613 Vortioxetine (Lu AA21004) Featured
Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
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DC8288 Vortioxetine hydrobromide Featured
Vortioxetine Hcl (Lu AA21004 Hcl) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
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DC9932 YL-0919 Featured
YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.
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DC70850 TPN672
TPN672 (TPN 672) a novel antipsychotic compound with high affinity for serotonin and dopamine receptors 5-HT1AR, (Ki=0.23 nM), 5-HT2AR (Ki=2.58 nM) as well as moderate affinity for D3R (Ki=11.55 nM) and D2R (Ki=17.91 nM).TPN672 acted as a potent 5-HT1AR agonist, D2R/D3R partial agonist, and 5-HT2AR antagonist in vitro functional assays.TPN672 displayed robust antipsychotic efficacy in rodent models (e.g., blocking phencyclidine-induced hyperactivity), significantly better than aripiprazole, and ameliorated negative symptoms and cognitive deficits in the sociability test, dark avoidance response, Morris water maze test, and novel object recognition test.
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DC70721 PZ-1361
PZ-1361 is a potent and selective 5-HT7 receptor antagonist with Ki of 33 nM, exhibit significant in vivo antidepressant and pro-cognitive properties in rodents.
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DC70468 GSK-588045
GSK-588045 is a potent and selective 5-HT1A/B/D receptor antagonist with Ki of 9.5/8.8/9.8, respectively; exhibits high selectivity over human hERG potassium channels, favorable pharmacokinetics, and excellent activity in vivo in rodent pharmacodynamic (PD) models; demonstrates potential as a faster acting antidepressant/anxiolytic with reduced side-effect burden.
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DC70215 ASP2205
ASP2205 (ASP2205 fumarate) is a potent, selective 5-HT2C receptor agonist with EC50 of 0.85/2.5 nM for human/rat 5-HT2C in the intracellular Ca2+ mobilization assays, respectively.ASP2205 showed partial agonistic action on human 5-HT2A receptor with EC50 of 96 nM, no agonistic action against 5-HT2B.ASP2205 (0.1-1 mg/kg, i.d.) significantly elevated the leak point pressure (LPP) in anesthetized rats in a dose-dependent manner.ASP2205 is a more potent and selective 5-HT2C receptor agonist than lorcaserin.
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DC70177 AGH-192
AGH-192 is a potent, selective, orally bioavailable 5-HT7 receptor agonist with Ki of 4 nM.AGH-192 displays excellent water solubility, high selectivity over related CNS targets, high metabolic stability, oral bioavailability and low cytotoxicity.AGH-192 could crosses blood-brain barrier to a high extent.AGH-192 alleviates the symptoms of neuropathic pain in a mouse model.
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DC9705 GSK163090 Featured
GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of  9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.
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DC49611 5-HT6/5-HT2AR antagonist-1
5-HT6/5-HT2AR antagonist-1 is a potent dual 5-HT6/5-HT2AR antagonist with Ki values of 11 nM and 39 nM, respectively.
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DC49610 Gentisein
Gentisein (NSC 329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM.
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DC49609 MS 245 oxalate
MS 245 oxalate is a potent antagonist of 5-HT6 receptor with a Ki of 2 nM.
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DC49607 CGS 12066 dimaleate
CGS 12066 (dimaleate) dimaleate is a selective 5-HT1B receptor agonist with an IC50 of 51 nM.
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DC49606 Sumatriptan
Sumatriptan (GR 43175 free base) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research.
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DC4147 Prucalopride Featured
Prucalopride is a selective, high affinity 5-HT receptor agonistfor 5-HT4a and 5-HT4b with Ki of 2.5 nM and 8 nM, respectively.
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DC28414 p-MPPI hydrochloride Featured
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
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DC49010 RS 39604
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites.
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DC48667 Tegaserod
Tegaserod is a serotonin receptor 4 agonist (HTR4) used in the treatment of irritable bowel syndrome (IBS). Anti-tumor activity.
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DC48645 5-HT2A receptor agonist-1
5-HT2A receptor agonist-1 shows the agonist activity at the 5-HT2A receptor with an EC50 of 5.54 nM.
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DC48638 UCSF678
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR.
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DC48606 UCSF686
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.
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DC9979 PRX-08066 Featured
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
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DC10309 Tianeptine Featured
Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.
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DC10537 8-OH-DPAT Featured
8-OH-DPAT is a research chemical of the aminotetralin chemical class and has been widely used to study the function of the 5-HT1A receptor.
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