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5-HT Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC71507 Blonanserin dihydrochloride
Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
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DC71506 Dehydroaripiprazole-d8
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole.
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DC71505 Cisapride monohydrate
Cisapride monohydrate is an orally and potent 5-HT4 receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut.
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DC71461 S-14506 hydrochloride
S-14506 hydrochloride is a potent 5-HT1A agonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.
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DC71221 CJ033466 Featured
CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect.
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DC71324 UCSF648
UCSF648 (Compound 5A6-48) is a chemical probe for the 5-HT5A serotonin receptor. UCSF648 weakly activates ADRA2A and MTNR1A.
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DC71323 F 14679
F 14679 is a prototypical 5-HT1A agonist with a pKi of 10.23. F 14679 induces large Ca2+ responses.
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DC71322 WAY-181187 oxalate
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
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DC11469 APD125(Nelotanserin) Featured
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
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DC9318 Piboserod Featured
Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.
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DC71250 LY393558
LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression.
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DC71227 MM 77 dihydrochloride
MM 77 dihydrochloride is a potent postsynaptic antagonist of the 5-HT1A receptor. MM 77 dihydrochloride exhibits anxiolytic-like activity.
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DC71224 LP 12 hydrochloride
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively).
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DC71213 LY-272015 hydrochloride
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
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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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