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GPCR/G Protein——5-HT Receptor

5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. Type: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics,antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.

GPCR/G Protein——5-HT Receptor(335)

Cat. No. Product Name CAS No. Purity Chemical Structure
KE7489 (+)-OSU 6162 160777-43-5 ≥95%
KE2883 (E)-tri-Pcoumaroylspermidine 131086-78-7 ≥95%
KE7511 (R)-Mirtazapine 61364-37-2 ≥95%
KM19273 (Rac)-Lorcaserin

(Rac)-Lorcaserin ((Rac)-APD356 free base) 是一种减肥药和 5-HT2C 受体激动剂。

616201-80-0 97%
KM17999 (Rac)-Lorcaserin hydrochloride

(Rac)-Lorcaserin hydrochloride ((Rac)-APD356) 是一种减肥药和 5-HT2C 受体激动剂。

1431697-94-7
KM11127 (Rac)-Rotigotine hydrochloride

(Rac)-Rotigotine hydrochloride 是 Rotigotine 的外消旋体。Rotigotine 是 dopamine receptor 激动剂,是 5-HT1A receptor 的部分激动剂,以及 α2B-adrenergic receptor 的拮抗剂,Ki 值分别为 0.71 nM (dopamine D3 receptor),4-15 nM (D2,D5,D4 receptors),83 nM (dopamine D1 receptor)。

102120-99-0 98%
KM2472 (Rac)-WAY-161503

(Rac)-WAY-161503 是一种有效的,选择性的,高亲和力的 5-HT2C 受体激动剂,Ki 为 4 nM,EC50 为 12 nM。(Rac)-WAY-161503 对 HT2C 的亲和力分别比 5-HT2A 和 5-HT2B 受体高。(Rac)-WAY-161503 具有抗肥胖和抗抑郁的作用。

75704-24-4 ≥99%
KM3107 (S)-Amisulpride

(S)-Amisulpride (Esamisulpride) 是一种有效的多巴胺 D2/D3 受体拮抗剂。(S)-Amisulpride 是 5-HT7 受体的拮抗剂,KI 值为 900 nM。(S)-Amisulpride 具有抗精神和抗抑郁作用。

71675-92-8 99%
KE7515 (S)-Mirtazapine 61337-87-9 ≥95%
KM3924 (Z)-Thiothixene

(Z)-Thiothixene 是 serotonergic receptor 的拮抗剂,来自专利 US 20150141345 A1。

3313-26-6 99%
KE4250 1-Hydroxy-2,3,4,7-tetramethoxyxanthone 14103-09-4 ≥95%
KM13881 2'-O-Methylisoliquiritigenin

2'-O-Methylisoliquiritigenin 可从Arachis 中分离得到,可上调5-HT、NE、DAGABA 信号通路,对 NE 通路影响不大。

51828-10-5
KM13316 2-Methyl-5-HT

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) 是一种有效的选择性 5-HT3 受体激动剂。2-Methyl-5-HT 显示出抗抑郁样作用。

78263-90-8 98%
KE7516 2-Methyl-5-HT maleate 78263-91-9 ≥95%
KM7306 3-Hydroxy agomelatine

3-Hydroxy agomelatine 是 Agomelatine 的代谢产物。3-Hydroxy agomelatine 是 5-HT2C 受体拮抗剂,IC50 为 3.2 μM,Ki 为 1.8 μM。

166526-99-4
KM14872 4,4-Diphenylbutylamine hydrochloride

4,4-Diphenylbutylamine 对 5-HT2AH1 受体的 Ki 值分别为 2589 和 1670 nM。

22101-90-2
KM5310 4F 4PP oxalate

4F 4PP (oxalate) 是一种选择性 5-HT2A 拮抗剂,其亲和力几乎与酮色胺一样高 (Ki= 5.3 nM),但对 5-HT2C 位点的亲和力要低得多 (Ki= 620 nM)。

144734-36-1
KE7497 4i 930478-88-9 ≥95%
KM9604 5-Carboxamidotryptamine maleate

5-Carboxamidotryptamine maleate (5-CT maleate) 是一种有效的 5-HT1A5-HT1B5-HT1D5-HT55-HT7 受体激动剂。

74885-72-6 99%
KM7831 5-HT1A modulator 1

5-HT1A modulator 1 对 5HT1A,肾上腺素能 α1 和多巴胺 D2 受体具有非常高的亲和力,IC50 分别为 2±0.3 nM,10±3 nM 和 40±9 nM。

142477-34-7 97%
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