Cyamemazine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cyamemazine 是一种抗精神病药，其中含有吩噻嗪发色团，通常被用作抗焦虑药。Cyamemazine 是具有抗精神病活性的有效的 5-HT3 (Ki 为 12 nM), 5-HT2A (Ki 为 1.5 nM) 和 5-HT2C (Ki 为 75 nM) 受体拮抗剂。

Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.

Cyamemazine exhibits a high affinity for dopamine receptors, which is consistent with its antipsychotic activity. The antagonist activity of Cyamemazine at muscarinic receptors is consistent with its affinity for M1 (Ki = 13 nM), M2 (Ki = 42 nM), M3 (Ki = 321 nM), M4 (Ki = 12 nM), and M5 (Ki = 35 nM) receptors.

Cyamemazine behaves as an antagonist at the 5-HT3, 5-HT2C, and 5-HT2A receptors in 5-HT3-dependent contraction of isolated guinea pig ileum and bradycardic responses in rats, in 5-HT2C-dependent phospholipase C stimulation in the rat brain membrane, and in 5-HT2A-dependent contraction of isolated rat aorta rings and isolated guinea pig trachea. Cyamemazine antagonizes 5-HT3 and 5-HT2C receptors and that this effect is partially involved in its therapeutic activity in anxiety disorders. Acute administration of low doses of Cyamemazine can reduces extracellular dopamine and metabolite concentrations in rat striatum.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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3546-03-0

323.46

C19H21N3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (309.16 mM; 超声助溶 )

N#CC1=CC=C2SC=3C=CC=CC3N(C2=C1)CC(C)CN(C)C

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(-20℃)

With Ice Pack

≥ 2 years