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Cyamemazine

CAS No. : 3546-03-0

MCE 站：Cyamemazine

产品活性：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 (K_i 为 12 nM), 5-HT_2A (K_i 为 1.5 nM) 和 5-HT_2C (K_i 为 75 nM) 受体拮抗剂。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: 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 (K_i = 13 nM), M₂ (K_i = 42 nM), M₃ (K_i = 321 nM), M₄ (K_i = 12 nM), and M₅ (K_i = 35 nM) receptors.

In Vivo: Cyamemazine behaves as an antagonist at the 5-HT₃, 5-HT_2C, and 5-HT_2A receptors in 5-HT₃-dependent contraction of isolated guinea pig ileum and bradycardic responses in rats, in 5-HT_2C-dependent phospholipase C stimulation in the rat brain membrane, and in 5-HT_2A-dependent contraction of isolated rat aorta rings and isolated guinea pig trachea. Cyamemazine antagonizes 5-HT₃ and 5-HT_2C 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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