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Clozapine

CAS No. : 5786-21-0

MCE 国际站：Clozapine

产品活性：Clozapine (HF 1854) 是用于研究精神分裂症的抗精神病药。Clozapine 对许多神经受体有高度的亲和力，是多巴胺受体的有效拮抗剂，K_i 值为 75 nM。Clozapine 抑制毒蕈碱 M1 受体和血清素 5HT2A 受体，K_i 值分别为 9.5 nM 和 4 nM。Clozapine 也是选择性的毒蕈碱 M4 受体的激动剂 (EC₅₀=11 nM)。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor  |  mAChR  |  Adrenergic Receptor  |  5-HT Receptor

In Vitro: Clozapine (HF 1854) is a D2 receptor antagonist with a K_i of 75 nM, blocks the serotonin 5HT2A receptor with a K_i of 4 nM, inhibits the muscarinic M1 receptor with a K_i of 9.5 nM, blocks α2-adrenoceptor with a K_i value of 51 nM.
?Clozapine (0-1 μM; 24 h) downregulates 5-HT₆ and upregulates 5-HT₇ receptors in HeLa cells.
?Clozapine is a full agonist at the muscarinic M4 receptor (EC₅₀=11 nM) expressed in CHO cells.

In Vivo: Clozapine (HF 1854) (25 mg/kg/day; i.p.; 21 days) shows antipsychotic effects in lysergic acid diethylamide-induced psychosis mouse model.

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