Quetiapine

Quetiapine (ICI204636) 是一种 5-HT 受体激动剂，对人 5-HT1A 受体的 pEC50 为 4.77。

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5mg

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货号: ajci12576
CAS: 111974-69-7
别名: 喹硫平; ICI204636
分子式: C21H25N3O2S
分子量: 383.51
纯度: >98%
溶解度: ≥ 19.2 mg/mL in DMSO, ≥ 29.55 mg/mL in EtOH with gentle warming
储存: Store at -20°C
库存: 现货

Background

Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].

Quetiapine (ICI204636) is indicated for the treatment of schizophrenia as well as for the treatment of acute manic episodes associated with bipolar I disorder. The antipsychotic effect of quetiapine is thought by some to be mediated through antagonist activity at dopamine and serotonin receptors. Specifically the D1 and D2 dopamine, the alpha 1 adrenoreceptor and alpha 2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine (ICI204636) also has an antagonistic effect on the histamine H1 receptor.

参考文献:
[1]. Cross AJ, et al. Quetiapine and its metabolite norquetiapine: translation from in vitro pharmacology to in vivo efficacy in rodent models. Br J Pharmacol. 2016 Jan;173(1):155-66.