Quetiapine
Quetiapine 是一种 5-HT 受体激动剂,对人 5-HT1A 的 pEC50 值为 4.77。Quetiapine 是多巴胺受体 (dopamine receptor) 拮抗剂,对人 D2 的 pIC50 值为 6.33。Quetiapine 对人 D2,HT1A,5-HT2A,5-HT2C 受体具有中高等亲和力,pKi 值为 7.25,5.74,7.54,5.55。具有抗抑郁和抗焦虑作用。
中文名:喹硫平
英文名:Quetiapine; ICI204636
CAS 号: 111974-69-7
分子式:C₂₁H₂₅N₃O₂S
分子量:383.51
纯度:>98.0%
Description | 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]. |
Target | 5-HT1A Receptor;D2 Receptor |
In Vitro | 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. |
References | [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. |
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