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氯氮平-d8是化合物氯氮平的氘标记形式。氯氮平被认为优先结合D4DR（D4-多巴胺）和SR-2（5HT | 2 | 5-羟色胺受体），并充当弱D1和D2拮抗剂。氯氮平也据报道与SR-2（5HT | 2 |），SR-6（5HT | 6 |）和SR-7（5HT | 7 |受体）结合。据报道，氯氮平的两种主要代谢物是N-去甲基氯氮平（标记的化合物； sc-219117）和氯氮平N-氧化物。另外，据报道反相HPLC是鉴定氯氮平及其两种主要代谢物的方法。在研究通过将氯氮平氧化为反应性亚硝酸根离子诱导家兔中性粒细胞凋
Clozapine-d8 is a deuterium-labeled version of the compound Clozapine . Clozapine is noted to bind preferentially to D4DR (D4-dopamine) and SR-2 (5HT|2|-serotonin receptors) and acts as a weak D1 and D2 antagonist. Clozapine is also reported to bind with the SR-2 (5HT|2|), SR-6 (5HT|6|) and SR-7 (5HT|7|receptors). Two major metabolites of Clozapine are reported to be N-Desmethyl Clozapine (labeled compound; sc-219117) and Clozapine N-oxide . Additionally, reversed-phase HPLC has been reported as a method of identification of Clozapine and its two major metabolites. In studies investigating the induction of neutrophil apoptosis in rabbits by oxidation of Clozapine into reactive nitrenium ion, it was noted that Clozapine increased the rate of neutrophil release from bone marrow while also affecting the neutrophil half-life in the peripheral blood stream of rabbits.
| pKa值 | pKₐ: 7.5, pKₐ: 7.33 (Predicted) (unlabeled) |
|---|---|
| Ki Data | Histamine H1 Receptor: Ki= 0.57 nM (human); mAChR M1: Ki= 0.98 nM (human); α2C-AR: Ki= 1.14 nM (human); SR-2A: Ki= 1.2 nM (human); SR-2C: Ki= 3.16 nM (human) (unlabeled) |
| IC50 | SR-2A: IC₅₀= 3 nM (bovine); AdrenergIC₅₀eceptor α-1: IC₅₀= 4 nM (rat); SR-2A: IC₅₀= 4.2 nM (human); Histamine H1 Receptor: IC₅₀= 4.91 nM (human); SR-2C: IC₅₀= 6.04 nM (human) (unlabeled) |
H301: 吞咽会中毒
H341: 怀疑引起遗传缺陷
H361: 怀疑破坏生育力或未出生的孩子
P201: 使用前获取特殊说明
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P281: 根据需要使用个人防护设备。
L2207782
危险品化学品经营许可证（带存储）