氯氮平与大鼠脑内组胺H3受体的相互作用。
Interaction of clozapine with the histamine H3 receptor in rat brain.
作者信息
Rodrigues A A, Jansen F P, Leurs R, Timmerman H, Prell G D
机构信息
Department of Pharmacology, Mount Sinai School of Medicine of the City University of New York, N.Y. 10029, USA.
出版信息
Br J Pharmacol. 1995 Apr;114(8):1523-4. doi: 10.1111/j.1476-5381.1995.tb14934.x.
Abstract
We examined possible interactions between neuroleptics and the histamine H3 receptor and found an interaction of clozapine with this receptor. In competition binding experiments, using the H3 antagonist, [125I]-iodophenpropit, we observed a Ki of 236 +/- 87 nM. Functionally, clozapine was studied on the H3-mediated inhibition of [3H]-5-hydroxytryptamine ([3H]-5-HT) release from rat brain cortex slices. Clozapine acts as an antagonist with an apparent KB value of 79.5 nM.
摘要
我们研究了抗精神病药物与组胺H3受体之间可能存在的相互作用，发现氯氮平与该受体存在相互作用。在竞争结合实验中，使用H3拮抗剂[125I] - 碘苯丙胺，我们观察到其抑制常数（Ki）为236±87 nM。在功能方面，我们研究了氯氮平对H3介导的大鼠脑皮质切片中[3H] - 5 - 羟色胺（[3H] - 5 - HT）释放的抑制作用。氯氮平表现为拮抗剂，其表观解离常数（KB）值为79.5 nM。
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