氯氮平对[^3H]QNB与鼠前脑匀浆特异性结合的影响  

Effects of clozapine on muscarinic cholinoreceptor binding in rat forebrain

作　　者：耿德勤[1,2] 胡刚[1,2] 姚兵 

机构地区：[1]徐州医学院附属医院 [2]徐州医学院神经药理研究室

出　　处：《临床精神医学杂志》1998年第2期74-76,共3页Journal of Clinical Psychiatry

基　　金：江苏省自然科学基金

摘　　要：为探讨氯氮平与毒蕈碱样胆碱受体结合的特性，比较其拮抗胆碱受体的强度，将不同浓度的氯氮平、阿托品、多虑平、酚妥拉明分别与含有标记配基［３Ｈ］—二苯羟乙酸奎宁酯（３Ｈ—ＱＮＢ）的鼠前脑匀浆进行放射配基结合分析实验。结果发现，氯氮平对毒蕈碱样受体有较强的结合能力，其强度低于阿托品，高于多虑平，Ｋｉ为１６０ｎｍｏｌ／Ｌ。作者认为，氯氮平拮抗胆碱能受体的能力，与其抗精神病药理作用机制有关。Objective:To study the affinity of clozapine to muscarinic acetylcholine receptors in the forebrain of rats and the inhibitory potency of clozapine, atropine, doxepine and regitine on QNB specific binding sites. Method:The radio-ligand QNB recepter assays of clozapine, atropine, doxepine and regitine in rat forebrain homogenates were performed. Results:Clozapine was a more potent muscarinic antagonist as compared to doxepin but was less potent than atropine.Its Ki was 160nmol/L. Discussion:The authors viewed that the anti-muscarinic effect of clozapine was related to its antipsychotic effects, especially for negative symptoms in chronic schizophrenic .

关 键 词：氯氮平 QNB 毒蕈碱样受体 鼠脑 

分 类 号：R971.4[医药卫生—药品] R965.2[医药卫生—药学]