ANTIMUSCARINIC EFFECTS OF ANTIHISTAMINES - QUANTITATIVE-EVALUATION BY RECEPTOR-BINDING ASSAY
ANTIMUSCARINIC EFFECTS OF ANTIHISTAMINES - QUANTITATIVE-EVALUATION BY RECEPTOR-BINDING ASSAY
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DOI：
10.1254/jjp.43.277
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发表时间：
1987-03-01
期刊：
影响因子：
--
通讯作者：
TANAKA, C
中科院分区：
文献类型：
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作者：
KUBO, N;SHIRAKAWA, O;TANAKA, C
使用受体结合试验定量评价抗组胺药（H1和H2受体拮抗剂）的抗毒蕈碱作用。测定了27种H1受体拮抗剂、1种相关抗抑郁药和3种H2受体拮抗剂对牛大脑皮层H1受体和M受体的抑制常数（Ki值）。所有的H2受体拮抗剂检查显示非常低的亲和力的毒蕈碱受体。另一方面，一些H1受体拮抗剂（美喹他嗪、环庚嗪、氯马斯汀、二苯吡林、异丙嗪、高氯环嗪和阿利马嗪）对毒蕈碱受体具有高亲和力（Ki=5.0-38 nM）。另一组H1受体拮抗剂（美托洛尔明、特非那定、metapyrilen、氮卓斯汀、羟嗪和美克洛嗪）对毒蕈碱受体的亲和力较低（Ki = 3，600 - 30，000 nM）。因此，证明了抗组胺药的广泛抗毒蕈碱效力。这些结果将为抗组胺药的临床和实验应用提供有用的信息。
Quantitative evaluation of antimuscarinic effects of antihistamines (H1- and H2-receptor antagonists) was carried out using a receptor-binding assay. The inhibition constants (Ki values) of twenty seven H1-receptor antagonists, one related antidepressant and three H2-receptor antagonists at H1-receptors and muscarinic receptors in the bovine cerebral cortex were determined. All the H2-receptor antagonists examined showed very low affinity for the muscarinic receptors. On the other hand, some H1-receptor antagonists (mequitazine, cyproheptazine, clemastine, diphenylpyraline, promethazine, homochlorcyclizine and alimemazine) had high affinity for the muscarinic receptors (Ki=5.0-38 nM). Another group of H1-receptor antagonists (mepyramine, terfenadine, metapyrilen, azelastine, hydroxyzine and meclizine) had low affinity for the muscarinic receptors (Ki = 3,600-30,000 nM). Thus, a broad range of antimuscarinic potencies among the antihistamines was demonstrated. These results should provide helpful information with regard to the clinical and experimental use of antihistamines.