Receptor-binding profiles of neuroleptics.
Receptor-binding profiles of neuroleptics.
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抗精神病药的受体结合谱。
DOI：
10.1007/978-3-642-70140-5_2
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发表时间：
1985
期刊：
影响因子：
--
通讯作者：
J. Arnt
中科院分区：
文献类型：
--
作者：
J. Hyttel;J. Larsen;A. V. Christensen;J. Arnt
多巴胺受体阻滞剂似乎是抗精神病药的一个突出作用。然而，其他受体的阻断可能有助于治疗效果。已经测试了一系列精神抑制剂对DA D-1和D-2受体、5-羟色胺受体（S2）、α-肾上腺素受体（α 1）、组胺受体（H1）和毒蕈碱胆碱能受体的亲和力。根据对DA D-1和D-2受体的亲和力，可将抗精神病药物分为不同的类别。噻吨对D-1和D-2受体都有亲和力;吩噻嗪对D-2受体有亲和力，对D-1受体的亲和力低得多;而丁酰苯酮、二苯基丁基哌啶和苯甲酰胺仅对D-2受体有亲和力。关于对其他受体的亲和力，唯一一致的发现是对S2受体的亲和力。这些发现的临床意义是推测性的。在一些行为测试中，也观察到D-1/D-2分类，并且表明D-1受体激活是运动障碍的原因，并且噻吨类-由于其D-1受体阻断作用-比其他精神抑制剂诱导较少的运动障碍。
Dopamine-receptor blockade seems to be a prominent effect of neuroleptics. Blockade of other receptors might, however, contribute to the therapeutic effect. A series of neuroleptics have been tested for affinity to DA D-1 and D-2 receptors, serotonin receptors (S2), alpha-adrenoceptors (alpha 1), histamine receptors (H1), and muscarinic cholinergic receptors. According to the affinity to DA D-1 and D-2 receptors, neuroleptics can be divided into different groups. Thioxanthenes have affinity for both D-1 and D-2 receptors; phenothiazines have affinity for D-2 receptors and considerably lower affinity for D-1 receptors; and butyrophenones, diphenylbutylpiperidines, and benzamides have affinity only for D-2 receptors. Concerning affinity to other receptors the only consistent finding is affinity for S2 receptors. The clinical significance of these findings is speculative. In several behavioral tests the D-1/D-2 classification is also observed, and it is suggested that D-1-receptor activation is responsible for dyskinesia, and that thioxanthenes - due to their D-1 receptor blocking effect-induce less dyskinesia than other neuroleptics.
抗精神病药对脑多巴胺、血清素、α-肾上腺素能和组胺受体的作用与临床效力的关系。
DOI：
10.1176/ajp.137.12.1518
发表时间：
1980
期刊：
The American journal of psychiatry
影响因子：
--
作者：
Peroutka,SJ;Synder,SH
通讯作者：
Synder,SH