传统和新型止吐药与多巴胺D2和5-羟色胺3受体的差异相互作用。
Differential interactions of traditional and novel antiemetics with dopamine D2 and 5-hydroxytryptamine3 receptors.
作者信息
Hamik A, Peroutka S J
机构信息
Department of Neurology, Stanford University Medical Center, CA 94305.
出版信息
Cancer Chemother Pharmacol. 1989;24(5):307-10. doi: 10.1007/BF00304763.
The affinities of 11 drugs for both dopamine D2 and 5-hydroxytryptamine3 (5-HT3) receptor sites were determined in brain membranes. The five "traditional" antiemetics (chlorpromazine, prochlorperazine, droperidol, fluphenazine, and domperidone) displayed high affinity (less than 20 nM) for dopamine D2 receptors in corpus striatum but were inactive at 5-HT3 receptors. In contrast, five recently developed 5-HT3 antagonists (BRL 43694, ICS 205-930, zacopride, Lilly 278584, and MDL 72222) displayed nanomolar affinity for the 5-HT3 site but were inactive (greater than 10,000 nM) at the dopamine D2 receptor. Metoclopramide was unique among these agents in that it was similarly potent at dopamine D2 (240 +/- 60 nM) and 5-HT3 (120 +/- 30 nM) receptors.
在脑膜中测定了11种药物对多巴胺D2和5-羟色胺3（5-HT3）受体位点的亲和力。五种“传统”止吐药（氯丙嗪、异丙嗪、氟哌利多、氟奋乃静和多潘立酮）对纹状体中的多巴胺D2受体表现出高亲和力（小于20 nM），但对5-HT3受体无活性。相比之下，五种最近开发的5-HT3拮抗剂（BRL 43694、ICS 205-930、扎考必利、礼来278584和MDL 72222）对5-HT3位点表现出纳摩尔亲和力，但对多巴胺D2受体无活性（大于10,000 nM）。甲氧氯普胺在这些药物中是独特的，因为它对多巴胺D2（240±60 nM）和5-HT3（120±30 nM）受体具有相似的效力。
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