OPIATE RECEPTOR-BINDING AFFECTED DIFFERENTIALLY BY OPIATES AND OPIOID PEPTIDES
OPIATE RECEPTOR-BINDING AFFECTED DIFFERENTIALLY BY OPIATES AND OPIOID PEPTIDES
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DOI：
10.1016/0014-2999(79)90142-0
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发表时间：
1979-01-01
影响因子：
5
通讯作者：
SNYDER, SH
中科院分区：
文献类型：
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作者：
CHILDERS, SR;CREESE, I;SNYDER, SH
不同的阿片类药物取代几种~3H-阿片类配体与大鼠脑膜结合的效力因配体的性质而异。阿片类拮抗剂、阿片肽和某些激动剂(埃托啡、左旋吗啡和非那可辛)在取代~3H-阿片或~3H-蛋氨酸脑啡肽结合方面表现出相似的亲和力，而其他激动剂(如吗啡和羟吗啡)则相当(20-50倍)。与~3H-二氢吗啡的结合相比，~3H-脑啡素的取代作用更弱。这些激动剂以浅的置换曲线竞争~3H-脑啡肽的结合，在钠存在下取代~3H-纳洛酮的结合作用大大减弱。这些激动剂与其他阿片类药物的不同之处在于，它们的C环部分具有相对亲水性的成分，这可能为药物与阿片受体的不同相互作用提供基础。
The potencies of various opiates in displacing several 3H-opiate ligands'' binding to rat brain membranes vary depending on the nature of the ligand. Whereas opiate antagonists, as well as the opioid peptides and some agonists (etorphine, levorphanol and phenazocine) display similar affinities in displacing either 3H-opiate or 3H-methionine enkephalin binding, other agonists (such as morphine and oxymorphone) are considerably (20-50 .times.) weaker in displacing 3H-enkaphalin than 3H-dihydromorphine binding. These agonists compete for 3H-enkephalin binding with shallow displacement curves, and are greatly weakened in displacing 3H-naloxone binding in the presence of Na. These agonists differ from the other opiate classes by possessing a relatively hydrophilic component in their C-ring moieties which may provide a basis for the differential interactions of drugs with the opiate receptor.