四氢异喹啉类化合物（salsolinol和四氢罂粟碱）的阿片受体结合及镇痛作用
Opiate receptor binding and analgesic effects of the tetrahydroisoquinolines salsolinol and tetrahydropapaveroline.
作者信息
Fertel R H, Greenwald J E, Schwarz R, Wong L, Bianchine J
出版信息
Res Commun Chem Pathol Pharmacol. 1980 Jan;27(1):3-16.
PMID:6244607
Abstract
Salosolinol and tetrahydropapaveroline bind to opiate receptors in rat brain with affinities of 6.2 and 1.95 x 10(-5)M respectively. Their ability to displace 3H-naloxone is decreased about 4-fold by 100 mM sodium ion. Both of these agents have antinociceptive effects when given to rats intraventricularly. Their potency is comparable to the enkephalins, and their effect is blocked by naloxone.
摘要
沙罗索林醇和四氢罂粟碱分别以6.2和1.95×10⁻⁵M的亲和力与大鼠脑中的阿片受体结合。它们置换³H-纳洛酮的能力因100 mM钠离子而降低约4倍。当给大鼠脑室内注射这两种药物时，它们都具有抗伤害感受作用。它们的效力与脑啡肽相当，且它们的作用被纳洛酮阻断。
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