OPIATE RECEPTOR - MODEL EXPLAINING STRUCTURE-ACTIVITY-RELATIONSHIPS OF OPIATE AGONISTS AND ANTAGONISTS

被引:170
作者
FEINBERG, AP
CREESE, I
SNYDER, SH
机构
[1] JOHNS HOPKINS UNIV, SCH MED, DEPT PHARMACOL, BALTIMORE, MD 21205 USA
[2] JOHNS HOPKINS UNIV, SCH MED, DEPT EXPTL THERAPEUTICS, BALTIMORE, MD 21205 USA
[3] JOHNS HOPKINS UNIV, SCH MED, DEPT PSYCHIAT & BEHAV SCI, BALTIMORE, MD 21205 USA
关键词
D O I
10.1073/pnas.73.11.4215
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
A model of the opiate receptor was proposed which explained the unique potency of certain opiates such as etonitazene, fentanyl, phenazocine and oripavines, the role of N-allyl substituents in conferring antagonist properties and chemical features that afford pure antagonists. The model indicated molecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.
引用
收藏
页码:4215 / 4219
页数:5
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