COMPARATIVE THERMODYNAMICS OF OPIOID RECEPTOR-LIGAND INTERACTION IN THE BOVINE ADRENAL-MEDULLA MEMBRANES - EVIDENCE OF OPIOID SITE HETEROGENEITY

被引：4
作者：
BOURHIM, N
CANTAU, P
GIRAUD, P
CASTANAS, E
机构：
[1] FAC SCI AIN CHOCK,BIOCHIM BIOL MOLEC & CELLULAIRE LAB,CASABLANCA,MOROCCO
[2] FAC MED CRETE,EXPTL ENDOCRINOL LAB,IRAKLION,GREECE
来源：
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-PHARMACOLOGY TOXICOLOGY & ENDOCRINOLOGY | 1993年 / 105卷 / 03期
关键词：
D O I：
10.1016/0742-8413(93)90083-W
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
1. A marked dependence on temperature of agonist binding delta, mu and kappa1-3 opioid sites in the bovine adrenal medulla was observed, at the range of 0 to 37-degrees-C. These changes concern kinetic (k1) and equilibrium constants (K(d)), but not binding capacities (B(max)). 2. These dependences are different for each ligand and each opioid receptor, suggesting their molecular heterogeneity. 3. The comparative thermodynamics indicates that the interaction of opioid agonists with their receptor is exergonic (DELTAG-degrees < 0) and entropy driven (DELTAS-degrees > 0). 4. The comparison of Van't Hoff and Arrhenius plots indicates a discrete mechanism in the binding of each opioid receptor.
引用
收藏
页码：435 / 442
页数：8
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