GUANINE NUCLEOTIDE-INDUCED POSITIVE COOPERATIVITY IN MUSCARINIC-CHOLINERGIC ANTAGONIST BINDING

被引:23
作者
BOYER, JL
MARTINEZCARCAMO, M
MONROYSANCHEZ, JA
POSADAS, C
GARCIASAINZ, JA
机构
[1] NATL AUTONOMOUS UNIV MEXICO, INST FISIOL CELULAR, DEPT BIOENERGET, APARTADO POSTAL 70-600, MEXICO CITY 04510, DF, MEXICO
[2] INST NACL CARDIOL DR IGNACIO CHAVEZ, DEPT ENDOCRINOL, JUAN BADIANO 1, MEXICO 14080, DF, MEXICO
关键词
D O I
10.1016/0006-291X(86)90543-7
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
The effect of guanine nucleotides on the binding of [3H]Quinuclidinyl benzilate to heart muscarinic receptors was studied. It was observed that GTP and Gpp(NH)p increased antagonist binding. Scatchard transformation of the data resulted in curvilinear plots (downward concavity) consistent with positive cooperativity. Graphic analysis for cooperativity indicated that guanine nucleotides: (a) increased slightly but consistently the affinity for the antagonist (independent of receptor occupancy) and (b) induce positive cooperativity in the binding of [3H]QNB (dependent of receptor occupancy).
引用
收藏
页码:172 / 177
页数:6
相关论文
共 19 条
[11]  
LOWRY OH, 1951, J BIOL CHEM, V193, P265
[12]  
MARTIN MW, 1984, J PHARMACOL EXP THER, V230, P424
[13]  
MATTERA R, 1985, J BIOL CHEM, V260, P7410
[14]   DIFFERENTIAL REGULATION OF THE ALPHA-2-ADRENERGIC RECEPTOR BY NA+ AND GUANINE-NUCLEOTIDES [J].
MICHEL, T ;
HOFFMAN, BB ;
LEFKOWITZ, RJ .
NATURE, 1980, 288 (5792) :709-711
[15]   OBLIGATORY ROLE OF A TRIS CHOLINE ALLOSTERIC SITE IN GUANINE-NUCLEOTIDE REGULATION OF [H-3] L-QNB BINDING TO MUSCARINIC ACETYLCHOLINE-RECEPTORS [J].
MURPHY, KMM ;
SASTRE, A .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1983, 113 (01) :280-285
[16]  
PAPPANO AJ, 1984, FED PROC, V43, P2607
[17]   ROLE OF HORMONE RECEPTORS AND GTP-REGULATORY PROTEINS IN MEMBRANE TRANSDUCTION [J].
RODBELL, M .
NATURE, 1980, 284 (5751) :17-22
[18]   REGULATION OF MUSCARINIC CHOLINERGIC RECEPTORS BY GUANINE-NUCLEOTIDES IN CARDIAC TISSUE [J].
ROSENBERGER, LB ;
ROESKE, WR ;
YAMAMURA, HI .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1979, 56 (1-2) :179-180
[19]   THE ATTRACTIONS OF PROTEINS FOR SMALL MOLECULES AND IONS [J].
SCATCHARD, G .
ANNALS OF THE NEW YORK ACADEMY OF SCIENCES, 1949, 51 (04) :660-672