Sensitivity of histamine H-3 receptor agonist-stimulated [S-35]GTP gamma[S] binding to pertussis toxin

被引:80
作者
Clark, EA [1 ]
Hill, SJ [1 ]
机构
[1] QUEENS MED CTR,SCH MED,DEPT PHYSIOL & PHARMACOL,NOTTINGHAM NG7 2UH,ENGLAND
基金
英国医学研究理事会;
关键词
S-35]GTP gamma[S] binding; histamine H-3 receptor; G-protein; pertussis toxin;
D O I
10.1016/0014-2999(95)00800-4
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of histamine H-3 receptor-selective ligands on [S-35]guanosine 5'-o-(gamma-thio)triphosphate ([S-35]GTP gamma[S]) binding has been examined in rat cerebral cortical membranes. R(alpha)-Methylhistamine and N-alpha-methylhistamine produced a concentration-dependent stimulation of [S-35]GTP gamma[S] binding which was attenuated in the presence of the selective histamine H-3 receptor antagonist thioperamide. In addition, treatment of brain membranes with pertussis toxin abolished the histamine H-3 receptor agonist stimulated binding of [S-35]GTP gamma[S]. These results provide the first evidence that histamine H-3 receptors couple directly to a G(i)/G(o) protein in mammalian brain.
引用
收藏
页码:223 / 225
页数:3
相关论文
共 11 条
[1]   HISTAMINE H-3 RECEPTOR-BINDING SITES IN RAT-BRAIN MEMBRANES - MODULATIONS BY GUANINE-NUCLEOTIDES AND DIVALENT-CATIONS [J].
ARRANG, JM ;
ROY, J ;
MORGAT, JL ;
SCHUNACK, W ;
SCHWARTZ, JC .
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1990, 188 (4-5) :219-227
[2]  
BRADFORD MM, 1976, ANAL BIOCHEM, V72, P248, DOI 10.1016/0003-2697(76)90527-3
[3]   DIFFERENTIAL EFFECT OF SODIUM-IONS AND GUANINE-NUCLEOTIDES ON THE BINDING OF THIOPERAMIDE AND CLOBENPROPIT TO HISTAMINE H-3 RECEPTORS IN RAT CEREBRAL CORTICAL MEMBRANES [J].
CLARK, EA ;
HILL, SJ .
BRITISH JOURNAL OF PHARMACOLOGY, 1995, 114 (02) :357-362
[4]  
ENDOU M, 1994, J PHARMACOL EXP THER, V269, P221
[5]  
FREDHOLM BB, 1994, PHARMACOL REV, V46, P143
[6]   MUSCARINIC ACETYLCHOLINE RECEPTOR-STIMULATED BINDING OF GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE) TO GUANINE-NUCLEOTIDE-BINDING PROTEINS IN CARDIAC MEMBRANES [J].
HILF, G ;
GIERSCHIK, P ;
JAKOBS, KH .
EUROPEAN JOURNAL OF BIOCHEMISTRY, 1989, 186 (03) :725-731
[7]  
HILL SJ, 1990, PHARMACOL REV, V42, P45
[8]   PHARMACOLOGICAL CHARACTERIZATION OF ACETYLCHOLINE-STIMULATED [S-35] GTP-GAMMA-S BINDING MEDIATED BY HUMAN MUSCARINIC M1-M4 RECEPTORS - ANTAGONIST STUDIES [J].
LAZARENO, S ;
BIRDSALL, NJM .
BRITISH JOURNAL OF PHARMACOLOGY, 1993, 109 (04) :1120-1127
[9]  
LORENZEN A, 1993, MOL PHARMACOL, V44, P115
[10]  
SWEENEY MI, 1995, J NEUROCHEM, V64, P2034