RECEPTOR-BINDING AT 2 DIFFERENT TEMPERATURES TO DISCRIMINATE AGONIST AND ANTAGONIST BEHAVIOR OF ADENOSINE-A1-RECEPTOR LIGANDS IN RAT-BRAIN

被引:8
作者
BOREA, PA [1 ]
VARANI, K [1 ]
MALAGUTI, V [1 ]
GILLI, G [1 ]
机构
[1] UNIV FERRARA,DIPARTMENTO CHIM,I-44100 FERRARA,ITALY
关键词
D O I
10.1111/j.2042-7158.1991.tb03197.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The inhibitory binding constants, K(i), at the adenosine A(l) receptor in rat brain have been measured at 0 and 25-degrees-C for 25 typical ligands. The K(i) ratios at the two temperatures are greater and smaller than unity for adenosine agonists and xanthine antagonists, respectively. These results suggest that two-temperature measurements of in-vitro K(i) constants represent a simple method of discriminating between in-vivo agonistic and antagonistic behaviour of A(l) adenosine receptor ligands.
引用
收藏
页码:866 / 868
页数:3
相关论文
共 8 条
[1]   ADENOSINE RECEPTORS IN BRAIN MEMBRANES - BINDING OF N6-CYCLOHEXYL[H-3]ADENOSINE AND 1,3-DIETHYL-8-[H-3]PHENYLXANTHINE [J].
BRUNS, RF ;
DALY, JW ;
SNYDER, SH .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1980, 77 (09) :5547-5551
[2]  
CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
[3]  
CREESE I, 1985, NEUROTRANSMITTER REC, P129
[4]  
GOODMAN RR, 1982, MOL PHARMACOL, V21, P329
[5]   AGONIST AND ANTAGONIST BENZODIAZEPINE RECEPTOR INTERACTION INVITRO [J].
MOHLER, H ;
RICHARDS, JG .
NATURE, 1981, 294 (5843) :763-765
[6]   LIGAND - A VERSATILE COMPUTERIZED APPROACH FOR CHARACTERIZATION OF LIGAND-BINDING SYSTEMS [J].
MUNSON, PJ ;
RODBARD, D .
ANALYTICAL BIOCHEMISTRY, 1980, 107 (01) :220-239
[7]  
MURPHY KMM, 1982, MOL PHARMACOL, V22, P250
[8]   FUNDAMENTAL DIFFERENCE BETWEEN THE MOLECULAR-INTERACTIONS OF AGONISTS AND ANTAGONISTS WITH THE BETA-ADRENERGIC-RECEPTOR [J].
WEILAND, GA ;
MINNEMAN, KP ;
MOLINOFF, PB .
NATURE, 1979, 281 (5727) :114-117