TEMPERATURE COEFFICIENTS OF AFFINITY CONSTANTS FOR THE BINDING OF ANTAGONISTS TO MUSCARINIC RECEPTORS IN THE RAT CEREBRAL-CORTEX

被引:32
作者
BARLOW, RB [1 ]
BIRDSALL, NJM [1 ]
HULME, EC [1 ]
机构
[1] NATL INST MED RES,DIV MOLEC PHARMACOL,LONDON NW7 1AA,ENGLAND
关键词
D O I
10.1111/j.1476-5381.1979.tb13698.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The temperature coefficients of binding of a series of muscarinic antagonists to their receptors in membrane preparations from the rat cerebral cortex has been examined. At 37°C the affinity constants agree with those determined by antagonism of acetylcholine‐induced contractions of the guinea‐pig ileum. The temperature‐dependence of the affinity constants is low; for the antagonists examined, the affinity constants at 0°C differ by less than a factor of 3 from those measured at 37°C. There are qualitative similarities between the estimates of the temperature coefficient of binding of the antagonists to receptors in ileum strips and in the cerebral cortex. 1979 British Pharmacological Society
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页码:587 / 590
页数:4
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