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TEMPERATURE COEFFICIENTS OF AFFINITY CONSTANTS FOR THE BINDING OF ANTAGONISTS TO MUSCARINIC RECEPTORS IN THE RAT CEREBRAL CORTEX
Author(s) -
BARLOW R.B.,
BIRDSALL N.J.M.,
HULME E.C.
Publication year - 1979
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1979.tb13698.x
Subject(s) - muscarinic acetylcholine receptor , cerebral cortex , chemistry , receptor , acetylcholine , binding site , biophysics , antagonism , guinea pig , endocrinology , medicine , biology , biochemistry
1 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. 2 At 37°C the affinity constants agree with those determined by antagonism of acetylcholine‐induced contractions of the guinea‐pig ileum. 3 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. 4 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.