Regulation of the solubilized bovine cerebral cortex muscarinic receptor by GTP and Na+.

Abstract:

:The muscarinic acetylcholine receptor was solubilized, in a sensitive form for GTP and Na+, from bovine cerebral cortex using a zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio]-1-propane sulfonate. The solubilized muscarinic receptor displayed characteristics as follows: (1) high affinity to nanomolar concentration of Z-[3H]quinuclidinyl benzilate; (2) muscarinic agonists and antagonists had similar inhibitory potencies as on the membrane-bound receptor; (3) without Na+, GTP did not significantly alter the binding affinity of muscarinic agonists and antagonists; (4) GTP in the presence of Na+, selectively decreased the affinity of muscarinic agonists, carbamylcholine and oxotremoline, but not the antagonist binding affinity; (5) Na+ in the absence or presence of GTP, reduced both muscarinic agonist and antagonist affinities.

authors

Kuno T,Shirakawa O,Tanaka C

doi

10.1016/0006-291x(83)91709-6

subject

Has Abstract

pub_date

1983-05-16 00:00:00

pages

948-53

issue

3

eissn

0006-291X

issn

1090-2104

pii

0006-291X(83)91709-6

journal_volume

112

pub_type

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