Regulation of the solubilized bovine cerebral cortex muscarinic receptor by GTP and Na+ |
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Authors: | T Kuno O Shirakawa C Tanaka |
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Institution: | Department of Obstetrics and Gynaecology, University of British Columbia Vancouver, B.C., Canada |
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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. |
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Keywords: | T testosterone DHT 5α-dihydrotestosterone 17β-estradiol 3α-diol 5α-androstane-3α 17β-diol |
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