MolPharm

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Waelbroeck, M.
Right arrow Articles by Christophe, J.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Waelbroeck, M.
Right arrow Articles by Christophe, J.

Rat cardiac muscarinic receptors. I. Effects of guanine nucleotides on high- and low-affinity binding sites

M Waelbroeck, P Robberecht, P Chatelain and J Christophe

The binding properties of muscarinic cholinergic binding sites were investigated in rat cardiac membranes, using the labeled agonist [3H] oxotremorine-M ([3H]Oxo-M) and the labeled antagonist L-[benzilic-4,4'- 3H]quinuclidinyl benzilate (L-[3H]QNB). The binding of both tracers was inhibited stereospecifically by dexetimide and levitimide. [3H]Oxo-M labeled only high-affinity agonist binding sites, whereas L-[3H]QNB bound to high- and low-affinity agonist binding sites with equal affinity. Agonists were unable to induce "negative cooperativity" interactions by increasing the dissociation of labeled agonist or antagonist. Guanine nucleotides decreased markedly the affinity of high- and low-affinity binding sites for agonists, without affecting their affinity for antagonists. In the presence of a maximally effective concentration of GTP, all muscarinic receptors showed the same low affinity for agonists. Among these agonists, carbamylcholine and oxotremorine (but not pilocarpine) displayed a lower affinity for both classes of binding sites in the presence of GTP.

Volume 21, Issue 3, pp. 581-588, 05/01/1982
Copyright © 1982 by American Society for Pharmacology and Experimental Therapeutics




This article has been cited by other articles:


Home page
 Learn. Mem.Home page
D. Saar, M. Dadon, M. Leibovich, H. Sharabani, Y. Grossman, and E. Heldman
Opposing effects on muscarinic acetylcholine receptors in the piriform cortex of odor-trained rats
Learn. Mem., March 9, 2007; 14(3): 224 - 228.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
M. Waelbroeck
Activation of Guanosine 5'-[{gamma}-35S]thio-triphosphate Binding through M1 Muscarinic Receptors in Transfected Chinese Hamster Ovary Cell Membranes: 1. Mathematical Analysis of Catalytic G Protein Activation
Mol. Pharmacol., April 1, 2001; 59(4): 875 - 885.
[Abstract] [Full Text]

Home page
 Mol. Pharmacol.Home page
J. A. Saugstad, J. M. Kinzie, M. M. Shinohara, T. P. Segerson, and G. L. Westbrook
Cloning and Expression of Rat Metabotropic Glutamate Receptor 8 Reveals a Distinct Pharmacological Profile
Mol. Pharmacol., January 1, 1997; 51(1): 119 - 125.
[Abstract] [Full Text]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1982 by the American Society for Pharmacology and Experimental Therapeutics