Distribution and pharmacological characterization of muscarinic-cholinergic receptors in the cockroach brain
The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard analysis indicated a Bmax of 604 pmol/mg protein. Kinetic analysis indicated that the ligand is binding in a complex fashion while dissociat...
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Published in | Archives of insect biochemistry and physiology Vol. 16; no. 2; p. 107 |
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Main Authors | , , |
Format | Journal Article |
Language | English |
Published |
United States
1991
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Subjects | |
Online Access | Get more information |
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Summary: | The binding of [3H]quinuclidinyl benzilate to a cockroach brain preparation was investigated. Specific binding was saturable with a Kd of 0.25 nM and Scatchard analysis indicated a Bmax of 604 pmol/mg protein. Kinetic analysis indicated that the ligand is binding in a complex fashion while dissociation followed a simple kinetic process. The pharmacology of the site was typical of muscarinic receptors but the site cannot be characterized in terms of vertebrate muscarinic-receptor subtypes. Affinity of the receptor for agonists was modulated by Mg2+ and guanylylimidodiphosphate but not by pertussis toxin indicating the involvement of a pertussis-toxin insensitive G-protein. Carbamylcholine did not inhibit basal or forskolin-stimulated adenylate cyclase activity. The binding site was localized autoradiographically and was restricted to the median and lateral calyces of the brain |
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Bibliography: | 9143682 L72 |
ISSN: | 0739-4462 1520-6327 |
DOI: | 10.1002/arch.940160204 |