Interactions between gallamine and muscarinic receptors: allosterism and subpopulation specificity are separate phenomena
| Autor: | Margaret Seidenberg, John Ellis |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Male
Allosteric regulation Molecular Conformation Scopolamine Derivatives In Vitro Techniques Pharmacology Muscarinic acetylcholine receptor medicine Animals Gallamine Triethiodide Chemistry Cerebrum Calcium channel Antagonist Rats Inbred Strains N-Methylscopolamine Receptors Muscarinic Rats Quinuclidinyl Benzilate medicine.anatomical_structure Verapamil Forebrain Biophysics Brainstem Brain Stem medicine.drug |
| Zdroj: | European Journal of Pharmacology. 144:39-44 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/0014-2999(87)90006-9 |
| Popis: | The quaternary antagonist gallamine discriminates subpopulations of muscarinic receptors in the forebrain and brainstem of the rat and also modulates the binding of other muscarinic ligands via an allosteric mechanism in both brain regions. The calcium channel antagonist verapamil exhibits a similar allosteric effect in both regions (at 100 μM) but does not differentiate the subpopulations that are defined by gallamine. On the other hand, N-methylatropine does not produce the allosteric effect at 100 μM, but shows a high degree of selectivity (about 1000-fold) for the gallamine-defined subpopulations. These studies indicate that the allosterism and subpopulation specificity of gallamine are separate phenomena and may be examined in isolation by appropriate ligands. |
| Databáze: | OpenAIRE |
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