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Goodman & Gilman's The Pharmacological Basis of Therapeutics, 12e
| Section II. Neuropharmacology > |
Chapter 9. Muscarinic Receptor Agonists and Antagonists
Sections: Acetylcholine and Its Muscarinic Receptor Target, Muscarinic Receptor Agonists, Muscarinic Receptor Antagonists, Clinical Summary, Bibliography.
Topics Discussed: autonomic nervous system; drugs affecting neurotransmission; sympathomimetics; adrenergic antagonists; cholinergics; anticholinergics; muscarinic agonists; muscarinic antagonists.
Excerpt:"Muscarinic acetylcholine receptors in the peripheral nervous system occur primarily on autonomic effector cells innervated by postganglionic parasympathetic nerves. Muscarinic receptors are also present in autonomic ganglia and on some cells (e.g., vascular endothelial cells) that, paradoxically, receive little or no cholinergic innervation. Within the central nervous system (CNS), the hippocampus, cortex, and thalamus have high densities of muscarinic receptors.Muscarinic receptors were characterized initially by analysis of the responses of cells and organ systems in the periphery and the CNS. For example, differential effects of two muscarinic agonists, bethanechol and McN-A-343, on the tone of the lower esophageal sphincter led to the initial designation of muscarinic receptors as M1 (ganglionic) and M2 (effector cell) (Goyal and Rattan, 1978). The cloning of the cDNAs that encode muscarinic receptors identified five distinct gene products (Bonner et al., 1987), now designated as M1 through M5 muscarinic receptors (Chapter 8). All of the known muscarinic receptors are G protein-coupled receptors that in turn couple to various cellular effectors (Chapter 3). Although selectivity is not absolute, stimulation of M1,..."
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