Heterogeneity of vascular muscarinic receptors. 1990

R M Eglen, and R L Whiting
Institute of Pharmacology, Syntex Research, Palo Alto, California 94303.

Muscarinic receptors mediate diverse effects on the vasculature. Recently, a consensus has been arrived at with regard to muscarinic receptor classification (Levine & Birdsall, 1989). As a result, it may now be possible to clarify the role of each subtype in the responses of vascular tissues to muscarinic agonists. It is apparent that vascular muscarinic receptors form a heterogeneous population. M1 receptors contract canine venous tissue, whilst M3 receptors contract porcine and bovine coronary arteries. M3 receptors also mediate EDRF-dependent relaxant responses in the majority of tissues studied to date. M2 receptors elicit relaxations by a decrease in sympathetic outflow in canine femoral vein, rabbit ear artery and rat portal vein. These conclusions are primarily derived from functional estimations of equilibrium dissociation constants, since comparable radioligand binding data are both scarce and contradictory. It is concluded that all three major subtypes of receptors are present in the vasculature. However, the limited selectivity of the available antagonists, the lack of extensive use of such compounds and the unavailability of selective agonists clearly indicate the need for more definitive studies to be undertaken.

UI MeSH Term Description Entries
D011976 Receptors, Muscarinic One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology. Muscarinic Acetylcholine Receptors,Muscarinic Receptors,Muscarinic Acetylcholine Receptor,Muscarinic Receptor,Acetylcholine Receptor, Muscarinic,Acetylcholine Receptors, Muscarinic,Receptor, Muscarinic,Receptor, Muscarinic Acetylcholine,Receptors, Muscarinic Acetylcholine
D001808 Blood Vessels Any of the tubular vessels conveying the blood (arteries, arterioles, capillaries, venules, and veins). Blood Vessel,Vessel, Blood,Vessels, Blood
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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