Muscarinic acetylcholine receptors are members of rhodopsin-like G-protein coupled receptor family. They play several important roles; they mediate many of the effects of acetylcholine in the central and peripheral nervous system and modulate a variety of physiological functions, such as airway, eye and intestinal smooth muscle contraction, heart rate and glandular secretions. The receptors have a widespread tissue distribution and are a major drug target in human disease. They may be effective therapeutic targets in Alzheimer's disease, schizophrenia, Parkinson's disease and chronic obstructive pulmonary disease. There are five muscarinic acetylcholine receptor subtypes, designated M1-5. The family can be further divided into two broad groups based on their primary coupling to G-proteins. M2 and M4 receptors couple to the pertussis-toxin sensitive Gi proteins, whereas M1, M3 and M5 receptors couple to Gq proteins, which activate phospholipase C. The different subtypes can also couple to a wide range of diverse signalling pathways, some of which are G protein-independent.All subtypes seem to serve as autoreceptors, and knockout mice reveal the important neuromodulatory role played by this receptor family.The muscarinic acetylcholine M5 receptor is primarily found in the CNS, but is also found in esophageal smooth muscle and in the heart. Binding of acetylcholine to the receptor triggers a number of cellular responses, such as adenylate cyclase inhibition, phosphoinositide degradation, and potassium channel modulation. The receptor has been shown to stimulate gastric acid secretion.
Taxonomy/Path:
InterPro : Endothelin receptor family / Muscarinic acetylcholine receptor M5