M3 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gq proteins. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine (ACh) in the central nervous system (CNS). M3 receptors are most densely populated in smooth muscle, endocrine and exocrine glands, lungs and CNS.
Activation of the M3 receptor leads to several responses, including the upregulation of phospholipase C, and inositol triphosphate (IP3), therefore increasing intracellular Ca2+. Hence, M3 receptor agonism can lead to smooth muscle constriction and bronchoconstriction. Conversely, receptor activation on vascular endothelial cells may upregulate the vasodilator nitric oxide (NO). Activation of M3 receptors also contributes towards many secretions (for example from the salivary gland, pancreas or stomach). Overall, M3 receptors are involved in numerous metabolic functions, including the maintenance of insulin release, regulation of glucose homeostasis.
M3 receptor antagonism is a potential therapeutic target in the treatment pulmonary obstructions. Activation of the M3 receptor by selective agonists may also be beneficial in the treatment of Type 2 diabetes.View all products for M3 Receptors »
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Literature for M3 Receptors
7-TM Receptor Signaling Poster
Written by Terry Kenakin et al, this poster highlights the multiple behaviors of seven-transmembrane (7-TM) receptors, including G-protein-dependent and -independent signaling and the concept of collateral efficacy. Compounds available from Tocris are listed.Request copy | View all posters
Written by Alan Palmer, this poster summarizes structural and functional changes observed in the progression of Alzheimer's disease (AD). The hypotheses behind the neurobiology of AD are discussed alongside the different stages in disease progression. Compounds available from Tocris are listed.Request copy | View all posters
Written by Janet Maguire and Anthony Davenport, this poster summarizes different GPCR classes of the vascular system and their cognate ligands. The predominant vasoactive response of blood vessels to specific receptor activation is also described. Endogenous ligands and Tocris compounds are listed.Request copy | View all posters
Written by Jacob Ballon et al, this poster highlights key signaling pathways implicated in the development of schizophrenia, and the most promising strategies in novel drug development. Current research targets include cholinergic and glutamatergic signaling pathways, and the D2 receptor. Compounds available from Tocris are listed.Request copy | View all posters
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