M3 Receptors
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 Receptor Antagonists |
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Cat. No. | Product Name / Activity |
0482 | 4-DAMP |
Muscarinic M3 antagonist | |
2096 | DAU 5884 hydrochloride |
M3 receptor antagonist | |
2507 | J 104129 fumarate |
Potent and selective M3 antagonist |
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.
External sources of pharmacological information for M3 Receptors :
Literature for M3 Receptors
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