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).

Products
Background
Gene Data

Antagonists

Cat No Product Name / Activity
0482 4-DAMP
Muscarinic M3 antagonist
2096 DAU 5884 hydrochloride
M3 receptor antagonist
2507 J 104129 fumarate
Potent, selective M3 antagonist
2579 Zamifenacin fumarate
Selective M3 antagonist

Other

Cat No Product Name / Activity
5548 DREADD agonist 21
Potent hM3Dq DREADD agonist
5549 Perlapine
Potent and selective hM3Dq DREADD agonist

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 :

M3 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human CHRM3 NM_000740 P20309
Mouse Chrm3 NM_033269 Q9ERZ3
Rat Chrm3 NM_012527 P08483