M2 Receptors
M2 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gi proteins, generally leading to inhibitory effects. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine in the CNS.
M2 Receptor Antagonists |
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Cat. No. | Product Name / Activity |
1105 | AF-DX 116 |
Selective M2 antagonist | |
1345 | AF-DX 384 |
Potent M2/M4 antagonist | |
2292 | AQ-RA 741 |
High affinity and selective M2 antagonist | |
1425 | (S)-(+)-Dimethindene maleate |
Selective M2 antagonist | |
M2 Receptor Modulators |
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Cat. No. | Product Name / Activity |
6964 | LY 2119620 |
Positive allosteric modulator of M2 and M4 receptors |
M2 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gi proteins, generally leading to inhibitory effects. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine (ACh) in the central nervous system (CNS). M2 receptors are densely populated in the heart, airway smooth muscle, the hippocampus and most other brain regions.
Activation of the M2 receptor leads to several responses, including the inhibition of adenylyl cyclase and activation of inward rectifier K+ channels (KIR), and Ca2+-activated K+ channels (KCa). M2 receptor antagonism can slow the speed of depolarization and returning the heart to sinus rhythm after sympathetic nervous system stimulation. Overall, M2 receptors are involved in numerous processes including the control of atrial force of contraction, regulation of the AV node conduction velocity, and have also been implicated in peripheral airway smooth muscle contraction and in cognitive processes such as memory and learning. M2 receptors antagonism has been suggested as a therapeutic target in the treatment of Alzheimer's Disease.
External sources of pharmacological information for M2 Receptors :
Literature for M2 Receptors
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