M5 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gq proteins. They are the last of five muscarinic receptors that act to control the metabotropic functions of acetylcholine (ACh) in the central nervous system (CNS).
|Product Name / Activity
|Selective positive allosteric modulator of M5 receptors
|Positive allosteric modulator of M5 receptors
M5 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gq proteins. They are the last of five muscarinic receptors that act to control the metabotropic functions of acetylcholine (ACh) in the central nervous system (CNS). M5 receptors are most densely populated in the dopamine-containing neuronal cells of the substantia nigra, hippocampus, cerebral cortex and striatum.
Activation of the M5 receptor leads to several responses, including the activation of ion channels such as K+ and Cl- and the inhibition of adenylyl cyclase. M5 receptor agonism modulates the activity of dopaminergic neurons and the release of dopamine into the striatum, which play an important role in mediating properties of abusive substances such as cocaine. In fact the M5 receptor has been implicated in drug addiction and may represent a therapeutic target. Endothelial M5 receptors also control the ability of acetylcholine to establish vasodilation in vascular beds, dramatically affecting cerebral blood flow.
M5 receptors may also be a potential therapeutic target in the treatment of memory deficits caused by impaired cerebrovascular function.
External sources of pharmacological information for M5 Receptors :
Literature for M5 Receptors
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