mAChR M4 Antagonists Small Molecules and Peptides

M₄ receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to G_i 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. M₄ receptors are densely populated in the striatum and the lungs.

Activation of the M₄ receptor leads to several responses, including the inhibition of adenylyl cyclase. One of the primary roles of M₄ receptor activation ...