The muscarinic acetylcholine receptor family consists of five GPCRs that mediate some of the neurotransmission functions of acetylcholine in the CNS and the periphery. Muscarinic 4 Receptor functions as inhibitory autoreceptor for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the striatum. The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release; albeit functioning actively primarily in the hippocampus and cerebral cortex. Muscarinic acetylcholine receptors possess a regulatory effect on dopaminergic neurotransmission. Activation of M4 receptors in the striatum inhibit D1-induced locomotor stimulation in mice. M4 receptor-deficient mice exhibit increased locomotor simulation in response to D1 agonists, amphetamine and cocaine. Neurotransmission in the striatum influences extrapyramidal motor control, thus alterations in M4 activity may contribute to conditions such as Parkinson’s disease. DAGNOMAD Muscarinic Acetylcholine Receptor M4 Cell Line from Innoprot allows the measurement of the activity and potency of ligands; such as oxotremorine.
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