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Muscarinic acetylcholine receptor M4

The muscarinic acetylcholine receptor M<sub>4</sub>, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the CHRM4 gene.

Function

M<sub>4</sub> muscarinic receptors are coupled to G<sub>i/o</sub> heterotrimeric proteins.

They function as inhibitory autoreceptors for acetylcholine. Activation of M<sub>4</sub> receptors inhibits acetylcholine release in the striatum. The M<sub>2</sub> 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 M<sub>4</sub> receptors in the striatum inhibit D<sub>1</sub>-induced locomotor stimulation in mice. M<sub>4</sub> receptor-deficient mice exhibit increased locomotor simulation in response to D<sub>1</sub> agonists, amphetamine and cocaine. Neurotransmission in the striatum influences extrapyramidal motor control, thus alterations in M<sub>4</sub> activity may contribute to conditions such as Parkinson's disease.

The M<sub>4</sub> muscarinic receptor has been found to be a regulator of erythroid progenitor cell differentiation. Inhibition of the M<sub>4</sub> muscarinic receptor provides therapeutic benefits in myelodysplastic syndrome and anemia.

Ligands

Agonists

Positive allosteric modulators

Antagonists

  • AFDX-384 (mixed M2/M4 antagonist, N-[2-[2-[(Dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide, CAS# 118290-27-0)
  • Dicycloverine
  • Diphenhydramine
  • Himbacine
  • Mamba toxin 3
  • NBI-1076968
  • PD-102,807 (3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-carboxylic acid ethyl ester, CAS# 23062-91-1)
  • PD-0298029
  • Tropicamide - moderate selectivity over other muscarinic subtypes (2-5x approx)
  • VU6028418

See also

References

Further reading

External links