- Klorfenamin
- Muscarinic acetylcholine receptor M4
- Muscarinic acetylcholine receptor M3
- Muscarinic acetylcholine receptor M2
- Muscarinic acetylcholine receptor M1
- Muscarinic acetylcholine receptor M5
- Acetylcholine receptor
- Muscarinic acetylcholine receptor
- Muscarinic antagonist
- Acetylcholine
- Muscarinic agonist
Muscarinic acetylcholine receptor M4 GudangMovies21 Rebahinxxi LK21
The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the CHRM4 gene.
Function
M4 muscarinic receptors are coupled to Gi/o heterotrimeric proteins.
They function as inhibitory autoreceptors 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.
The M4 muscarinic receptor has been found to be a regulator of erythroid progenitor cell differentiation. Inhibition of the M4 muscarinic receptor provides therapeutic benefits in myelodysplastic syndrome and anemia.
Ligands
= Agonists
=Acetylcholine
Carbachol
CMI-936
NBI-1117568 (HTL-0016878)
ML-007
Oxotremorine
Xanomeline
= Positive allosteric modulators
=Emraclidine (CVL-231, PF-06852231)
LY-2033298
NS-136
SUVN-L3307032
VU-0152100 (ML-108)
VU-0152099
= 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)
See also
Muscarinic acetylcholine receptor
References
Further reading
External links
Overview of all the structural information available in the PDB for UniProt: P08173 (Muscarinic acetylcholine receptor M4) at the PDBe-KB.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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