Muscarinic acetylcholine receptor M4

From Self-sufficiency
Jump to: navigation, search
edit
Cholinergic receptor, muscarinic 4
Identifiers
SymbolsCHRM4; HM4
External IDsOMIM118495 MGI88399 HomoloGene20192 IUPHAR: M4 GeneCards: CHRM4 Gene
Orthologs
SpeciesHumanMouse
Entrez113212672
Ensembln/aENSMUSG00000040495
UniProtP08173Q0VBU3
RefSeq (mRNA)NM_000741NM_007699
RefSeq (protein)NP_000732NP_031725
Location (UCSC)n/aChr 2:
91.73 - 91.73 Mb
PubMed search[1][2]

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.[1][2]

Function

The muscarinic cholinergic receptors belong to a larger family of G protein-coupled receptors. The functional diversity of these receptors is defined by the binding of acetylcholine and includes cellular responses such as adenylate cyclase inhibition, phosphoinositide degeneration, and potassium channel modulation. Muscarinic receptors mediate many effects of acetylcholine in the central and peripheral nervous system. The clinical implications of this receptor are unknown; however, mouse studies link its function to adenylyl cyclase inhibition.[1]

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 and amphetamine.[3] Neurotransmission in the striatum influences extrapyramidal motor control, thus alterations in M4 activity may contribute to conditions such as Parkinson's Disease.

Ligands

Orthosteric agonists

Allosteric Agonists

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)
  • Himbacine
  • 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)
  • Tropicamide

See also

References

Cite error: Invalid <references> tag; parameter "group" is allowed only.

Use <references />, or <references group="..." />

Further reading

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


es:Receptor muscarínico M4
  1. 1.0 1.1 "Entrez Gene: CHRM4 cholinergic receptor, muscarinic 4". 
  2. Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  3. Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  4. Chan WY, McKinzie DL, Bose S; et al. (2008). "Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia". PNAS. 105 (31): 10978–83. doi:10.1073/pnas.0800567105. PMC 2495016Freely accessible. PMID 18678919. 
  5. Brady AE, Jones CK, Bridges TM; et al. (2008). "Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats". J. Pharmacol. Exp. Ther. 327 (3): 941–53. doi:10.1124/jpet.108.140350. PMC 2745822Freely accessible. PMID 18772318.