Muscarinic acetylcholine receptor M4
From Self-sufficiency
| edit |
| Cholinergic receptor, muscarinic 4 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Identifiers | |||||||||||||
| Symbols | CHRM4; HM4 | ||||||||||||
| External IDs | OMIM: 118495 MGI: 88399 HomoloGene: 20192 IUPHAR: M4 GeneCards: CHRM4 Gene | ||||||||||||
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| Orthologs | |||||||||||||
| Species | Human | Mouse | |||||||||||
| Entrez | 1132 | 12672 | |||||||||||
| Ensembl | n/a | ENSMUSG00000040495 | |||||||||||
| UniProt | P08173 | Q0VBU3 | |||||||||||
| RefSeq (mRNA) | NM_000741 | NM_007699 | |||||||||||
| RefSeq (protein) | NP_000732 | NP_031725 | |||||||||||
| Location (UCSC) | n/a | Chr 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]
Contents
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
- LY-2033298 [4]
- VU-0152100
- VU-0152099 [5]
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
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<references />, or <references group="..." />Further reading
- Goyal RK; Underhill, Lisa H.; Goyal, Raj K. (1989). "Muscarinic receptor subtypes. Physiology and clinical implications". N. Engl. J. Med. 321 (15): 1022–9. doi:10.1056/NEJM198910123211506. PMID 2674717.
- Brann MR, Ellis J, Jørgensen H; et al. (1994). "Muscarinic acetylcholine receptor subtypes: localization and structure/function". Prog. Brain Res. 98: 121–7. doi:10.1016/S0079-6123(08)62388-2. PMID 8248499.
- Grewal RP, Martinez M, Hoehe M; et al. (1992). "Genetic linkage mapping of the m4 human muscarinic receptor (CHRM4)". Genomics. 13 (1): 239–40. doi:10.1016/0888-7543(92)90236-L. PMID 1577490.
- Detera-Wadleigh SD, Wiesch D, Bonner TI (1989). "An SstI polymorphism for the human muscarinic acetylcholine receptor gene, m4 (CHRM 4)". Nucleic Acids Res. 17 (15): 6431. doi:10.1093/nar/17.15.6431. PMC 318330 Freely accessible. PMID 2570410.
- Ashkenazi A, Ramachandran J, Capon DJ (1989). "Acetylcholine analogue stimulates DNA synthesis in brain-derived cells via specific muscarinic receptor subtypes". Nature. 340 (6229): 146–50. doi:10.1038/340146a0. PMID 2739737.
- Bonner TI, Buckley NJ, Young AC, Brann MR (1987). "Identification of a family of muscarinic acetylcholine receptor genes". Science. 237 (4814): 527–32. doi:10.1126/science.3037705. PMID 3037705.
- Bonner TI, Young AC, Brann MR, Buckley NJ (1990). "Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes". Neuron. 1 (5): 403–10. doi:10.1016/0896-6273(88)90190-0. PMID 3272174.
- Peralta EG, Ashkenazi A, Winslow JW; et al. (1988). "Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors". EMBO J. 6 (13): 3923–9. PMC 553870 Freely accessible. PMID 3443095.
- van Koppen CJ, Lenz W, Nathanson NM (1993). "Isolation, sequence and functional expression of the mouse m4 muscarinic acetylcholine receptor gene". Biochim. Biophys. Acta. 1173 (3): 342–4. PMID 7916637.
- Haga K, Kameyama K, Haga T; et al. (1996). "Phosphorylation of human m1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 and protein kinase C". J. Biol. Chem. 271 (5): 2776–82. doi:10.1074/jbc.271.5.2776. PMID 8576254.
- von der Kammer H, Mayhaus M, Albrecht C; et al. (1998). "Muscarinic acetylcholine receptors activate expression of the EGR gene family of transcription factors". J. Biol. Chem. 273 (23): 14538–44. doi:10.1074/jbc.273.23.14538. PMID 9603968.
- Oldenhof J, Vickery R, Anafi M; et al. (1998). "SH3 binding domains in the dopamine D4 receptor". Biochemistry. 37 (45): 15726–36. doi:10.1021/bi981634. PMID 9843378.
- Sato KZ, Fujii T, Watanabe Y; et al. (1999). "Diversity of mRNA expression for muscarinic acetylcholine receptor subtypes and neuronal nicotinic acetylcholine receptor subunits in human mononuclear leukocytes and leukemic cell lines". Neurosci. Lett. 266 (1): 17–20. doi:10.1016/S0304-3940(99)00259-1. PMID 10336173.
- Dias Neto E, Correa RG, Verjovski-Almeida S; et al. (2000). "Shotgun sequencing of the human transcriptome with ORF expressed sequence tags". Proc. Natl. Acad. Sci. U.S.A. 97 (7): 3491–6. doi:10.1073/pnas.97.7.3491. PMC 16267 Freely accessible. PMID 10737800.
- Wang H, Han H, Zhang L; et al. (2001). "Expression of multiple subtypes of muscarinic receptors and cellular distribution in the human heart". Mol. Pharmacol. 59 (5): 1029–36. PMID 11306684.
- Buchli R, Ndoye A, Arredondo J; et al. (2002). "Identification and characterization of muscarinic acetylcholine receptor subtypes expressed in human skin melanocytes". Mol. Cell. Biochem. 228 (1-2): 57–72. doi:10.1023/A:1013368509855. PMID 11855742.
- McClatchy DB, Knudsen CR, Clark BF; et al. (2002). "Novel interaction between the M4 muscarinic acetylcholine receptor and elongation factor 1A2". J. Biol. Chem. 277 (32): 29268–74. doi:10.1074/jbc.M203081200. PMID 12048193.
- Dean B, McLeod M, Keriakous D; et al. (2003). "Decreased muscarinic1 receptors in the dorsolateral prefrontal cortex of subjects with schizophrenia". Mol. Psychiatry. 7 (10): 1083–91. doi:10.1038/sj.mp.4001199. PMID 12476323.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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- ↑ 1.0 1.1 "Entrez Gene: CHRM4 cholinergic receptor, muscarinic 4".
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- ↑ 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 2495016 Freely accessible. PMID 18678919.
- ↑ 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 2745822 Freely accessible. PMID 18772318.
