Muscarinic_acetylcholine_receptor_M4

Muscarinic acetylcholine receptor M4

The correct title of this article is Muscarinic acetylcholine receptor M₄. It appears incorrectly here because of technical restrictions.

Cholinergic receptor, muscarinic 4

Identifiers

CHRM4; HM4

External IDs

OMIM: 118495 MGI: 88399 HomoloGene: 20192

Gene ontology
Molecular function:	• rhodopsin-like receptor activity • receptor activity • muscarinic acetylcholine receptor activity
Cellular component:	• plasma membrane • integral to plasma membrane • postsynaptic membrane
Biological process:	• acetylcholine receptor signaling, muscarinic pathway • cell proliferation

Orthologs

Human

Mouse

n/a

ENSMUSG00000040495

n/a

Refseq

NM_000741 (mRNA)
NP_000732 (protein)

NM_007699 (mRNA)
NP_031725 (protein)

Location

n/a

Chr 2: 91.73 - 91.73 Mb

Pubmed search

The muscarinic acetylcholine receptor M₄, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a human gene.¹

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

Contents

1 Orthosteric Agonists
2 Allosteric Agonists
3 See also
4 References
5 Further reading

Orthosteric Agonists

Allosteric Agonists

LY2033298 ²

See also

Muscarinic acetylcholine receptor

References

^ ^a ^b "Entrez Gene: CHRM4 cholinergic receptor, muscarinic 4".
^ Chan WY, McKinzie DL, Bose S, Mitchell SN, Witkin JM, Thompson RC, christopoulos A, Lazareno S, Birdsall NJM, Bymaster FP, Felder CC (2008). "Allosteric modulation of the muscarinic M₄ receptor as an approach to treating schizophrenia". PNAS 105 (31): 10979-83. PMID 18678919.

Further reading

Goyal RK (1989). "Muscarinic receptor subtypes. Physiology and clinical implications.". N. Engl. J. Med. 321 (15): 1022–9. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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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v • d • e

Transmembrane receptor: G protein-coupled receptors

Class A: Rhodopsin like

Adrenergic	α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3

Eicosanoid	CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP, EP (1, 2, 3, 4), PGF) • Prostacyclin • Thromboxane

Neuropeptide	B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5) • Neuromedin (B, U (1, 2)) • Neurotensin (1, 2)

Orphan	GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172A, 173, 174, 176, 177, 182)

Purinergics	Adenosine (A1, A2a, A2b, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)

Serotonin	(all but 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)

Other	Acetylcholine (M1, M2, M3, M4, M5) • Adrenomedullin • Anaphylatoxin (C3a, C5a) • Angiotensin (1, 2) • Apelin • Bile acid • Bombesin (BRS3, GRPR, NMBR) • Bradykinin (B1, B2) • Cannabinoid (CB1, CB2) • Chemokine • Cholecystokinin (A, B) • Dopamine (D1, D2, D3, D4, D5) • EBI2 • Endothelin (A, B) • Estrogen • Formyl peptide (1, L1, L2) • Free fatty acid (1, 2, 3, 4) • FSH • Galanin (1, 2, 3) • Gonadotropin-releasing hormone (1, 2) • Ghrelin • Histamine (H1, H2, H3, H4) • Kisspeptin • Luteinizing hormone/choriogonadotropin • Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanocortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Melatonin (1A, 1B) • Motilin • Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) • Olfactory • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Orexin (1, 2) • Oxytocin • Oxoglutarate • PAF • Prokineticin (1, 2) • Prolactin-releasing peptide • Protease-activated (1, 2, 3, 4) • Relaxin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • SREB • Succinate • TAAR (1, 2, 3, 5, 6, 8, 9) • Tachykinin (1, 2, 3) • Thyrotropin • Thyrotropin-releasing hormone • Urotensin-II • Vasopressin (1A, 1B, 2)

Class B: Secretin like

Orphan	GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157)

Other	Brain-specific angiogenesis inhibitor (1, 2, 3) • Cadherin (1, 2, 3) • Calcitonin • CALCRL • CD97 • Corticotropin-releasing hormone (1, 2) • EMR (1, 2, 3) • Glucagon (GR, GIPR, GLP1R, GLP2R) • Growth hormone releasing hormone • PACAPR1 • GPR • Latrophilin (1, 2, 3, ELTD1) • Parathyroid hormone (1, 2) • Secretin • Vasoactive intestinal peptide (1, 2)

Class C: Metabotropic
glutamate / pheromone

Taste	TAS1R (1, 2, 3) • TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)

Other	Calcium-sensing receptor • GABA B (1, 2) • Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • GPR (156, 158, 179) • RAIG (1, 2, 3, 4)

Frizzled / Smoothened

Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) • Smoothened