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Muscarinic acetylcholine receptor M5: Wikis

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Cholinergic receptor, muscarinic 5
Identifiers
Symbols CHRM5; HM5; MGC41838; ACM5
External IDs OMIM118496 MGI109248 HomoloGene22697 IUPHAR: M5 GeneCards: CHRM5 Gene
RNA expression pattern
PBB GE CHRM5 221347 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 1133 213788
Ensembl ENSG00000184984 ENSMUSG00000074939
UniProt P08912 Q0VBI9
RefSeq (mRNA) NM_012125 NM_205783
RefSeq (protein) NP_036257 NP_991352
Location (UCSC) Chr 15:
32.14 - 32.14 Mb
Chr 2:
112.28 - 112.28 Mb
PubMed search [1] [2]

The human muscarinic acetylcholine receptor M5 which is encoded by the CHRM5 gene is a member of the G protein-coupled receptor superfamily of integral membrane proteins. Binding of the endogenous ligand acetylcholine to the M5 receptor triggers a number of cellular responses such as adenylate cyclase inhibition, phosphoinositide degradation, and potassium channel modulation. Muscarinic receptors mediate many of the effects of acetylcholine in the central and peripheral nervous system. The clinical implications of this receptor have not been fully explored; however, stimulation of this receptor is known to increase cyclic AMP levels.[1]

Contents

Ligands

No highly selective agonists or antagonists for the M5 receptor have been discovered as of 2009, but several non-selective muscarinic agonists and antagonists have significant affinity for M5.

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Agonists

  • Milameline ((E)-1,2,5,6-Tetrahydro-1-methyl-3-pyridinecarboxaldehyde-O-methyloxime, CAS# 139886-32-1)
  • Sabcomeline

Positive allosteric modulators

  • VU-0238429: EC50 = 1.16 μM; >30-fold selectivity versus M1 and M3, inactive at M2 and M4.[2]

Antagonists

See also

References

  1. ^ "Entrez Gene: CHRM5 cholinergic receptor, muscarinic 5". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1133.  
  2. ^ Bridges TM, Marlo JE, Niswender CM, et al. (June 2009). "Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins". J. Med. Chem. 52 (11): 3445–8. doi:10.1021/jm900286j. PMID 19438238.  
  3. ^ Grant MK, El-Fakahany EE (October 2005). "Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor". J. Pharmacol. Exp. Ther. 315 (1): 313–9. doi:10.1124/jpet.105.090134. PMID 16002459.  

External links

Further reading

  • 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.  
  • Gutkind JS, Novotny EA, Brann MR, Robbins KC (1991). "Muscarinic acetylcholine receptor subtypes as agonist-dependent oncogenes.". Proc. Natl. Acad. Sci. U.S.A. 88 (11): 4703–7. doi:10.1073/pnas.88.11.4703. PMID 1905013.  
  • Liao CF, Themmen AP, Joho R, et al. (1989). "Molecular cloning and expression of a fifth muscarinic acetylcholine receptor.". J. Biol. Chem. 264 (13): 7328–37. PMID 2540186.  
  • 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.  
  • Crespo P, Xu N, Daniotti JL, et al. (1994). "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. Evidence for a protein kinase C-independent pathway.". J. Biol. Chem. 269 (33): 21103–9. PMID 8063729.  
  • 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.  
  • Kohn EC, Alessandro R, Probst J, et al. (1996). "Identification and molecular characterization of a m5 muscarinic receptor in A2058 human melanoma cells. Coupling to inhibition of adenylyl cyclase and stimulation of phospholipase A2.". J. Biol. Chem. 271 (29): 17476–84. doi:10.1074/jbc.271.29.17476. PMID 8663391.  
  • Burstein ES, Spalding TA, Brann MR (1998). "The second intracellular loop of the m5 muscarinic receptor is the switch which enables G-protein coupling.". J. Biol. Chem. 273 (38): 24322–7. doi:10.1074/jbc.273.38.24322. PMID 9733718.  
  • 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.  
  • 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.  
  • Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMID 12477932.  
  • Fujii T, Watanabe Y, Inoue T, Kawashima K (2003). "Upregulation of mRNA encoding the M5 muscarinic acetylcholine receptor in human T- and B-lymphocytes during immunological responses.". Neurochem. Res. 28 (3-4): 423–9. doi:10.1023/A:1022840416292. PMID 12675126.  
  • Ota T, Suzuki Y, Nishikawa T, et al. (2004). "Complete sequencing and characterization of 21,243 full-length human cDNAs.". Nat. Genet. 36 (1): 40–5. doi:10.1038/ng1285. PMID 14702039.  
  • De Luca V, Wang H, Squassina A, et al. (2004). "Linkage of M5 muscarinic and alpha7-nicotinic receptor genes on 15q13 to schizophrenia.". Neuropsychobiology 50 (2): 124–7. doi:10.1159/000079102. PMID 15292665.  
  • Qu J, Zhou X, Xie R, et al. (2006). "The presence of m1 to m5 receptors in human sclera: evidence of the sclera as a potential site of action for muscarinic receptor antagonists.". Curr. Eye Res. 31 (7-8): 587–97. doi:10.1080/02713680600770609. PMID 16877267.  
  • Anney RJ, Lotfi-Miri M, Olsson CA, et al. (2007). "Variation in the gene coding for the M5 muscarinic receptor (CHRM5) influences cigarette dose but is not associated with dependence to drugs of addiction: evidence from a prospective population based cohort study of young adults.". BMC Genet. 8: 46. doi:10.1186/1471-2156-8-46. PMID 17608938.  

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


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