Muscarinic acetylcholine receptor M5

Muscarinic acetylcholine receptor M5
Cholinergic receptor, muscarinic 5
Symbols CHRM5; HM5; MGC41838
External IDs OMIM118496 MGI109248 HomoloGene22697 IUPHAR: M5 GeneCards: CHRM5 Gene
RNA expression pattern
PBB GE CHRM5 221347 at tn.png
More reference expression data
Species Human Mouse
Entrez 1133 213788
Ensembl ENSG00000184984 ENSMUSG00000074939
UniProt P08912 Q0VBI9
RefSeq (mRNA) NM_012125.3 NM_205783.2
RefSeq (protein) NP_036257.1 NP_991352.2
Location (UCSC) Chr 15:
34.26 – 34.36 Mb
Chr 2:
112.32 – 112.32 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 effectively decrease cyclic AMP levels and downregulate the activity of protein kinase A (PKA).



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.


  • 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.[1]


See also


  1. ^ 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. 
  2. ^ 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. 

Further reading

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

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