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M5 receptor

Family: Acetylcholine receptors (muscarinic)

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Allosteric Regulators
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
General Comments
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 532 15q26 CHRM5 cholinergic receptor, muscarinic 5 4
Mouse 7 532 2 E3 Chrm5 cholinergic receptor, muscarinic 5 30
Rat 7 531 3q34 Chrm5 cholinergic receptor, muscarinic 5 4,23,29,38
Previous and Unofficial Names
m5
acetylcholine receptor, muscarinic 5
cholinergic receptor, muscarinic 5
muscarinic acetylcholine receptor M5
muscarinic acetylcholine receptor 5
M5R
Database Links
ChEMBL Target 215 (Hs), 12204 (Mm), 10688 (Rn)
DrugBank Target 274 (Hs)
Ensembl ENSG00000184984 (Hs), ENSMUSG00000074939 (Mm), ENSRNOG00000006397 (Rn)
Entrez Gene 1133 (Hs), 213788 (Mm), 53949 (Rn)
GeneCards CHRM5 (Hs)
GenitoUrinary Development Molecular Anatomy Project Chrm5 (Mm)
HomoloGene 22697 (Hs)
Human Protein Reference Database 00331 (Hs)
InterPro P08912 (Hs), Q920H4 (Mm), P08911 (Rn)
KEGG Gene hsa:1133 (Hs), mmu:213788 (Mm), rno:53949 (Rn)
OMIM 118496 (Hs)
PharmGKB Gene PA26486 (Hs)
PhosphoSitePlus P08912 (Hs), Q920H4 (Mm), P08911 (Rn)
Protein Ontology (PRO) PRO:000001617 (Hs)
RefSeq Nucleotide NM_012125 (Hs), NM_205783 (Mm), NM_017362 (Rn)
RefSeq Protein NP_036257 (Hs), NP_991352 (Mm), NP_059058 (Rn)
TreeFam ENSG00000184984 (Hs), ENSMUSG00000074939 (Mm), ENSRNOG00000006397 (Rn)
UniGene Hs. 128216 (Hs)
UniProt P08912 (Hs), Q920H4 (Mm), P08911 (Rn)
Wikipedia M5 receptor
Acetylcholine receptors (muscarinic)
Search for 3D structures on the PDB
Search by keyword: Acetylcholine receptors (muscarinic) M5 receptor Search by accession number: P08911, P08912, Q920H4
Natural/Endogenous Ligand(s)
acetylcholine
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
NNC 11-1585 Hs Full agonist 8.3 pKi 12
NNC 11-1607 Hs Full agonist 8.2 pKi 12
NNC 11-1314 Hs Full agonist 7.8 pKi 12
sabcomeline Hs Partial agonist 7.1 pKi 51
xanomeline Hs Partial agonist 6.7 – 7.4 pKi 19,45,51
acetylcholine Hs Full agonist 6.1 pKi 10
milameline Hs Partial agonist 5.4 pKi 51
pilocarpine Hs Partial agonist 5.0 pKi 19
carbachol Hs Full agonist 4.9 pKi 51
McN-A-343 Hs Partial agonist 4.9 pKi 35
(+)aceclidine Hs Full agonist 5.5 pEC50 14
(-)aceclidine Hs Partial agonist 5.1 pEC50 14
Agonist Comments
Please consult references [6,26,35,43] for further details of the activity of some of the ligands in this list.
Oxotremorine has also been found to be a partial agonist at the M5 receptor [35,43] (no binding data available).
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]N-methyl scopolamine Hs Antagonist 8.1 – 9.7 pKd 9-10,20,22,24,43
atropine Hs Antagonist 9.3 – 9.7 pKi 7,20
atropine Rn Antagonist 9.4 pKi 23
4-DAMP Hs Antagonist 9.0 pKi 13
4-DAMP Rn Antagonist 8.9 pKi 23
ipratropium Hs Antagonist 8.8 pKi 20
silahexocyclium Hs Antagonist 8.7 pKi 7
darifenacin Hs Antagonist 8.6 pKi 20
hexocyclium Hs Antagonist 8.4 pKi 7
HHSiD Rn Antagonist 7.4 pKi 23
hexahydrodifenidol Hs Antagonist 7.1 pKi 7
pirenzepine Rn Antagonist 7.1 pKi 23
HHSiD Hs Antagonist 6.8 – 7.2 pKi 7,16
methoctramine Hs Antagonist 6.3 – 7.2 pKi 7,16
pirenzepine Hs Antagonist 6.2 – 6.9 pKi 7,16,22
AFDX384 Hs Antagonist 6.3 pKi 13
p-F-HHSiD Hs Antagonist 6.3 pKi 16
MT3 Hs Antagonist 6.0 pKi 22
himbacine Hs Antagonist 5.4 – 6.5 pKi 22,33
AF-DX 116 Rn Antagonist 5.7 pKi 23
VU0255035 Hs Antagonist 5.6 pKi 36
AF-DX 116 Hs Antagonist 5.3 – 5.6 pKi 7,16
lithocholylcholine Hs Antagonist 5.2 pKi 10
View species-specific antagonist tables
Allosteric Regulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
N-chloromethyl-brucine Hs Negative 4.4 pKd 27
N-benzyl brucine Hs Neutral 3.7 pKd 27
N-benzyl brucine Hs Negative 3.7 pKd 27
strychnine Hs Negative 3.6 pKd 25
brucine Hs Negative 2.9 pKd 27
brucine N-oxide Hs Positive 2.3 pKd 27
brucine N-oxide Hs Negative 2.3 pKd 27

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  5
Tissue Distribution
Ciliary muscle.
Species:  Human
Technique:  In situ hybridisation and Northern blotting.
References:  58
Esophageal smooth muscle.
Species:  Human
Technique:  Radioligand binding.
References:  34
Vestibular system.
Species:  Human
Technique:  RT-PCR.
References:  41
Bladder.
Species:  Human
Technique:  RT-PCR.
References:  39
Vestibular system.
Species:  Rat
Technique:  RT-PCR.
References:  41
CNS: basal forebrain, parabigeminal nucleus.
Species:  Rat
Technique:  in situ hybridisation.
References:  40
CNS: cerebral cortex, hippocampus, corpus striatum, olfactory tubercle, midbrain, pons-medulla, cerebellum.
Species:  Rat
Technique:  Immunoprecipitation.
References:  55
CNS: substantia nigra, pars compacta and vental tegmental area.
Species:  Rat
Technique:  in situ hybridisation.
References:  47
Expression Datasets

Click here to show/hide data

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of the levels of IPs in CHO cells transfected with the human M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IPs accumulation.
References:  46
Measurement of IP1 levels in murine fibroblast cells (B82) transfected with the rat M5 receptor.
Species:  Rat
Tissue:  B82 cells.
Response measured:  Stimulation of IP1 accumulation.
References:  23
Measurement of PLC activity and Ca2+ levels in murine L cells transfected with the rat M5 receptor.
Species:  Rat
Tissue:  Murine L cells.
Response measured:  Stimulation of PLC activity and Ca2+ mobilisation.
References:  28
Measurement of IP1 levels in CHO cells transfected with the human M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP1 accumulation.
References:  35
Measurement of Ca2+ levels in Sf9 cells transfected with the rat M5 receptor.
Species:  Rat
Tissue:  Sf9 cells.
Response measured:  Ca2+ mobilisation.
References:  21
Measurement of PI hydrolysis in CHO cells transfected with the human M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of PI hydrolysis.
References:  12
Measurement of NO synthetase activity in CHO cells transfected with the M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Activation of nitric oxide synthetase.
References:  44
Measurement of ERK1/2 activity.
Species:  Human
Tissue: 
Response measured:  Increase in ERK1/2 activity.
References:  52
Physiological Functions
Modulation of dopaminergic neurotransmission.
Species:  Rat
Tissue:  In vivo (nucleus accumbens/striatum).
References:  32
Stimulation of gastric acid secretion.
Species:  Mouse
Tissue:  In vivo (stomach).
References:  1
Vasodilation.
Species:  Human
Tissue:  Intracortical arterioles.
References:  15
Physiological Consequences of Altering Gene Expression
M5 receptor knockout mice exhibit impaired gastric acid secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  1
M5 receptor knockout mice exhibit a lack of agonist-induced cerebral blood vessel dilation, as seen in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  54
Striatal slices from M5 receptor knockout mice exhibit a decrease in agonist-induced potentiation of dopamine release.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  54,57
M5 receptor knockout mice exhibit a reduction in the reinforcing effects and withdrawal symptoms of morphine.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  3
M5 receptor knockout mice exhibit a reduction in the reinforcing effects and withdrawal symptoms of cocaine.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  17,37
M5 receptor knockout mice exhibit an increase in antagonist-induced locomotion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  11
M5 receptor knockout mice exhibit an abolished late phase activation of dopaminergic neurons.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  18,56
M5 receptor knockout mice exhibit an increase in D2 receptor expression in some brain areas, a decrease in amphetamine-induced locomotion and an increase in latent inhibition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  42
M5 muscarinic receptor knockout mice show significantly reduced cerebral blood flow and exhibit impairments in hippocampus-dependent learning and hippocampal neuronal plasticity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  2
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Chrm5tm1Jwe Chrm5tm1Jwe/Chrm5tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:109248  MP:0001905 abnormal dopamine level PMID: 11707605 
Chrm5tm1Minm Chrm5tm1Minm/Chrm5tm1Minm
B6.129X1-Chrm5		 MGI:109248  MP:0002503 abnormal histamine physiology PMID: 15691866 
Chrm5tm1Jabe Chrm5tm1Jabe/Chrm5tm1Jabe
involves: C57BL/6		 MGI:109248  MP:0010149 abnormal synaptic dopamine release PMID: 20664521 
Chrm5tm1Jwe Chrm5tm1Jwe/Chrm5tm1Jwe
B6.129S6-Chrm5		 MGI:109248  MP:0010149 abnormal synaptic dopamine release PMID: 20664521 
Chrm5tm1Jwe Chrm5tm1Jwe/Chrm5tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:109248  MP:0001613 abnormal vasodilation PMID: 11707605 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
involves: 129X1/SvJ * CD-1		 MGI:109248  MP:0001529 abnormal vocalization PMID: 18382674 
Chrm5tm1Minm Chrm5tm1Minm/Chrm5tm1Minm
B6.129X1-Chrm5		 MGI:109248  MP:0000505 decreased digestive secretion PMID: 15691866 
Chrm1tm1Kano|Chrm5tm1Minm Chrm1tm1Kano/Chrm1tm1Kano,Chrm5tm1Minm/Chrm5tm1Minm
involves: 129X1/SvJ * C57BL/6		 MGI:109248  MGI:88396  MP:0000505 decreased digestive secretion PMID: 15691866 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
Not Specified		 MGI:109248  MP:0000623 decreased salivation PMID: 11900778 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
Not Specified		 MGI:109248  MP:0005111 hyperdipsia PMID: 11900778 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
involves: 129X1/SvJ * CD-1		 MGI:109248  MP:0009750 impaired behavioral response to addictive substance PMID: 18382674 
General Comments
For reviews on muscarinic receptor knockout mice see [8,31,48-50].
For a review specifically on M5 receptor knockout mice see [53].

REFERENCES

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1. Aihara, T., Nakamura, Y., Taketo, M. M., Matsui, M. and Okabe, S. (2005) Cholinergically stimulated gastric acid secretion is mediated by M(3) and M(5) but not M(1) muscarinic acetylcholine receptors in mice. Am J Physiol Gastrointest Liver Physiol, 288: G1199-G1207. [PMID:15691866]

2. Araya, R., Noguchi, T., Yuhki, M., Kitamura, N., Higuchi, M., Saido, T. C., Seki, K., Itohara, S., Kawano, M., Tanemura, K., Takashima, A., Yamada, K., Kondoh, Y., Kanno, I., Wess, J. and Yamada, M. (2006) Loss of M5 muscarinic acetylcholine receptors leads to cerebrovascular and neuronal abnormalities and cognitive deficits in mice. Neurobiol Dis, 24: 334-344. [PMID:16956767]

3. Basile, A. S., Fedorova, I., Zapata, A., Liu, X., Shippenberg, T., Duttaroy, A., Yamada, M. and Wess, J. (2002) Deletion of the M5 muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia. Proc Natl Acad Sci U S A, 99: 11452-11457. [PMID:12154229]

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7. Buckley, N. J., Bonner, T. I., Buckley, C. M. and Brann, M. R. (1989) Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells. Mol Pharmacol, 35: 469-476. [PMID:2704370]

8. Bymaster, F. P., McKinzie, D. L., Felder, C. C. and Wess, J. (2003) Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res, 28: 437-442. [PMID:12675128]

9. Cembala, T. M., Sherwin, J. D., Tidmarsh, M. D., Appadu, B. L. and Lambert, D. G. (1998) Interaction of neuromuscular blocking drugs with recombinant human m1-m5 muscarinic receptors expressed in Chinese hamster ovary cells. Br J Pharmacol, 125: 1088-1094. [PMID:9846649]

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15. Elhusseiny, A. and Hamel, E. (2000) Muscarinic--but not nicotinic--acetylcholine receptors mediate a nitric oxide-dependent dilation in brain cortical arterioles: a possible role for the M5 receptor subtype. J Cereb Blood Flow Metab, 20: 298-305. [PMID:10698067]

16. Esqueda, E. E., Gerstin, E. H., Griffin, M. T. and Ehlert, F. J. (1996) Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung. Biochem Pharmacol, 52: 643-658. [PMID:8759038]

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18. Forster, G. L., Yeomans, J. S., Takeuchi, J. and Blaha, C. D. (2002) M5 muscarinic receptors are required for prolonged accumbal dopamine release after electrical stimulation of the pons in mice. J Neurosci, 22: RC190-RC190. [PMID:11756520]

19. Grant, M. K. and El-Fakahany, E. E. (2005) Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor. J Pharmacol Exp Ther, 315: 313-319. [PMID:16002459]

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21. Hu, Y., Rajan, L. and Schilling, W. P. (1994) Ca2+ signaling in Sf9 insect cells and the functional expression of a rat brain M5 muscarinic receptor. Am J Physiol, 266: C1736-C1743. [PMID:8023903]

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36. Sheffler, DJ; Williams, R; Bridges, TM; Xiang, Z; Kane, AS; Byun, NE; Jadhav, S; Mock, MM; Zheng, F; Lewis, LM; et al.. (2009) A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol. Pharmacol., 76 (2): 356-68. [PMID:19407080]

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42. Wang, H., Ng, K., Hayes, D., Gao, X., Forster, G., Blaha, C. and Yeomans, J. (2004) Decreased amphetamine-induced locomotion and improved latent inhibition in mice mutant for the M5 muscarinic receptor gene found in the human 15q schizophrenia region. Neuropsychopharmacology, 29: 2126-2139. [PMID:15213703]

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To cite this database page, please use the following:

Nigel J. M. Birdsall, David A. Brown, Noel J. Buckley, Arthur Christopoulos, Richard M. Eglen, Frederick Ehlert, Rudolf Hammer, Heinz J. Kilbinger, Günter Lambrecht, Fred Mitchelson, Ernst Mutschler, Neil M. Nathanson, Roy D. Schwarz, Andrew B. Tobin, Jurgen Wess.
Acetylcholine receptors (muscarinic): M5 receptor. Last modified on 28/11/2012. Accessed on 22/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=17.


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