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M1 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
Biologically Significant Variants
General Comments
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 460 11q13 CHRM1 cholinergic receptor, muscarinic 1 7,68
Mouse 7 460 19 A Chrm1 cholinergic receptor, muscarinic 1, CNS 58,75
Rat 7 460 1q43-q51 Chrm1 cholinergic receptor, muscarinic 1 43,66,80,85
Previous and Unofficial Names
m1
acetylcholine receptor, muscarinic 1
Cholinergic receptor muscarin 1
Cholinergic receptor, muscarin 1
M1 muscarinic acetylcholine receptor
cholinergic receptor, muscarinic 1
m1 muscarinic acetylcholine receptor protein
muscarinic acetylcholine receptor M1
muscarinic acetylcholine receptor 1
Chrm-1
M1R
AW495047
Database Links
ChEMBL Target 61 (Hs), 11780 (Mm), 10647 (Rn)
DrugBank Target 103 (Hs)
Ensembl ENSG00000168539 (Hs), ENSMUSG00000032773 (Mm), ENSRNOG00000018385 (Rn)
Entrez Gene 1128 (Hs), 12669 (Mm), 25229 (Rn)
GeneCards CHRM1 (Hs)
GenitoUrinary Development Molecular Anatomy Project Chrm1 (Mm)
HomoloGene 20189 (Hs)
Human Protein Reference Database 00338 (Hs)
InterPro P11229 (Hs), P12657 (Mm), P08482 (Rn)
KEGG Gene hsa:1128 (Hs), mmu:12669 (Mm), rno:25229 (Rn)
OMIM 118510 (Hs)
PharmGKB Gene PA26484 (Hs)
PhosphoSitePlus P11229 (Hs), P12657 (Mm), P08482 (Rn)
Protein Ontology (PRO) PRO:000001613 (Hs)
RefSeq Nucleotide NM_000738 (Hs), NM_007698 (Mm), NM_080773 (Rn)
RefSeq Protein NP_000729 (Hs), NP_031724 (Mm), NP_542951 (Rn)
TreeFam ENSG00000168539 (Hs), ENSMUSG00000032773 (Mm), ENSRNOG00000018385 (Rn)
UniGene Hs. 632119 (Hs)
UniProt P11229 (Hs), P12657 (Mm), P08482 (Rn)
Wikipedia M1 receptor
Acetylcholine receptors (muscarinic)
Search for 3D structures on the PDB
Search by keyword: Acetylcholine receptors (muscarinic) M1 receptor Search by accession number: P08482, P11229, P12657
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 9.9 pKi 16
NNC 11-1607 Hs Full agonist 8.6 pKi 16
pentylthio-TZTP Hs Full agonist 8.6 pKi 38
NNC 11-1314 Hs Full agonist 7.4 pKi 16
xanomeline Hs Partial agonist 6.7 – 7.9 pKi 17,39,92,102
sabcomeline Hs Partial agonist 6.7 pKi 102
arecaidine propargyl ester Hs Full agonist 6.4 pKi 38
AC-42 Hs Full agonist 6.2 pKi 46
oxotremorine Rn Partial agonist 6.0 pKi 60
arecoline Hs Full agonist 5.7 pKi 38
oxotremorine-M Rn Full agonist 5.6 pKi 60
oxotremorine Hs Partial agonist 5.5 pKi 38
arecoline Rn Partial agonist 5.3 pKi 60
McN-A-343 Rn Partial agonist 5.1 pKi 60
oxotremorine-M Hs Full agonist 5.1 pKi 38
pilocarpine Hs Partial agonist 5.1 pKi 38
acetylcholine Rn Full agonist 5.0 pKi 14
McN-A-343 Hs Partial agonist 4.8 – 5.2 pKi 71
pilocarpine Rn Partial agonist 4.9 pKi 60
milameline Hs Partial agonist 4.8 pKi 102
acetylcholine Hs Full agonist 4.3 – 4.9 pKi 38,48
methylfurmethide Hs Full agonist 4.6 pKi 38
(-)YM796 Hs Partial agonist 4.3 – 4.8 pKi 94
(±)YM796 Hs Partial agonist 4.1 – 4.7 pKi 94
carbachol Hs Full agonist 3.2 – 5.3 pKi 17,38,102
furmethide Hs Full agonist 4.1 pKi 38
bethanechol Hs Full agonist 4.0 pKi 38
carbachol Rn Full agonist 3.9 pKi 14
bethanechol Rn Full agonist 3.7 pKi 60
(+)aceclidine Hs Full agonist 5.4 pEC50 20
(-)aceclidine Hs Partial agonist 5.0 pEC50 20
View species-specific agonist tables
Agonist Comments
Please consult references [10,50,71,90,99] for further details of the activity of some of the ligands in this list.
Pilocarpine has been found to be a partial agonist [50,71,99] as well as a full agonist [90] at the M1 receptor.
Oxotremorine has been found to be a partial agonist [50,71,90] as well as a full agonist [71] at the M1 receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]QNB Hs Antagonist 10.6 – 10.8 pKd 15,68
[3H]N-methyl scopolamine Rn Antagonist 9.7 pKd 14,90
[3H]N-methyl scopolamine Hs Antagonist 8.8 – 10.3 pKd 13,15,17,35,38-40,42,48
[3H]darifenacin Hs Antagonist 8.8 pKd 78
[3H]pirenzepine Hs Antagonist 7.9 pKd 93
MT7 Hs Antagonist 11.0 – 11.1 pKi 64
N-methyl scopolamine Hs Antagonist 9.9 pKi 23
propantheline Hs Antagonist 9.7 pKi 37
atropine Rn Antagonist 9.0 – 9.7 pKi 11,14,41
ipratropium Hs Antagonist 9.3 pKi 35
4-DAMP Hs Antagonist 9.2 pKi 19
atropine Hs Antagonist 8.5 – 9.6 pKi 17,23,35,37,68,78
scopolamine Hs Antagonist 9.0 pKi 37
4-DAMP Rn Antagonist 8.9 pKi 41
tripitramine Hs Antagonist 8.8 pKi 56
silahexocyclium Rn Antagonist 8.7 pKi 11
hexocyclium Rn Antagonist 8.6 pKi 11
darifenacin Hs Antagonist 8.3 pKi 35
hexahydrodifenidol Rn Antagonist 8.0 pKi 11
pirenzepine Rn Antagonist 7.8 – 7.9 pKi 11,41
methoctramine Rn Antagonist 7.8 pKi 11
VU0255035 Hs Antagonist 7.8 pKi 76
HHSiD Hs Antagonist 7.7 pKi 21
HHSiD Rn Antagonist 7.4 – 7.9 pKi 11,41
AFDX384 Hs Antagonist 7.5 pKi 19
guanylpirenzepine Rn Antagonist 7.3 – 7.6 pKi 1,89
p-F-HHSiD Hs Antagonist 7.1 – 7.8 pKi 21,37
MT1 Hs Antagonist 7.3 – 7.6 pKi 23,32
pirenzepine Hs Antagonist 6.3 – 8.3 pKi 21,37,40,68
methoctramine Hs Antagonist 7.0 – 7.3 pKi 21,78
himbacine Hs Antagonist 6.7 – 7.1 pKi 40,62
MT3 Hs Antagonist 6.5 – 7.1 pKi 40
MT2 Hs Antagonist 6.4 pKi 32
AF-DX 116 Hs Antagonist 6.2 pKi 21
AF-DX 116 Rn Antagonist 5.9 – 6.3 pKi 11,41
lithocholylcholine Rn Antagonist 5.6 pKi 14
View species-specific antagonist tables
Antagonist Comments
Recombinant MT7 (rMT7) is often used for bioassays due to the limited availability of the M1 muscarinic receptor-selective mamba toxin MT7 or m1-toxin 1 (rMT7 has comparable affinity for M1[64])
Allosteric Regulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
KT 5720 Hs Positive 6.4 pKd 52
staurosporine Hs Positive 5.9 pKd 52
Gö 7874 Hs Negative 5.8 pKd 52
WIN 51,708 Hs Negative 5.8 pKd 53
KT 5823 Hs Positive 5.7 pKd 52
WIN 62,577 Hs Negative 5.5 pKd 53
brucine Hs Positive 4.5 – 5.7 pKd 38,51
eburnamonine Hs Neutral 5.1 pKd 38
K-252a Hs Positive 5.1 pKd 52
alcuronium Hs Negative 5.0 pKd 38
strychnine Hs Neutral 4.9 – 5.0 pKd 38,48
strychnine Hs Negative 4.9 pKd 48
vincamine Hs Neutral 4.8 pKd 38
brucine Hs Neutral 4.5 pKd 51
N-benzyl brucine Hs Negative 4.4 pKd 51
N-chloromethyl-brucine Hs Negative 4.1 pKd 51
thiochrome Hs Neutral 4.1 pKd 49
brucine N-oxide Hs Positive 3.2 pKd 51
brucine N-oxide Hs Neutral 3.2 pKd 51
AC-42 Hs Negative 6.2 pKi 46
clozapine Hs Positive 7.9 pIC50 82
clozapine Rn Positive 7.7 pIC50 79
N-desmethylclozapine Hs Positive 7.3 pIC50 82
N-desmethylclozapine Rn Positive 6.8 pIC50 79
AC-260584 Rn Positive 5.9 pIC50 79
View species-specific allosteric regulator tables

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

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  5,9,67,73
Tissue Distribution
Esophageal smooth muscle.
Species:  Human
Technique:  Radioligand binding.
References:  70
Bladder.
Species:  Human
Technique:  RT-PCR.
References:  86
Vestibular system.
Species:  Human
Technique:  RT-PCR.
References:  88
CNS: cerebral cortex, basal ganglia, limbic areas.
Species:  Human
Technique:  Radioligand binding.
References:  18
CNS: forebrain.
Species:  Mouse
Technique:  immunocytochemistry.
References:  36
CNS: cerbral cortex, corpus striatum, hippocampus, thalamus.
Species:  Mouse
Technique:  Radioligand binding.
References:  65
CNS: cerebral cortex, hippocampus, corpus striatum, olfactory tubercle, midbrain, pons-medulla, cerebellum.
Species:  Rat
Technique:  Immunoprecipitation.
References:  104
CNS: hippocampus.
Species:  Rat
Technique:  immunocytochemistry.
References:  54
CNS: caudate putamen, nucleus accumbens, olfactory tubercle.
Species:  Rat
Technique:  in situ hybridisation.
References:  95
CNS: pons.
Species:  Rat
Technique:  Radioligand binding.
References:  3
Heart: intrinsic neurons.
Species:  Rat
Technique:  in situ hybridisation.
References:  33
Vestibular system.
Species:  Rat
Technique:  RT-PCR.
References:  88
CNS: cranial nerve nuclei.
Species:  Rat
Technique:  in situ hybridisation.
References:  87
Expression Datasets

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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 PI levels in mouse Y1 adrenal cells transfected with the mouse M1 receptor.
Species:  Mouse
Tissue:  Y1 adrenal cells.
Response measured:  Stimulation of PI hydrolysis.
References:  75
Measurement of PI hydrolysis, Ca2+ mobilisation and [3H]arachidonic acid release in A9 L cells transfected with the human M1 receptor.
Species:  Human
Tissue:  A9 L cells.
Response measured:  Stimulation of PI hydrolysis, Ca2+ mobilisation and [3H]arachidonic acid release.
References:  4
Measurement of PI hydrolysis in CHO cells transfected with the human M1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of PI hydrolysis.
References:  16
Measurement of ERK1/2 activity in hippocampal cells endogenously expressing the M1 receptor.
Species:  Rat
Tissue:  Post-ischemic hippocampus.
Response measured:  Increase in ERK1/2 activity.
References:  84
Measurement of activation of ERK1/2 in PC12D cells endogeneously expressing the M1 receptor.
Species:  Rat
Tissue:  Neuronal PC12D cells.
Response measured:  Activation of ERK1/2.
References:  28
Measurement of activation of neuronal nitric oxide synthetase in chinese hamster overy cells transfected with the M1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Activation of nitric oxide synthetase.
References:  91
Measurement of ERK1/2 activity in COS-7 cells transfected with the human M2 receptor.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Increase in ERK1/2 activity.
References:  72
Measurement of GIRK channel activity in Xenopus oocytes transfected with the human M1 receptor.
Species:  Human
Tissue:  Xenopus oocytes.
Response measured:  Inhibition of GIRK channels.
References:  34
Measurement of the effects of a ligand on the level, or rate, of binding of GTPγ35S to membranes.
Species:  Human
Tissue:  CHO cell membranes.
Response measured:  The binding of GTPγ35S to G proteins coupled to the receptor.
References:  6,47-50,52-53
Measurement of the effects of a ligand on the rate of hydrolysis of GTP by G proteins in membranes.
Species:  Human
Tissue:  CHO cells.
Response measured:  Generation of 32Pi from [γ-32P]GTP.
References:  50
Physiological Functions
Bronchoconstriction.
Species:  Human
Tissue:  In vivo.
References:  45
Vasodilation.
Species:  Rat
Tissue:  Lung.
References:  100
Modulation of NMDA receptor-meditated excitatory synaptic transmission.
Species:  Rat
Tissue:  Hippocampal CA1 pyramidal cells.
References:  57
Regulation of circadian rhythms.
Species:  Rat
Tissue:  Hypothalamic suprachiasmatic nucleus.
References:  27
Automaticity of the heart.
Species:  Mouse
Tissue:  Heart.
References:  101
Autoreceptor: modulation of ACh release.
Species:  Rat
Tissue:  Basal forebrain slices.
References:  83
Autoreceptor: modulation of ACh release.
Species:  Human
Tissue:  Neocortex slices.
References:  22
Stimulation of water consumption.
Species:  Rat
Tissue:  In vivo.
References:  69
Hypothermia.
Species:  Rat
Tissue:  In vivo.
References:  74
Spinal analgesia.
Species:  Rat
Tissue:  In vivo.
References:  26
Memory function.
Species:  Rat
Tissue:  In vivo.
References:  61
Stimulation of urination.
Species:  Rat
Tissue:  In vivo.
References:  44
Physiological Consequences of Altering Gene Expression
M1 receptor knockout mice exhibit reduced seizure activity in the pilocarpine model of epilepsy.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  31
M1 receptor knockout mice exhibit loss of regulation of M-current potassium channel activity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  31
M1 receptor knockout mice exhibit a loss of the positive chronotropic and inotropic responses.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  30
M1 receptor knockout mice exhibit increased locomotor activity and hyperactivity under stress.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  63
M1 receptor knockout mice exhibit increased dopamine levels in the striatum and increased locomotor activity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  25
M1 receptor knockout mice showed normal or even enhanced memory for tasks that involve matching-to-sample problems but significant impairments in non-matching-to-sample working memory and consolidation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  2
M1 receptor knockout mice exhibit reduced salivary flow.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  24
M1 receptor knockout mice exhibit disrupted tonotopic organisation and frequency tuning in the auditory cortex.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  105-106
M1 receptor knockout mice exhibit reduced gastric pepsinogen secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  103
Hippocampal slices from M1 receptor knockout mice do not exhibit carbachol-induced enhancement of LTP of excitatory synaptic transmission as seen in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  77
M1 receptor knockout mice exhibit reduced carbachol-stimulated ion secretion in the colon compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  29
Lung slices from M1 receptor knockout mice exhibit increased agonist-induced bronchoconstriction compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  81
M1 receptor knockout mice exhibit an increased tidal volume of the lung at rest.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  8
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Chrm1tm1Nmn Chrm1tm1Nmn/Chrm1tm1Nmn
B6.129X1-Chrm1		 MGI:88396  MP:0004631 abnormal auditory cortex morphology PMID: 15721569 
Chrm1tm1Nmn Chrm1tm1Nmn/Chrm1tm1Nmn
B6.129X1-Chrm1		 MGI:88396  MP:0004788 abnormal auditory cortex tonotopy PMID: 15721569 
Chrm1tm1Nmn Chrm1tm1Nmn/Chrm1tm1Nmn
B6.129X1-Chrm1		 MGI:88396  MP:0004996 abnormal CNS synapse formation PMID: 15721569 
Chrm1tm1Jwe|Chrm4tm1Jwe Chrm1tm1Jwe/Chrm1tm1Jwe,Chrm4tm1Jwe/Chrm4tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88396  MGI:88399  MP:0002206 abnormal CNS synaptic transmission PMID: 15919709 
Chrm1tm2.1Stl|Emx1tm1.1(cre)Ito Chrm1tm2.1Stl/Chrm1tm2.1Stl,Emx1tm1.1(cre)Ito/0
involves: 129P2/OlaHsd		 MGI:88396  MGI:95387  MP:0002910 abnormal excitatory postsynaptic currents PMID: 20080609 
Chrm1tm2.1Stl|Tg(Grik4-cre)G32-4Stl Chrm1tm2.1Stl/Chrm1tm2.1Stl,Tg(Grik4-cre)G32-4Stl/0
involves: 129P2/OlaHsd * C57BL/6		 MGI:2448783  MGI:88396  MP:0002910 abnormal excitatory postsynaptic currents PMID: 20080609 
Chrm1tm1Stl Chrm1tm1Stl/Chrm1tm1Stl
involves: C57BL/6		 MGI:88396  MP:0002912 abnormal excitatory postsynaptic potential PMID: 16290192 
Chrm1tm1Kano Chrm1tm1Kano/Chrm1tm1Kano
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 12859343 
Chrm1tm1Kano|Chrm3tm1Mmt Chrm1tm1Kano/Chrm1tm1Kano,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MGI:88398  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 12859343 
Chrm1tm2.1Stl|Emx1tm1.1(cre)Ito Chrm1tm2.1Stl/Chrm1tm2.1Stl,Emx1tm1.1(cre)Ito/0
involves: 129P2/OlaHsd		 MGI:88396  MGI:95387  MP:0001898 abnormal long term depression PMID: 20080609 
Chrm1tm2.1Stl|Tg(Grik4-cre)G32-4Stl Chrm1tm2.1Stl/Chrm1tm2.1Stl,Tg(Grik4-cre)G32-4Stl/0
involves: 129P2/OlaHsd * C57BL/6		 MGI:2448783  MGI:88396  MP:0001898 abnormal long term depression PMID: 20080609 
Chrm1tm2.1Stl|Emx1tm1.1(cre)Ito Chrm1tm2.1Stl/Chrm1tm2.1Stl,Emx1tm1.1(cre)Ito/0
involves: 129P2/OlaHsd		 MGI:88396  MGI:95387  MP:0004753 abnormal miniature excitatory postsynaptic currents PMID: 20080609 
Chrm1tm1Jwe Chrm1tm1Jwe/Chrm1tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88396  MP:0002272 abnormal nervous system electrophysiology PMID: 11856534 
Chrm1tm1Kano|Chrm3tm1Mmt Chrm1tm1Kano/Chrm1tm1Kano,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MGI:88398  MP:0005310 abnormal salivary gland physiology PMID: 15146045 
Chrm1tm1Jwe Chrm1tm1Jwe/Chrm1tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88396  MP:0001945 bronchoconstriction PMID: 14645675 
Chrm1tm1Kano|Chrm5tm1Minm Chrm1tm1Kano/Chrm1tm1Kano,Chrm5tm1Minm/Chrm5tm1Minm
involves: 129X1/SvJ * C57BL/6		 MGI:109248  MGI:88396  MP:0000505 decreased digestive secretion PMID: 15691866 
Chrm1tm1Stl Chrm1tm1Stl/Chrm1tm1Stl
involves: C57BL/6		 MGI:88396  MP:0002920 decreased paired-pulse facilitation PMID: 16290192 
Chrm1tm2.1Stl|Emx1tm1.1(cre)Ito Chrm1tm2.1Stl/Chrm1tm2.1Stl,Emx1tm1.1(cre)Ito/0
involves: 129P2/OlaHsd		 MGI:88396  MGI:95387  MP:0002920 decreased paired-pulse facilitation PMID: 20080609 
Chrm1tm2.1Stl|Tg(Grik4-cre)G32-4Stl Chrm1tm2.1Stl/Chrm1tm2.1Stl,Tg(Grik4-cre)G32-4Stl/0
involves: 129P2/OlaHsd * C57BL/6		 MGI:2448783  MGI:88396  MP:0002920 decreased paired-pulse facilitation PMID: 20080609 
Chrm1tm1Kano|Chrm3tm1Mmt Chrm1tm1Kano/Chrm1tm1Kano,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MGI:88398  MP:0000623 decreased salivation PMID: 15146045 
Chrm1tm1Jwe|Chrm4tm1Jwe Chrm1tm1Jwe/Chrm1tm1Jwe,Chrm4tm1Jwe/Chrm4tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88396  MGI:88399  MP:0002917 decreased synaptic depression PMID: 15919709 
Chrm1tm1Jwe Chrm1tm1Jwe/Chrm1tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88396  MP:0005079 defective cytotoxic T cell cytolysis PMID: 15913791 
Chrm1tm1Stl Chrm1tm1Stl/Chrm1tm1Stl
C57BL/6-Chrm1		 MGI:88396  MP:0001399 hyperactivity PMID: 11752469 
Chrm1+|Chrm1tm1Stl Chrm1tm1Stl/Chrm1+
C57BL/6-Chrm1		 MGI:88396  MP:0001399 hyperactivity PMID: 11752469 
Chrm1tm1Stl Chrm1tm1Stl/Chrm1tm1Stl
C57BL/6-Chrm1		 MGI:88396  MP:0001906 increased dopamine level PMID: 11752469 
Chrm1tm1Stl Chrm1tm1Stl/Chrm1tm1Stl
involves: C57BL/6		 MGI:88396  MP:0001475 reduced long term depression PMID: 16290192 
Biologically Significant Variants
Cys417 is a highly conserved residue in TM7 and is essential to receptor function. A rare Cys417 -> Arg mutation has been found in the human genome with possible physiological consequences.
Type:  Single nucleotide polymorphism.
Species:  Human
References:  55
General Comments
For reviews on muscarinic receptor knockout mice see [12,59,96-98].

REFERENCES

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1. Akbulut, H; Gören, Z; Iskender, E; Eraslan, A; Ozdemir, O; Oktay, S. (1999) Subtypes of muscarinic receptors in rat duodenum: a comparison with rabbit vas deferens, rat atria, guinea-pig ileum and gallbladder by using imperialine. Gen. Pharmacol., 32 (4): 505-11. [PMID:10323493]

2. Anagnostaras, S. G., Murphy, G. G., Hamilton, S. E., Mitchell, S. L., Rahnama, N. P., Nathanson, N. M. and Silva, A. J. (2003) Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice. Nat Neurosci, 6: 51-58. [PMID:12483218]

3. Baghdoyan, H. A. (1997) Location and quantification of muscarinic receptor subtypes in rat pons: implications for REM sleep generation. Am J Physiol, 273: R896-R904. [PMID:9321865]

4. Baumgold, J., Dyer, K., Falcone, J. F. and Bymaster, F. P. (1995) Comparison of second-messenger responses to muscarinic receptor stimulation in M1-transfected A9 L cells. Cell Signal, 7: 39-43. [PMID:7756109]

5. Biddlecome, G. H., Berstein, G. and Ross, E. M. (1996) Regulation of phospholipase C-beta1 by Gq and m1 muscarinic cholinergic receptor. Steady-state balance of receptor-mediated activation and GTPase-activating protein-promoted deactivation. J Biol Chem, 271: 7999-8007. [PMID:8626481]

6. Birdsall, N. J. M., Farries, T., Gharagozloo, P., Kobayashi, S., Lazareno, S. and Sugimoto, M. (1999) Subtype selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: functional studies. Mol. Pharmacol., 55: 778-786. [PMID:10101037]

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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): M1 receptor. Last modified on 05/03/2013. Accessed on 18/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=13.


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