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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 mediation. Muscarinic receptors influence many effects of acetylcholine in the central and peripheral nervous system. The muscarinic cholinergic receptor 1 is involved in mediation of vagally-induced bronchoconstriction and in the acid secretion of the gastrointestinal tract. The gene encoding this receptor is localized to 11q13. [provided by RefSeq, Jul 2008]
CHRM1 (Cholinergic Receptor Muscarinic 1) is a Protein Coding gene. Diseases associated with CHRM1 include Heart Block, Congenital and Alzheimer Disease. Among its related pathways are Signaling by GPCR and Peptide ligand-binding receptors. Gene Ontology (GO) annotations related to this gene include G protein-coupled receptor activity and phosphatidylinositol phospholipase C activity. An important paralog of this gene is CHRM5.
Muscarinic receptors are widely distributed throughout the body and control distinct functions according to location and subtype (M1 - M5).They are predominantly expressed in the parasympathetic nervous system where they exert both inhibitory and excitatory effects.
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0004435 | phosphatidylinositol phospholipase C activity | TAS | 9614217 |
GO:0004930 | G protein-coupled receptor activity | IEA | -- |
GO:0004993 | G protein-coupled serotonin receptor activity | IBA | 21873635 |
GO:0005515 | protein binding | IPI | 21056967 |
GO:0016907 | G protein-coupled acetylcholine receptor activity | IEA,IBA | 21873635 |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0005886 | plasma membrane | IEA,TAS | -- |
GO:0005887 | integral component of plasma membrane | IEA,IBA | 21873635 |
GO:0014069 | postsynaptic density | IEA | -- |
GO:0016020 | membrane | IEA,TAS | 7925360 |
GO:0016021 | integral component of membrane | IEA | -- |
SuperPathway | Contained pathways | ||
---|---|---|---|
1 | Peptide ligand-binding receptors | ||
2 | Monoamine GPCRs |
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3 | Signaling by GPCR | ||
4 | Pathways of neurodegeneration - multiple diseases | ||
5 | Regulation of actin cytoskeleton |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0007165 | signal transduction | IEA,TAS | 1411529 |
GO:0007186 | G protein-coupled receptor signaling pathway | IEA,TAS | -- |
GO:0007187 | G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | IBA | 21873635 |
GO:0007197 | adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway | IBA | 21873635 |
GO:0007205 | protein kinase C-activating G protein-coupled receptor signaling pathway | TAS | 9603968 |
Name | Status | Disease Links | Group | Role | Mechanism of Action | Clinical Trials |
---|---|---|---|---|---|---|
Atropine | Approved, Vet_approved | Pharma | Antagonist, Target | MAChRs antagonist | 221 | |
Darifenacin | Approved, Investigational | Pharma | Antagonist, Target | 26 | ||
Ipratropium | Approved, Experimental | Pharma | Antagonist, Target | 161 | ||
Pilocarpine | Approved, Investigational | Pharma | Agonist, Partial agonist, Target | 43 | ||
Pirenzepine | Approved | Pharma | Antagonist, Target | 1 |
Name | Synonyms | Role | CAS Number | PubChem IDs | PubMed IDs | |
---|---|---|---|---|---|---|
(-)aceclidine |
|
Agonist, Partial agonist |
|
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(-)YM796 |
|
Agonist, Partial agonist |
|
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(+)aceclidine |
|
Agonist, Full agonist |
|
|||
HHSiD |
|
Antagonist |
|
|||
N-Dealkylated tolterodine |
|
Compound | Action | Cas Number |
---|---|---|
Cevimeline hydrochloride | Selective M1 agonist | 107220-28-0 |
McN-A 343 | Selective M1 muscarinic agonist | 55-45-8 |
Nitrocaramiphen hydrochloride | Muscarinic antagonist, M1 > M2 | 98636-73-8 |
Pirenzepine dihydrochloride | Selective M1 muscarinic antagonist | 29868-97-1 |
Xanomeline oxalate | Functionally selective M1 agonist | 141064-23-5 |
Compound | Action | Cas Number |
---|---|---|
(+)-Muscarine iodide | 24570-49-8 | |
(±)-Acetylcarnitine chloride | cholinergic agonist | 2504-11-2 |
(±)-Decanoylcarnitine chloride | cholinergic agonist | 14919-36-9 |
(±)-Hexanoylcarnitine chloride | cholinergic agonist | 6920-35-0 |
(±)-Myristoylcarnitine chloride | cholinergic agonist | 14919-38-1 |
(±)-Octanoylcarnitine chloride | 18822-86-1 | |
(±)-Propionylcarnitine chloride | 18828-58-5 | |
(R)-(+)-Tolterodine | 124937-51-5 | |
(S)-(+)-Dimethindene maleate | 136152-65-3 | |
4-DAMP | 1952-15-4 | |
5-Methylfurmethiodide | 1197-60-0 | |
Aclidinium Bromide | LAMAs antagonist | 320345-99-1 |
AF-DX 116 | 102394-31-0 | |
AF-DX 384 | 118290-26-9 | |
Arecaidine but-2-ynyl ester tosylate | 119630-77-2 | |
Arecaidine propargyl ester tosylate | 147202-94-6 | |
Arecoline hydrobromide | Muscarinic receptor agonist | 300-08-3 |
Atropine | MAChRs antagonist | 5908-99-6 |
Bethanechol chloride | Muscarinic receptor agonist | 590-63-6 |
Biperiden HCl | Anticholinergic drug | 1235-82-1 |
Cevimeline | Muscarinic receptor agonist | 107233-08-9 |
Cevimeline hydrochloride hemihydrate | Agonist of muscarinic receptor (M1/M3) | 153504-70-2 |
Darifenacin HBr | 133099-07-7 | |
DAU 5884 hydrochloride | 131780-48-8 | |
Dicyclomine HCl | 67-92-5 | |
Diphenylpyraline HCl | 132-18-3 | |
Fesoterodine Fumarate | 286930-03-8 | |
Glycopyrrolate | 596-51-0 | |
Homatropine Bromide | Muscarinic AChR antagonist | 51-56-9 |
Homatropine Methylbromide | Muscarinic AChR antagonist | 80-49-9 |
J 104129 fumarate | 257603-40-0 | |
McN-A 343 | 55-45-8 | |
Mepenzolate Bromide | mAChR antagonist | 76-90-4 |
Methscopolamine | Muscarinic acetylcholine receptor blocker | 155-41-9 |
Milameline hydrochloride | 139886-04-7 | |
Nitrocaramiphen hydrochloride | 98636-73-8 | |
Oxotremorine M | 3854-04-4 | |
Oxotremorine sesquifumarate | 17360-35-9 | |
PD 102807 | 23062-91-1 | |
Pirenzepine dihydrochloride | 29868-97-1 | |
Pridinol Methanesulfonate | 6856-31-1 | |
PTAC oxalate | 201939-40-4 | |
Scopolamine butylbromide | 149-64-4 | |
Scopolamine hydrobromide | 114-49-8 | |
Solifenacin succinate | Muscarinic receptor antagonist | 242478-38-2 |
Telenzepine dihydrochloride | 147416-96-4 | |
Tiotropium Bromide | MAChR M antagonist | 136310-93-5 |
Tiotropium Bromide hydrate | Muscarinic antagonist | 139404-48-1 |
Tolterodine tartrate | 124937-52-6 | |
Tropicamide | Antimuscarinic drug | 1508-75-4 |
Trospium chloride | Antimuscarinic agent | 10405-02-4 |
Umeclidinium bromide | MAChR antagonist | 869113-09-7 |
VU 0238429 | 1160247-92-6 | |
VU 0255035 | 1135243-19-4 | |
VU 0357017 hydrochloride | 1135242-13-5 | |
VU 0365114 | 1208222-39-2 | |
VU 10010 | 633283-39-3 | |
W-84 dibromide | 21093-51-6 | |
Zamifenacin fumarate | 127308-98-9 |
This gene was present in the common ancestor of animals.
Organism | Taxonomy | Gene | Similarity | Type | Details |
---|---|---|---|---|---|
Chimpanzee (Pan troglodytes) |
Mammalia | CHRM1 30 31 |
|
OneToOne | |
Cow (Bos Taurus) |
Mammalia | CHRM1 30 31 |
|
OneToOne | |
Dog (Canis familiaris) |
Mammalia | CHRM1 30 31 |
|
OneToOne | |
Rat (Rattus norvegicus) |
Mammalia | Chrm1 30 |
|
||
Mouse (Mus musculus) |
Mammalia | Chrm1 30 17 31 |
|
OneToOne | |
Oppossum (Monodelphis domestica) |
Mammalia | CHRM1 31 |
|
OneToOne | |
Lizard (Anolis carolinensis) |
Reptilia | CHRM1 31 |
|
OneToOne | |
Tropical Clawed Frog (Silurana tropicalis) |
Amphibia | LOC100490434 30 |
|
||
Zebrafish (Danio rerio) |
Actinopterygii | CU019640.1 31 |
|
OneToMany | |
CHRM1 (1 of 2) 31 |
|
OneToMany | |||
Fruit Fly (Drosophila melanogaster) |
Insecta | mAcR-60C 30 31 32 |
|
OneToMany | |
CG7918 32 |
|
|
|||
African malaria mosquito (Anopheles gambiae) |
Insecta | GPRMAC1 30 |
|
||
Worm (Caenorhabditis elegans) |
Secernentea | gar-3 30 31 |
|
OneToMany | |
Sea Squirt (Ciona savignyi) |
Ascidiacea | -- 31 |
|
OneToMany |
SNP ID | Clinical significance and condition | Chr 11 pos | Variation | AA Info | Type |
---|---|---|---|---|---|
rs138454662 | Likely Benign: not provided | 62,910,369(-) |
A/T NM_000738.3(CHRM1):c.732T>A (p.Ser244=) |
SYNONYMOUS | |
rs139087623 | Uncertain Significance: not provided | 62,910,483(-) |
C/T NM_000738.3(CHRM1):c.618G>A (p.Thr206=) |
SYNONYMOUS | |
rs144107564 | Likely Benign: not provided | 62,910,411(-) |
C/T NM_000738.3(CHRM1):c.690G>A (p.Thr230=) |
SYNONYMOUS | |
rs148741609 | Benign: not provided | 62,909,964(-) |
T/G NM_000738.3(CHRM1):c.1137A>C (p.Thr379=) |
SYNONYMOUS | |
rs201075402 | Likely Benign: not provided | 62,911,059(-) |
G/A NM_000738.3(CHRM1):c.42C>T (p.Thr14=) |
SYNONYMOUS |
Disorder | Aliases | PubMed IDs |
---|---|---|
heart block, congenital |
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alzheimer disease |
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schizophrenia |
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attention deficit-hyperactivity disorder |
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disease of mental health |
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