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muscarinic M2 receptor; muscarinic acetylcholine receptor M2 (CHRM2)
Function:
- muscarinic acetylcholine receptor
- primary transducing effect is inhibition of adenylate cyclase (via Gi protein)
- in the CNS, CHRM2 is a presynaptic autoreceptor which down-regulates release of acetylcholine from presynaptic terminals
Structure: belongs to the G-protein coupled receptor 1 family
Compartment:
- cell membrane, cell junction, synapse
- presynaptic cell membrane
Polymorphism:
- genetic variations in CHRM2 can influence susceptibility to alcoholism
- genetic variations in CHRM2 can influence susceptibility to major depressive disorder
General
muscarinic receptor
phosphoprotein
Properties
SIZE: entity length = 466 aa
MW = 52 kD
COMPARTMENT: synaptic membrane
CELL: neuron
MOTIF: exoplasmic domain {1-22}
MOTIF: N-glycosylation site {N2}
N-glycosylation site {N3}
N-glycosylation site {N6}
N-glycosylation site {N9}
transmembrane domain {23-45}
cytoplasmic domain {46-59}
transmembrane domain {60-80}
exoplasmic domain {81-97}
MOTIF: cysteine residue {C96}
MODIFICATION: cysteine residue {C176}
transmembrane domain {98-119}
cytoplasmic domain {120-139}
transmembrane domain {140-162}
exoplasmic domain {163-184}
MOTIF: cysteine residue {C176}
MODIFICATION: cysteine residue {C96}
transmembrane domain {185-207}
cytoplasmic domain {208-388}
transmembrane domain {389-409}
exoplasmic domain {410-423}
transmembrane domain {424-443}
cytoplasmic domain {444-466}
MOTIF: Thr phosphorylation site {T446}
Thr phosphorylation site {T450}
Thr phosphorylation site {T465}
MISC-INFO: Ki [PIRENZEPINE] HIGH
INHIBITOR = AFDX116
INHIBITOR = METHOCTRAMINE
INHIBITOR = HIMBACINE
INHIBITOR = TRIPITRAMINE
Database Correlations
OMIM correlations
UniProt P08172
Pfam PF00001
Entrez Gene 1129
Kegg hsa:1129
References
- Conkilin et al PNAS 85:8698 (1988)
- Role of cholinergic therapy in treatment of Alzheimer's
disease & other dementias, Farlow, M et al, 2001
- Entrez Gene :accession 1129
- OMIM :accession 103780