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histamine H1 receptor (HRH1)
Function:
- action may be mediated via phosphoinositide hydrolysis [2]
- in peripheral tissues, histamine H1 receptors:
a) mediate contraction of smooth muscles
b) increase capillary permeability due to contraction of terminal venules
c) mediate catecholamine release from adrenal medulla
- in CNS, histamine H1 receptors mediate neurotransmission
- potential sites of phosphorylation in the 3rd cytoplasmic loop may play a role in regulating signal transduction
- blockade causes weight gain & sedation
Structure:
- belongs to the G-protein coupled receptor 1 family
- membrane pocket formed by 7 transmembrane regions forms ligand binding site & provides for interaction of receptor with G protein
Compartment: cell membrane
Interactions
molecular events
General
glycoprotein
histamine receptor
Properties
SIZE: entity length = 487 aa
MW = 56 kD
COMPARTMENT: cellular membrane
MOTIF: exoplasmic domain {1-29}
MOTIF: N-glycosylation site {N5}
N-glycosylation site {N18}
transmembrane domain {30-49}
cytoplasmic loop {50-63}
transmembrane domain {64-83}
exoplasmic loop {84-101}
MOTIF: cysteine residue {C100}
MODIFICATION: cysteine residue {C180}
transmembrane domain {102-123}
cytoplasmic loop {124-145}
transmembrane domain {146-165}
exoplasmic loop {166-189}
MOTIF: cysteine residue {C180}
MODIFICATION: cysteine residue {C100}
transmembrane domain {190-210}
cytoplasmic loop {211-418}
transmembrane domain {419-438}
exoplasmic loop {439-450}
MOTIF: cysteine residue {C445}
MODIFICATION: palmitate
COMPARTMENT: membrane
transmembrane domain {451-470}
cytoplasmic domain {471-487}
MISC-INFO: INHIBITOR = PYRILAMINE
Database Correlations
OMIM 600167
UniProt P35367
Pfam PF00001
Kegg hsa:3269
References
- UniProt :accession P35367
- Tilly BC et al.
Histamine-H1-receptor-mediated phosphoinositide hydrolysis,
Ca2+ signalling and membrane-potential oscillations in human
HeLa carcinoma cells.
Biochem J. 1990 Feb 15;266(1):235-43.
PMID: 2155607