histamine H2 receptor; H2R; gastric receptor I (HRH2)

Function: - H2 subclass of histamine receptors mediates gastric acid secretion - also appears to regulate gastrointestinal motility & intestinal secretion - possible role in regulating cell growth & differentiation - activity is mediated by G proteins which activate adenylyl cyclase (Gs proteins) &, through a separate G protein-dependent mechanism, the phosphoinositide/ protein kinase C (PKC) signaling pathway (putative) 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 Pharmacology: - histamine-H2-receptor antagonists are used in treatment of gastirc acid disorders, i.e. dyspepsia, peptic ulcer disease, gastritis, GERD

General

glycoprotein histamine receptor

Properties

SIZE: entity length = 359 aa MW = 40 kD COMPARTMENT: cellular membrane MOTIF: exoplasmic domain {1-22} MOTIF: N-glycosylation site {N4} transmembrane domain {23-44} cytoplasmic loop {45-57} transmembrane domain {58-81} exoplasmic loop {82-92} MOTIF: cysteine residue {C91} MODIFICATION: cysteine residue {C174} transmembrane domain {93-114} MOTIF: aspartate residue {98} cytoplasmic loop {115-134} transmembrane domain {135-159} exoplasmic loop {160-180} MOTIF: cysteine residue {C174} MODIFICATION: cysteine residue {C91} transmembrane domain {181-204} MOTIF: aspartate residue {186} threonine residue {190} cytoplasmic loop {205-234} transmembrane domain {235-258} exoplasmic loop {259-267} transmembrane domain {268-289} cytoplasmic domain {290-359} MOTIF: cysteine residue {C305} MODIFICATION: palmitate COMPARTMENT: membrane

Database Correlations

OMIM 142703 UniProt P25021 Pfam PF00001 Kegg hsa:3274