Target intelligence / Profile preview

Histamine Receptor H2 Subtype

Molecular classification
G protein-coupled receptor, GPCR, Family 1/rhodopsin-like GPCRs
01

Overview

The histamine receptor H2 is a member of the rhodopsin-like family of G protein-coupled receptors (GPCRs). It is an integral membrane protein that plays a central role in mediating the physiological effects of histamine, particularly in stimulating gastric acid secretion. It couples primarily to the Gs alpha subunit, leading to activation of adenylate cyclase and increased cyclic AMP (cAMP) production.

Other names
H2 receptorHRH2
02

Mechanism of action

H2 receptor antagonists competitively block the binding of histamine to H2 receptors on parietal cells, reducing gastric acid secretion.

03

Biological functions

Stimulation of gastric acid secretionRegulation of gastrointestinal motilityRegulation of intestinal secretionModulation of cell growthModulation of cell differentiationVasodilationNeurotransmission
04

Disease associations

Gastroesophageal reflux disease (GERD)Peptic ulcersZollinger-Ellison syndrome
05

Interacting drugs

Famotidine

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