Drug intelligence / Profile preview

histamine

Development stage
Approved
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Topical
01

Overview

Histamine is an endogenous biogenic amine derived from the decarboxylation of the amino acid histidine. It acts as a potent mediator in immune and inflammatory responses, primarily stored in mast cells and basophils in tissues throughout the body. Upon release, it exerts multiple physiological effects by binding to four known G protein-coupled receptors (H1, H2, H3, H4). These actions include vasodilation and increased vascular permeability (contributing to inflammation), smooth muscle contraction (notably bronchoconstriction), stimulation of gastric acid secretion in the stomach, acceleration of heart rate, neurotransmission within the central nervous system (as a monoaminergic neurotransmitter), and modulation of immune cell chemotaxis. Histamine is also present in various plants and bacteria; it can be found naturally or produced during food spoilage or fermentation[2][4][6].

Brand names
Histatrol
Other names
组胺1H-imidazole-4-ethanamineErgamineErgotidineβ-Imidazolyl-4-ethylamineImidazole-4-ethylamineImidazole4-ethylamineImidazole 4-ethylamine2-(4-Imidazolyl)ethylamine5-ImidazoleethylamineEthylamine, 2-imidazol-4-yl-Free histamineImidazole, 4-(2-aminoethyl)-Theramine4-(2-Aminoethyl)-1H-imidazoleβ-Aminoethylglyoxaline
02

Targets

HRH4 (Histamine H4 receptor)HRH1 (Histamine H1 Receptor)HRH2 (Histamine H2 Receptor)HRH3 (Histamine Receptor H3)

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