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PMID: 7555464 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Review

An update on histamine H3 receptors and gastrointestinal functions.

Digestive diseases and sciences ·Vol. 40 ·No. 9 ·1995-09-00 ·Pages 2052-63

Bertaccini G, Coruzzi G

Abstract

The distribution and functions of histamine H3 receptors in the gastrointestinal tract is reviewed with particular reference to the effects on gastric acid secretion, mucosal protection, and intestinal motility. Histamine H3 receptor activation has negative effects on acid secretion induced by indirect secretagogues in cats, dogs, and rabbits; less clear effects were found in rats. An inhibitory effect on histamine release induced by different stimuli was observed in rats, rabbits, and dogs after H3 receptor agonists, thus supporting the idea that H3 receptors occur in ECL cells. (R)-alpha-methylhistamine has a marked protective effect against gastric lesions induced by ethanol in rats, being slightly less effective against aspirin and stress. H3 receptor activation decreases the intestinal motility induced by electrical stimulation in a variety of gut preparations, reducing both cholinergic and NANC neurotransmitter release. In this tissue the inhibitory effects mediated by histamine H3 receptors seem to be coupled, via a G protein, to a restriction of Ca2+ access into the nerve terminal; other mechanisms, however, have been suggested in the gastric mucosa. Histamine H3 receptors have already been subdivided into two receptor subtypes, H3A and H3B, the former being the subtype predominant in the gastrointestinal tissue. The increasing availability of selective agonists and antagonists of H3 receptors will unravel possible novel actions and physiological roles of histamine.

MeSH Terms
Animals Digestive System Physiological Phenomena Gastric Acid/metabolism Gastric Mucosa/physiology Gastrointestinal Motility/physiology Humans Intestinal Mucosa/physiology Receptors, Histamine H3/physiology
Chemicals
Receptors, Histamine H3
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Bertaccini G
Institute of Pharmacology, University of Parma, Italy.
Coruzzi G
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Article Info
Journal
Digestive diseases and sciences
Abbr.
Dig Dis Sci
ISSN
0163-2116
DOI
10.1007/BF02208678
Published
1995-09-00
Pages
2052-63
Language
English
Region
United States
NLM ID
7902782
Subset
IM
External Links
PubMed source DOI: 10.1007/BF02208678 View journal details
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