Abstract
In an attempt to assess the role of histamine H3 receptors in the control of gastric acid secretion, the effects of the selective histamine H3 receptor agonist, (R) alpha-methylhistamine and antagonist, thioperamide were evaluated in the conscious gastric fistula cat under basal conditions and against different stimuli. (R) alpha-methylhistamine (0.05-0.2 mumol/kg/h) was ineffective against spontaneous and dimaprit-induced acid secretion; it also did not reduce significantly pentagastrin-induced acid output, but caused a dose-dependent (0.05-0.1 mumol/kg/h) and significant inhibition of the acid response to 2-deoxy-D-glucose. Thioperamide (0.02-0.04 mumol/kg/h) did not modify spontaneous acid secretion, whereas it evoked a significant enhancement of the acid response to submaximal doses (50 mg/kg i.v.) of 2-deoxy-D-glucose. Thioperamide completely reversed the inhibitory effect of (R) alpha-methylhistamine against 2-deoxy-D-glucose-induced secretion, while leaving unaffected the inhibition induced by somatostatin. These data suggest that histamine H3 receptors may be involved in the control of acid secretion stimulated by indirectly acting secretagogues.
MeSH Terms
Animals
Cats
Female
Gastric Acid/metabolism
Gastric Fistula/physiopathology
Methylhistamines/pharmacology
Piperidines/pharmacology
Receptors, Histamine/drug effects,physiology
Receptors, Histamine H3
Chemicals
Methylhistamines
Piperidines
Receptors, Histamine
Receptors, Histamine H3
alpha-methylhistamine
thioperamide
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Coruzzi G
Institute of Pharmacology, University of Parma, Italy.
Bertaccini G
Schwartz J C
References (10)
10 references, click to expand
-
Histamine release in the isolated vascularly perfused stomach of the rat: regulation by autoreceptors.
Br J Pharmacol. 1989 Mar;96(3):557-62
PMID: 2470453
-
Vagal gastric secretory stimulation by 2-deoxy-D-glucose.
Am J Physiol. 1965 Sep;209(3):452-60
PMID: 5320025
-
A novel class (H3) of histamine receptors on perivascular nerve terminals.
Nature. 1987 May 14-20;327(6118):158-60
PMID: 3033517
-
Definition and antagonism of histamine H 2 -receptors.
Nature. 1972 Apr 21;236(5347):385-90
PMID: 4401751
-
Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor.
Nature. 1983 Apr 28;302(5911):832-7
PMID: 6188956
-
Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H1, H2 and H3 receptor agonists and antagonists.
Eur J Clin Invest. 1989 Feb;19(1):1-10
PMID: 2567239
-
Histamine H3-receptors inhibit cholinergic neurotransmission in guinea-pig airways.
Br J Pharmacol. 1989 May;97(1):13-5
PMID: 2541854
-
Inhibition of guinea pig ileum contractions mediated by a class of histamine receptor resembling the H3 subtype.
J Pharmacol Exp Ther. 1987 Dec;243(3):874-80
PMID: 2826760
-
Highly potent and selective ligands for histamine H3-receptors.
Nature. 1987 May 14-20;327(6118):117-23
PMID: 3033516
-
The location of the chemoreceptor controlling gastric acid secretion during hypoglycaemia.
J Physiol. 1970 Feb;206(2):397-409
PMID: 5498491