Action of histamine receptor agonists and antagonists on the rat uterus

British Journal of Pharmacology
G BertacciniL Zappia

Abstract

1 Histamine and a series of compounds acting selectively on H1- and H2-receptors were tested on the isolated oestrous uterus of the rat. 2 Histamine had a dose-dependent inhibitory effect on the contractions elicited by acetylcholine. This action was unaffected by H1-blockers but was competitively inhibited by H2-blockers. The H1-selective agonist, 2-(2-aminoethyl)thiazole was ineffective at doses 100 times greater than those of histamine. Conversely, all the H2-agonists showed activity in the order of potency: N'-methylhistamine greater than histamine greater than N'-N'-dimethylhistamine greater than 5-methylhistamine greater than 5-methyl-N'-methylhistamine. Among the non-imidazole compounds, dimaprit had an activity identical to that of histamine, but all the dimaprit-like compounds showed negligible activity. 3 The data obtained suggest that in the rat uterus, (a) the activation of H2-receptors is responsible for the inhibitory effect of histamine and its analogues; (b) the integrity of the histamine molecule seems to be less crucial than that of the dimaprit molecule for the maintenance of the H2-activity, since changes in its structure modify but do not abolish the biological activity as they do in the case of dimaprit; (...Continue Reading

References

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Citations

Nov 1, 1986·Agents and Actions·G BertacciniM Adami
Feb 5, 1982·European Journal of Pharmacology·R K Goyal, S C Verma
Jan 13, 1984·European Journal of Pharmacology·J CortijoE Rubio
Jun 1, 1994·Respiration Physiology·K YamadaT Takishima
Jun 1, 1997·Journal of Veterinary Pharmacology and Therapeutics·T KitazawaT Taneike
Nov 1, 1984·Pharmacological Research Communications·E PoliG Bertaccini
Mar 1, 1989·The Journal of Pharmacy and Pharmacology·S E Ohia, A A Laniyonu
Feb 1, 1981·British Journal of Pharmacology·G Bertaccini, G Coruzzi
Feb 14, 2015·Journal of Ethnopharmacology·Tariro MawozaCharles Nhachi
Oct 13, 2005·Phytotherapy Research : PTR·Muhammad Nabeel Ghayur, Anwarul Hassan Gilani
Jan 1, 1993·The American Review of Respiratory Disease·K SekizawaT Takishima

Related Concepts

Metazoa
Castration
Antihistamines, Classical
Histamine H2 Antagonists
Imidazoles
Histamine Receptor
Uterine Contraction
Rats, Laboratory
In Vitro [Publication Type]

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