British Journal of Pharmacology · 1975 · 75 citations · 11 references
MedicinePharmacologyAnesthesiaBiochemical PharmacologyPharmacodynamicsCardiovascular PharmacodynamicsVasodilator TherapyDose-response Curve FittingHistamine H1 Receptor AntagonistsHistamine Receptor AntagonismHistamine Receptor AntagonistsHistamine Receptor PharmacologyHistamine ReceptorsSelective Receptor AgonismVasodilator Pharmacology
1. The vasodilator activity of histamine has been studied in anaesthetized cats. 2. Histamine causes dose-dependent vasodilatation in the vasculature of the hind-limb and mesentery, perfused with blood at constant flow. 3. Experiments using the selective antagonists mepyramine and metiamide indicate the involvement of both H1- and H2-receptors in the vasodilator responses to histamine. Mepyramine (2.5 X 10(-6) mol/kg), causes displacement of the histamine dose-response curve. This displacement is maximum with a dose-ratio of about 10. Further dose-dependent displacement of the dose-response curve occurred after metiamide (4 X 10(-7) mol kg-1 min-1 and 2 X 10(-6) mol kg-1 min-1), although these doses of metiamide had no effect on histamine responses in the absence of mepyramine. 4. Vasodilator responses could also be elicited by the selective H1-receptor agonists, 2-methylhistamine, 2-(2-aminoethyl)pyridine and 2-(2-aminoethyl)thiazole and the selective H2-receptor agonist, 4-methylhistamine. 5. The selectivity of mepyramine and metiamide as histamine receptor antagonists was confirmed by their failure to reduce the vasodilator responses to acetylcholine, isoprenaline and bradykinin.
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Definition and Antagonism of Histamine H2-receptors
J. W. Black, W. A. M. Duncan, C. J. DURANT et al. · Nature · 1972 · 2.3K citations
The physiological action of β‐iminazolylethylamine
H. H. Dale, P. P. Laidlaw · The Journal of Physiology · 1910 · 880 citations · Full text