Champion, Hunter C., Trinity J. Bivalacqua, David G. Lambert, Rasheed A. Abassi, and Philip J. Kadowitz. Analysis of vasoconstrictor responses to histamine in the hindlimb vascular bed of the rabbit. Am. J. Physiol. 277 (Regulatory Integrative Comp. Physiol. 46): R1179–R1187, 1999.—Hemodynamic responses to histamine were investigated in the anesthetized rabbit. Intravenous injections of histami...

Few drugs have so rapidly gained an established place in modern medicine as the histamine H, receptor antagonists. As a result of the inventiveness of James Black and his colleagues, the theoretical concept of a second class of histamine receptors became a therapeutic reality. The failure of classic antihistamine drugs (more appropriately H1 receptor antagonists) to block the actions of histami...

1 Histamine and 2-methyl-histamine (H1-receptor agonist) caused dose-dependent increases in capillary permeability in albino mice, but 4-methyl-histamine (H2-receptor agonist) caused no significant increase. 2 Mepyramine (H1-receptor antagonist) blocked the histamine-induced increase in capillary permeability whereas burimamide (H2-receptor antagonist) produced no significant blockade of the hi...

Histamine caused a fall in blood pressure in anesthetized dogs and cats which was only partially attenuated by mepyramine (pyrilamine), a histamine type H1-receptor antagonist. Further treatment with burimide or metiamide, type H2-receptor antagonists, caused nearly complete attenuation of the response to histamine. Burimamide alone had no effect on vasodilatation produced by histamine in the d...

In a previous study, the relaxant and anticholinergic (functional antagonism) effects of Bunium persicum (B. persicum ) have been demonstrated on guinea pig tracheal chains. To elucidate the other mechanisms responsible for this relaxant effect, the inhibitory effect of this plant on histamine H1 receptors was examined in this study. The antihistaminic effects of aqueous and macerated extracts,...

1 Histamine produced dose-dependent contractile responses on both isolated perfused ear arteries and aortic strips of the rabbit. These responses were blocked by mepyramine and potentiated by both metiamide and dithiothreitol. 2 In the presence of maximum potentiation by metiamide, dithiothreitol still potentiated the contractile response to histamine of both preparations. 3 In the presence of ...

Histamine membrane receptors are defined as either H1 (blocked by diphenhydramine-like antagonists) or H2 (blocked by cimetidine-like agents). We now report the solubilization, separation, and partial characterization of specific H1 and H2 membrane receptors from calf thymocytes. Membrane fragments were incubated with [3H]histamine either alone or with unlabeled histamine, diphenhydramine, or c...

in a previous study, the relaxant and anticholinergic (functional antagonism) effects of bunium persicum (b. persicum ) have been demonstrated on guinea pig tracheal chains. to elucidate the other mechanisms responsible for this relaxant effect, the inhibitory effect of this plant on histamine h1 receptors was examined in this study. the antihistaminic effects of aqueous and macerated extracts,...

Several lines of evidence have indicated that many nuclei in the brain including preoptic nucleus, AV3V, subfornical organ, septal area and lateral hypothalamus are the targets of efferents from chemo-sensitive and pressure-sensitive systems. These areas may concern with regulation of fluid homeostasis. In the present study, intracerebroventricular injections were carried out in all experiments...

Competition experiments with [H]mepyramine showed that cetirizine and its enantiomers, levocetirizine and (S)-cetirizine, bound with high affinity and stereoselectivity to human H1 histamine receptors (Ki values of 6, 3, and 100 nM, respectively). Cetirizine and levocetirizine were 600-fold more selective for H1 receptors compared with a panel of receptors and channels. Binding results indicate...