The aim of this study was to evaluate the effects of H(1) (antazoline and astemizole) or H(2) (cimetidine and famotidine) histamine receptor antagonists on the clonic phase, tonic seizures and morality of mice challenged with aminophylline to induce convulsions in mice. Moreover, the total plasma and brain concentrations of theophylline were evaluated. Astemizole (1 mg/kg) did not affect the th...

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...

Histamine H3 receptor (H3R) antagonists enhance neurotransmitter release and are being developed for the treatment of a variety of neurological and cognitive disorders. Many potent histamine H3R antagonists contain an imidazole moiety that limits receptor selectivity and the tolerability of this class of compounds. Here we present the in vitro pharmacological data for two novel piperazine amide...

Adrenal steroidogenesis is closely correlated with increases in adrenal blood flow. Many reports have studied the regulation of adrenal blood flow in vivo and in perfused glands, but until recently few studies have been conducted on isolated adrenal arteries. The present study examined vasomotor responses of isolated bovine small adrenal cortical arteries to histamine, an endogenous vasoactive ...

In the present study the effects of both CCK receptor agonists and antagonists on antinociception induced by morphine in the tail-flick test have been evaluated. M orphine induced dose-dependent antinociception in mice. The response of morphine was potentiated by sulfated cholecystokinin-8 (CCK-8S) but not by unsulfated cholecystokinin-8 (CCK-8U). The CCK receptor antagonists MK-329 and L-...

Effects of histamine per se along with its specific agonists and antagonists were studied on the skin melanophores of Hemidactylus flaviviridis to study the role of histamine receptors in pigmentation. Histamine and 2-methyl histamine induced powerful melanin aggregation effects, leading to paling of the skin through stimulation of H1 receptors. On the other hand, 4-methyl histamine, a specific...

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...

Mast cell has a long history of being recognized as an important mediator-secreting cell in allergic diseases, and has been discovered to be involved in IBD in last two decades. Histamine is a major mediator in allergic diseases, and has multiple effects that are mediated by specific surface receptors on target cells. Four types of histamine receptors have now been recognized pharmacologically ...

foeniculum vulgare (fennel) has been widely used in traditional medicine for treatment of variousdiseases including pediatric colic. this study was designed to assess the antinociceptive effects of aqueousextract of f. vulgare on visceral pain and possible involvement of opioidergic, serotonergic, adrenergic andhistaminergic systems. the results of this study showed that aqueous extract of f. v...

To evaluate the ability of histamine to induce ventricular arrhythmias, we studied the effects of histamine on ventricular rhythmicity in the isolated guinea pig heart with complete atrioventricular conduction block. As a function of dose (0.1-30 microgram), histamine enhanced the idioventricular rate by increasing the rate of firing of the original pacemaker and also by causing the sudden appe...