It has been reported that some of H1 receptor antagonists have important effects on cardiovascular system. Terfenadine as a non-sedative H1 receptor antagonist has an arrhythmogenic activity. In this study we have shown the effects of four antihistamine drugs: terfenadine, loratadine, clemastine and diphenhydramine, on the rate and contractions of isolated rat atria. Terfenadine (1-10 μM) cause...

Pharmacodynamic mechanisms of diabetes induced by antipsychotic drugs remain unclear, while numerous receptors have been suspected to be involved in the genesis of this Adverse Drug Reaction (ADR). We investigated potential relationships between antipsychotics׳ receptor occupancy (serotonin 5-HT1A, 5-HT2A, 5-HT2C, histamine H1, muscarinic M3, adrenergic α1, α2 or dopaminergic D2 D3 occupancies)...

OBJECTIVE Crocin, as an active constituent of saffron, has many biological functions including antioxidant and anti-inflammatory activities. The present study was aimed to investigate the effects of crocin and chlorpheniramine on local edema induced by histamine. MATERIALS AND METHODS Local edema was induced by subcutaneous injection of histamine (100 μl, 0.1%) in ventral surface of right hin...

In the present study, effects of intracerebroventricular (icv) administration of histamine, mepyramine (H1-receptor antagonist) and famotidine (H2-receptor antagonist) have been investigated on the formalin test in rats. Subcutaneous injection of formalin (50 microl, 1%) into the ventral surface of the left hind paw produced a marked biphasic pain response (first phase: 0-5 min and second phase...

Vasoactive intestinal peptide (VIP) is known to induce histamine release in human skin and known to include a NO-dependent dilation in several other vascular beds. However, the relative contribution of histamine and NO to VIP-mediated vasodilation in human skin is unknown. Forty three subjects volunteered to participate in two studies designed to examine the mechanism of VIP-mediated vasodilati...

Although histamine plays an important role in the pathophysiology of asthma through stimulation of H1 receptors, H1 antagonists are of only limited use in this disease when given orally. In order to investigate the pharmacological response to a specific H1 antagonist administered by different routes, we measured the effect of inhaled clemastine on airway responsiveness to histamine aerosol and ...

Vasoactive intestinal peptide (VIP) is known to induce histamine release in human skin and to include a nitric oxide (NO)-dependent dilation in several other vascular beds. However, the relative contribution of histamine and NO to VIP-mediated vasodilation in human skin is unknown. Forty-three subjects volunteered to participate in two studies designed to examine the mechanism of VIP-mediated v...

We examined ZO-1 protein content in cultured retinal vascular endothelial cells to test the hypothesis that histamine alters tight-junction-protein expression. Histamine (10(-9) -10(-4) M) causes a reversible concentration-dependent reduction of ZO-1 protein content, mediated by both H1 and H2 receptors. Histamine reduces ZO-1 expression within the time associated with increased paracellular pe...

It is well known that histamine produces constriction via H1 receptors and decreases tracheal smooth muscle tone via H2 and H3 receptors. In addition, it has already been reported that 3-methylhistamine and phenylethylamine are competitive antagonists of histamine N-methyl-transferase (HMT), the enzyme responsible for rapid inactivation of histamine. Our results suggest the possibility that 3me...