The regulation of interleukin (IL)-6 synthesis by CAMP-increasing agents remains an unresolved issue. Since an increase in CAMP levels via activation of histamine Hz receptors does not induce IL-lP synthesis but enhances self-induction of IL-1 (Vannier, E., and Dinarello, C. k (1993) J. Clin. Invest. 92,281-28'71, we investigated whether histamine regulates IL-6 synthesis. Human peripheral b...

Histamine H3 receptor antagonists are being developed to treat a variety of neurological and cognitive disorders that may be ameliorated by enhancement of central neurotransmitter release. Here, we present the in vitro pharmacological and in vivo pharmacokinetic profiles for the nonimidazole, benzofuran ligand ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile] and ...

BACKGROUND Histamine can induce coronary vasospasm, leading to variant angina and acute myocardial infarction. However, the role of histamine in thrombus formation is ill defined. Hence, this study investigates whether histamine induces tissue factor (TF) expression in vascular cells. METHODS AND RESULTS Histamine (10(-8) to 10(-5) mol/L) induced TF expression in a concentration-dependent man...

conclusions the application of 5-ht1a, 5-ht2, 5-ht3, 5-ht4, 5-ht6 and 5-ht7 receptor antagonists, applied at concentrations lower than 1.0 µm did not modify the efs-induced contraction and relaxation responses, whichsuggests the unlikely involvement of endogenous 5-ht in mediating responses to efs in the described test conditions. materials and methods segments taken from the rat duodenum, jeju...

Exercise-induced arterial hypoxemia (EIAH) in human subjects may be associated with pulmonary injury/capillary stress failure-induced histamine release and is reported to be ameliorated by administration of H1 antihistiminics. EIAH is a routine occurrence in strenuously exercising Thoroughbreds, 75–100% of which also experience exercise-induced pulmonary hemorrhage (EIPH). In contrast with repo...

Cyclizine (1-benzhydryl-4-methyl-piperazine, CAS 82-92-8, CYC, I), a piperazine derivative, belongs to H1 antihistamine group of drugs that shows such pharmacological properties as anti-inflammatory, anti-allergic and anti-platelet effects, similar to other H1-receptor antagonists. In this study, two new tolyl and cumene derivatives of I (1-ethyl-4-[(p-isopropylphenyl) (p-tolyl) methyl]-piperaz...

We tested the novel hypothesis that endogenous adenosine (eADO) activates low-affinity A3 receptors in a model of neurogenic diarrhea in the guinea pig colon. Dimaprit activation of H2 receptors was used to trigger a cyclic coordinated response of contraction and Cl(-) secretion. Contraction-relaxation was monitored by sonomicrometry (via intracrystal distance) simultaneously with short-circuit...

BACKGROUND Gastro-oesophageal reflux afflicts up to 7% of all infants. Histamine-2 receptor antagonists are the most commonly prescribed medications for this disorder, but few controlled studies support this practice. AIM To evaluate the safety and efficacy of famotidine for infant gastro-oesophageal reflux disease. METHODS Thirty-five infants, 1.3-10.5 months of age, entered an 8-week, mul...

The net ionic fluxes of H+ and Na+ were examined in Heidenhain pouches during damage with sodium taurocholate solution. The increase in ionic flux which occurred with taurocholate could be prevented in animals given H1 and H2 histamine antagonists in combination. The results suggest that histamine mediates changes in the transmucosal ionic flux produced by bile acid.