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The ability of azelastine to influence antigen-induced contractile responses (Schultz-Dale phenomenon) in isolated tracheal segments of the guinea-pig was investigated and compared with selected antiallergic drugs and inhibitors of arachidonic acid metabolism. Indomethacin produced a significant

Recently, mast cell stabilizers, so called antiallergic drugs, that also have blocking effects on receptors for chemical mediators (CM) have been developed. The present study investigated the effects of a new antiallergic drug, epinastine (3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazol [1,5-a]azepine

In order to clarify the interspecies differences in the metabolism of emedastine difumarate (KG-2413), in vitro metabolism was studied with liver preparations of rats and guinea pigs. The activities of hydroxylase, N-oxidase and N-demethylase, of emedastine were evaluated with liver 9000 x g

LA 2851, 2-4-diamino-7-methyl-pyrazolo (1,5a) 1, 3, 5 triazine has been found to possess potent bronchodilator and inhibitor properties on experimental active and passive anaphylaxis. In vitro evaluation on guinea-pig trachea indicated that LA 2851 had relaxant properties on unstimulated and

Tylogenin, a steroidal aglycone generated by acid hydrolysis from two seasonal glycosides occurring in Tylophora sylvatica, inhibits IgE-induced basophil mediator release for allergic reactions. In the rabbit basophil-dependent serotonin release (BDSR) assay system, the inhibitory activity of

SQ 13,847, a pyrazolo[1,5-c]quinazoline with potent oral antiallergic activity in the rat, was compared with its principal oxidative metabolite, SQ 12,903, for ability to block the release of histamine from the rat mast cell in vitro. SQ 12,903, at concentrations in the range of 0.3 to 2 micrometer,

The ability of azelastine to inhibit allergic histamine release from rabbit mixed leukocytes was studied and compared with selected antiallergic drugs. Azelastine, ketotifen, diphenhydramine, theophylline and disodium cromoglycate (DSCG) produced concentration-dependent inhibition of allergic

Selected derivatives of 9-oxo-1H,9H-benzothiopyrano[2,3-d]-1,2,3-triazole, a new heterocyclic ring system, and their S-oxides have been prepared and evaluated for antiallergic activity in the rat passive cutaneous anaphylaxis screen. Several of the compounds show intravenous potencies similar to or

The antihistaminic effect of 2-[2-[4-(diphenylmethyl)-1-piperadinyl]ethoxy] benzoic acid maleate (ZCR-2060), a newly synthesized antiallergic agent, was investigated in both in vitro and in vivo studies. ZCR-2060 clearly antagonized histamine-induced contraction of isolated guinea pig ileum and

Some benzothienoquinolinecarboxylic acids were synthesized and tested in the rat passive cutaneous anaphylaxis (PCA) assay as potential antiallergic agents. Many of the compounds showed activity comparable to that shown by disodium cromoglycate (DSFG); two of them,

OBJECTIVE The aim of this study was to investigate the cytotoxic effect of topical ocular allergic agents with H1-receptor antagonism and inhibition of histamine release from mast cells on the cultured conjunctival cells of rabbit in vitro. METHODS Cell damage by the topical ocular antiallergic

Interspecies differences in the pharmacokinetics of an antiallergic agent, 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1,4-diazepin-1-yl)benzimid azole difumarate (KG-2413) after intravenous administration were investigated in rats, guinea pigs and dogs. The disappearance of unchanged KG-2413 base was

Effects of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazol e difumarate (KB-2413) on chemical mediators were investigated in vitro and in vivo. Antihistaminic activity of KB-2413 in vitro was about 2, 7 and 5 times more potent than those of chlorpheniramine, diphenhydramine and

Inosine pranobex (INPX) at concentrations greater than 10(-3) M inhibits significantly the concanavalin A or antihuman IgE induced histamine release from human mast cells. The inosine moiety of the compound does not contribute to this effect, but rather interferes with it. The other component, the

In the present report we describe the preparation of LC-6.2HCl, a soluble derivative of the synthetic bispyrazole LC-6. Because the latter was practically insoluble in aqueous and organic media, experiments which indicated that it had antiallergic activity were confined to in vivo studies following