Active cutaneous anaphylaxis test

The synthetic P-o-glucopyranoside 30 was converted to the cyanoglucoside rho-diocyanoside A (38a), which was isolated from the underground part of Rhodiola quadrifida (Pall.) Fisch. et Mey. (Crassulaceae) and found to show antiallergic activity in a passive cutaneous anaphylaxis test in rat. Acetylation of 30 gave an acetate (98% yield) which was subjected to ozonolysis to afford the aldehyde 39. The Horner-Emmons reaction of 39 using diethyl (l-cyanoethyl)phosphonate furnished (Z)-40a (32% yield from 30) and ( )-40b (10% yield from 30). The physical... 

Typical protocols for dermal sensitization, active systemic anaphylaxis, and passive cutaneous anaphylaxis tests are given in the article Animals in Drug Development, in this encyclopedia. In a typical gel-diffusion test, solutions of test compound, egg albumin (positive control), or vehicle (usually saline) are mixed with complete Freund s adjuvant. These mixtures are injected into animals (usually guinea pigs) of the... 

Chloro-oxazolo[4,5-/i]quinoline-2-carboxylic acid methyl ester was the most active compound in tests for inhibitors of antigen-induced release of histamine in vitro from rat peritoneal mast cells (IC50 of 0.3 p,M) and as inhibitors of IgE-mediated passive cutaneous anaphylaxis in the rat (ED50 (intraperitoneal) of 0.1 mg/kg in dose 0.5 mg/kg as an inhibitor of the test)—10 times and 60 times more potent, respectively, than the disodium salt of cromoglycic acid (85JMC1255). 

Hexahydropyrimido[l,2-a]azepin-4-ones 456, 463, and 467 display analgetic activity (77MI1). 10-Aminomethylene and 10-phenylhydrazino derivatives 478 (R = H) possess weak antiallergic effects in the passive cutaneous anaphylaxis (PCA) test (84JMC1253). 

Comments on the Studies in Rats. Passive cutaneous anaphylaxis in rats has been used extensively in the study of cromo-glycate-like compounds. Upon intravenous administration these compounds can abolish the vascular permeability changes, which follow mediator release from sensitized mast cells. This activity appears at doses which do not inhibit the effects of exogenous mediators. The oral activity of this type of compounds is generally nil and this holds also for doxanthrazole, which was inactive in the standard conditions of our test. 

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