Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0220723 (PCA)
 4,687 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Influences of the new compound MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano (3,2-C) quinoline-2-carboxylate and its metabolites were investigated on 48-hr rat homologous PCA (PCA) and the release of histamine from rat peritoneal mast cells induced by antigen antibody reaction (histamine release). MY-5116 (30 mg/kg) inhibited PCA significantly from 10 min to 2 hr after oral administration, and its ID50 (30 min) was 19.1 mg/kg. The inhibitory effect of its main metabolite, MY-1250, was the most potent among all the metabolites, 7HPQ, 8HPQ, 7CPQ and 8CPQ on the PCA (i.v.). Effect of MY-5116 suspended in 1% CMC on the PCA increased gradually after intravenous administration, but MY-1250 suppressed PCA immediately after intravenous injection. MY-5116 dissolved in DMSO in the concentration of 10(-7)-10(-6) g/ml didn't inhibit the histamine release, but the metabolite MY-1250 inhibited the histamine release. On the other experiment, MY-1250 inhibited the histamine release (IC50: 1.4 X 10(-7) g/ml), and MY-1250 was 17 times more potent than DSCG (2.4 X 10(-6) g/ml). From these results, it is suggested that MY-1250 is the main active metabolite of MY-5116.
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PMID:[Effects of MY-5116 on PCA reaction and on the histamine release from peritoneal cells induced by antigen antibody reactions]. 242 Jun 88

The effects of a new anti-allergic agent, MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylate, and its main metabolite, MY-1250: 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylic acid, on 48 hr homologous PCA (PCA) in rats and the release of histamine and SRS from rat peritoneal exudate cells (PEC) induced by IgE antibody in comparison with other anti-allergic agents were investigated. Also, the effects of MY-5116 and MY-1250 on antagonistic action against histamine and LTD4 were studied. MY-5116, tranilast and ketotifen inhibited PCA at oral doses of more than 3 mg/kg, 300 mg/kg and 0.3 mg/kg, respectively. MY-1250, DSCG and tranilast inhibited significantly the release of histamine from PEC induced by the antigen-antibody reaction in a dose-dependent manner, and the values of IC50 were 4.9 X 10(-8), 4.8 X 10(-6) and 4.6 X 10(-6) g/ml, respectively. Ketotifen inhibited significantly the release of histamine at a concentration of 10(-5) g/ml, but it accelerated significantly the release of histamine from PEC at a concentration of 10(-4) g/ml. MY-1250 and tranilast suppressed the release of SRS from PEC induced by the antigen-antibody reaction. The values of IC50 of MY-1250 and tranilast were 1.5 X 10(-6) and 2.1 X 10(-6) g/ml, respectively. MY-1250 suppressed slightly the release of SRS from PEC induced by A23187. MY-5116 showed no effect on the increase of vascular permeability induced by histamine, bradykinin and serotonin in rats.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Inhibitory effect on the release of mediators from rat peritoneal exudate cells and the antagonistic effect against mediators of MY-5116 and other anti-allergic agents]. 243 83

The effects of a new anti-allergic agent, MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylate, on experimental animal models of type I approximately type IV allergic reactions and the formation of IgE antibody were investigated. MY-5116 administered intraperitoneally at doses of 30 and 100 mg/kg suppressed significantly the homologous PCA in guinea pigs. MY-5116 administered intraperitoneally at the dose of 100 mg/kg also suppressed significantly the heterologous PCA in guinea pigs. MY-1250, the main active metabolite of MY-5116, showed no suppression on the Schultz-Dale reaction in guinea pigs, and MY-5116 showed no inhibition on the active systemic anaphylaxis in mice (type I). MY-5116 showed no inhibition on the reversed cutaneous anaphylaxis in rats (type II), the Forssman reaction in guinea pigs (type II), the Arthus reaction in mice (type III) and the delayed type hypersensitivity in mice (type IV). MY-5116 showed no suppression on the formation of IgE antibody in C3H/He and BALB/c mice and rats. From these results, it is concluded that MY-5116 selectively suppresses the experimental models of type I allergic reaction.
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PMID:[Effects of MY-5116 on experimental animal models of type I-type IV allergic reactions and the formation of IgE antibody]. 294 41