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[Effects of MY-5116 on PCA reaction and on the histamine release from peritoneal cells induced by antigen antibody reactions].
Nihon Yakurigaku Zasshi. 1986 Jan; 87(1):29-39.NY

Abstract

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.

Authors

No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
English Abstract
Journal Article

Language

jpn

PubMed ID

2420688

Citation

Takahashi, K, and T Shono. "[Effects of MY-5116 On PCA Reaction and On the Histamine Release From Peritoneal Cells Induced By Antigen Antibody Reactions]." Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica, vol. 87, no. 1, 1986, pp. 29-39.
Takahashi K, Shono T. [Effects of MY-5116 on PCA reaction and on the histamine release from peritoneal cells induced by antigen antibody reactions]. Nihon Yakurigaku Zasshi. 1986;87(1):29-39.
Takahashi, K., & Shono, T. (1986). [Effects of MY-5116 on PCA reaction and on the histamine release from peritoneal cells induced by antigen antibody reactions]. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica, 87(1), 29-39.
Takahashi K, Shono T. [Effects of MY-5116 On PCA Reaction and On the Histamine Release From Peritoneal Cells Induced By Antigen Antibody Reactions]. Nihon Yakurigaku Zasshi. 1986;87(1):29-39. PubMed PMID: 2420688.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Effects of MY-5116 on PCA reaction and on the histamine release from peritoneal cells induced by antigen antibody reactions]. AU - Takahashi,K, AU - Shono,T, PY - 1986/1/1/pubmed PY - 1986/1/1/medline PY - 1986/1/1/entrez SP - 29 EP - 39 JF - Nihon yakurigaku zasshi. Folia pharmacologica Japonica JO - Nihon Yakurigaku Zasshi VL - 87 IS - 1 N2 - 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. SN - 0015-5691 UR - https://www.unboundmedicine.com/medline/citation/2420688/[Effects_of_MY_5116_on_PCA_reaction_and_on_the_histamine_release_from_peritoneal_cells_induced_by_antigen_antibody_reactions]_ L2 - https://www.medicalonline.jp/meteo_linkout.php?issn=0015-5691&volume=87&issue=1&spage=29 DB - PRIME DP - Unbound Medicine ER -