Name | 6-(1-Pyrrolidinyl)-N-(2H-tetrazol-5-yl)-2-pyrazinecarboxamide |
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Synonyms |
6-(1-Pyrazolyl)-2-quinolone
2(1H)-Quinolinone,6-(1H-pyrazol-1-yl) 6-(1-pyrrolidinyl)-N-(1H-tetrazol-5-yl)-2-pyrazine-5-carboxamide HSR6071 |
Description | HSR6071 is an antiallergic agent with potential for the treatment of asthma. |
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Related Catalog | |
In Vivo | HSR-6071 suppresses antigen-induced histamine and SRS-A release from minced lung tissues of guinea-pigs sensitized passively with rabbit anti-EA serum and is a more potent inhibitor of the release of SRS-A than of histamine. On the other hand, histamine- or acetylcholine-induced bronchoconstriction in guinea-pigs is scarcely affected by HSR-6071 at doses sufficient to inhibit the experimental asthma, but LTD4-induced bronchoconstriction is dramatically inhibited. HSR-6071 inhibits cyclic AMP phosphodiesterase activity and produces relaxation of the guinea-pig isolated trachea[1]. HSR-6071 inhibits the IgE-mediated histamine release with an IC50 of 0.46 nM. HSR-6071 is effective not only by i.v. but also by p.o. administration on the IgE mediated PCA in rats. The most potent inhibition with HSR-6071 is observed when it is given p.o. 5 min before the antigen challenge, indicating the rapid absorption of HSR-6071 through the gastrointestinal tract[2]. |
Animal Admin | Rats: In order to find out the proper pre treatment time with HSR-6071, 0.03 mg/kg, i.vi or 1 mg/kg, p.o. of HSR-6071 was given at varying times before the antigen challenge[2]. |
References |
Density | 1.555g/cm3 |
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Molecular Formula | C10H12N8O |
Molecular Weight | 260.25500 |
Exact Mass | 260.11300 |
PSA | 116.07000 |
LogP | 0.29120 |
Index of Refraction | 1.717 |
Storage condition | 2-8℃ |
~84% 111374-21-1 |
Literature: Chemical and Pharmaceutical Bulletin, , vol. 38, # 1 p. 201 - 207 |
~% 111374-21-1 |
Literature: Chemical and Pharmaceutical Bulletin, , vol. 38, # 1 p. 201 - 207 |