产品
编 号:F038917
分子式:C10H12N8O
分子量:260.26
产品类型
结构图
CAS No: 111374-21-1
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产品详情
生物活性:
HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models.
体内研究:
The experimental asthma caused by IgE antibody in rats is inhibited by HSR-6071 (0.01-0.1 mg/kg; i.v.) in a dose-dependent manner. The bronchoconstriction mediated by IgE or IgG antibody in guinea-pigs is also prevented by HSR-6071 (0.3, 1,3 mg/kg; i.v.). HSR-6071 inhibits cyclic AMP phosphodiesterase activity and produces relaxation of the guinea-pig isolated trachea. 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.