| Bioactivity | HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models[1][2]. | ||||||||||||
| In Vivo | 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[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]. | ||||||||||||
| Name | HSR6071 | ||||||||||||
| CAS | 111374-21-1 | ||||||||||||
| Formula | C10H12N8O | ||||||||||||
| Molar Mass | 260.26 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Makino E, et al. Inhibitory effect of HSR-6071, a new anti-allergic agent, on experimental asthma in rats and guinea-pigs. J Pharm Pharmacol. 1990 Apr;42(4):236-41. [2]. Makino E, et al. Potent inhibitory activity of HSR-6071, a new antiallergic agent, on passive cutaneousanaphylaxis (PCA). Jpn J Pharmacol. 1990 Jan;52(1):87-94. |