For research use only. Not for therapeutic Use.
HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models[1][2].
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].
| Catalog Number | I013354 |
| CAS Number | 111374-21-1 |
| Synonyms | 6-pyrrolidin-1-yl-N-(2H-tetrazol-5-yl)pyrazine-2-carboxamide |
| Molecular Formula | C10H12N8O |
| Purity | ≥95% |
| InChI | InChI=1S/C10H12N8O/c19-9(13-10-14-16-17-15-10)7-5-11-6-8(12-7)18-3-1-2-4-18/h5-6H,1-4H2,(H2,13,14,15,16,17,19) |
| InChIKey | LUJDHCXCWJFNOJ-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)C2=NC(=CN=C2)C(=O)NC3=NNN=N3 |
| 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. |
