| Identification | Back Directory | [Name]
HSR 6071 | [CAS]
111374-21-1 | [Synonyms]
HSR 6071
6-(1-Pyrrolidinyl)-N-(1H-tetrazol-5-yl)pyrazine-2-carboxamide
N-(1H-Tetrazol-5-yl)-6-(1-pyrrolidinyl)pyrazine-2-carboxamide
2-Pyrazinecarboxamide, 6-(1-pyrrolidinyl)-N-2H-tetrazol-5-yl- | [Molecular Formula]
C10H12N8O | [MOL File]
111374-21-1.mol | [Molecular Weight]
260.26 |
| Chemical Properties | Back Directory | [Melting point ]
288-294 °C (decomp)(Solv: dimethyl sulfoxide (67-68-5)) | [density ]
1.555±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
2.61±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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].
| [References]
[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. DOI:10.1111/j.2042-7158.1990.tb05399.x
[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. DOI:10.1254/jjp.52.87 |
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| Company Name: |
BOC Sciences
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| Website: |
https://www.bocsci.com |
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