| Identification | Back Directory | [Name]
FK-021 | [CAS]
101193-62-8 | [Synonyms]
FK-021 FR-71021 Quinotolast sodium 4-Oxo-1-phenoxy-N-(1-sodio-1H-tetrazol-5-yl)-4H-quinolizine-3-carboxamide | [Molecular Formula]
C17H13N6NaO3 | [MDL Number]
MFCD31382142 | [MOL File]
101193-62-8.mol | [Molecular Weight]
372.32 |
| Hazard Information | Back Directory | [Uses]
Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner. | [in vivo]
Quinotolast potently inhibits such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. When Quinotolast is given i.v. to rats, Quinotolast, dose-dependently inhibits PCA. The doses of Quinotolast required to inhibit the reaction by 50% (ED50) is 0.0063 mg/kg. Given p.o., Quinotolast inhibits the reaction. ED50 value for Quinotolast is 0.0081 mg/kg. Although almost complete inhibition is observed with Quinotolast at a dose of 0.32 mg/kg, its effect is slightly attenuated at a dose of 1 mg/kg[2]. | [IC 50]
Histamine; LTC4 | [References]
[1] Okayama Y, et al. Inhibition of histamine and eicosanoid release from dispersed human lung cells in vitro byquinotolast. Jpn J Pharmacol. 1995 Dec;69(4):375-80. DOI:10.1254/jjp.69.375 [2] Kobayashi K, et al. Effects of quinotolast, a new orally active antiallergic drug, on experimental allergic models. Jpn J Pharmacol. 1993 Sep;63(1):73-81. DOI:10.1254/jjp.63.73 |
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