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烷基取代吡唑并[3,4 - d]嘧啶(化合物88 - 765)的抗过敏活性

Antiallergic activity of alkyl substituted pyrazolo[3, 4-d]pyrimidine (compound 88-765).

作者信息

Gupta P P, Srimal R C, Avasthi K, Garg N, Chandra T, Bhakuni D S

机构信息

Division of Pharmacology, Central Drug Research Institute, Lucknow, India.

出版信息

Indian J Exp Biol. 1995 Jan;33(1):38-40.

PMID:9135673
Abstract

Compound 88-765 (4-amino-6-methylthio-1-(2', 2'-diethoxyethyl)-1 H-pyrazolo[3, 4-d]pyrimidine) has shown potent antiallergic activity in experimental models. The compound inhibited the passive cutaneous anaphylaxis (PCA) reaction in rats in dose-dependent manner (5-100 mg/kg, po) by 47 to 87%. In mice it inhibited PCA by 78% at 50 mg/kg, po. It also inhibited mast cell degranulation of normal and passively sensitised rats induced by compound 48/80 and egg albumin, respectively. These effects of Compound 88-765 were comparable with that of disodium cromoglycate (DSCG). The results suggest that compound 88-765 possesses potent antiallergic activity.

摘要

化合物88 - 765(4 - 氨基 - 6 - 甲硫基 - 1 -(2', 2'- 二乙氧基乙基)- 1H - 吡唑并[3, 4 - d]嘧啶)在实验模型中显示出强效抗过敏活性。该化合物以剂量依赖性方式(5 - 100毫克/千克,口服)抑制大鼠被动皮肤过敏反应(PCA),抑制率为47%至87%。在小鼠中,口服50毫克/千克时,它对PCA的抑制率为78%。它还分别抑制了由化合物48/80和卵清蛋白诱导的正常大鼠和被动致敏大鼠的肥大细胞脱颗粒。化合物88 - 765的这些作用与色甘酸钠(DSCG)相当。结果表明化合物88 - 765具有强效抗过敏活性。

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