6-二甲基氨基-9-（β-D-阿拉伯呋喃糖基）-9H-嘌呤：感染猴水痘病毒的猴子体内的药代动力学及抗病毒活性

6-Dimethylamino-9-(beta-D-arabinofuranosyl)-9H-purine: pharmacokinetics and antiviral activity in simian varicella virus-infected monkeys.

作者信息

Soike K F, Huang J L, Lambe C U, Nelson D J, Ellis M N, Krenitsky T A, Koszalka G W

机构信息

Tulane Regional Primate Research Center, Tulane University, Covington, LA 70433.

出版信息

Antiviral Res. 1993 Jan;20(1):13-20. doi: 10.1016/0166-3542(93)90055-n.

DOI:10.1016/0166-3542(93)90055-n

PMID:8457145

Abstract

6-Dimethylamino-9-(beta-D-arabinofuranosyl)-9H-purine (ara-DMAP) effectively prevented the development of rash and appreciably reduced viremia in simian varicella virus-infected monkeys. Doses of 100 and 50 mg/kg/day, administered orally, were highly effective. The lowest dose of 20 mg/kg/day was much less effective in preventing moderate viremia. However, the 20 mg/kg/day did prevent the development of rash in two of three monkeys. All three doses of ara-DMAP reduced liver infection as reflected by lower aspartate aminotransferase values in the sera of the African green monkeys. Orally administered ara-DMAP was rapidly absorbed. However, significant variation among individual monkeys in the AUC values, peak plasma levels, and plasma half-lives were observed.

摘要

6-二甲基氨基-9-(β-D-阿拉伯呋喃糖基)-9H-嘌呤（ara-DMAP）能有效预防皮疹的出现，并显著降低猿猴水痘病毒感染猴子的病毒血症。口服剂量为100和50毫克/千克/天非常有效。最低剂量20毫克/千克/天在预防中度病毒血症方面效果要差得多。然而，20毫克/千克/天的剂量确实在三只猴子中的两只身上预防了皮疹的出现。所有三种剂量的ara-DMAP都降低了肝脏感染，这从非洲绿猴血清中较低的天冬氨酸转氨酶值可以看出。口服ara-DMAP吸收迅速。然而，观察到个体猴子在AUC值、血浆峰值水平和血浆半衰期方面存在显著差异。