Local Anti-inflammatory Activity and Systemic Side Effects of NM-135, a New Prodrug Glucocorticoid, in an Experimental Inflammatory Rat Model

The Japanese Journal of Pharmacology

Hirofumi Kai²  Nobuyuki Kibushi¹  Isao Kijima-Suda¹  Noriko Tanaka¹  Chiaki Sato¹  Kei Sugai¹  Takashi Nakajima¹  Takayuki Ishii¹  Takeshi Miyata²  Tae Kakuta¹ 

[1] Tokyo Pharmaceutical Research Laboratories, Nissin Food Products Co., Ltd.;Department of Pharmacological Sciences, Faculty of Pharmaceutical Sciences, Kumamoto University

关键词: Glucocorticoid;    Systemic side effect;    Prodrug;   

DOI  :  10.1254/jjp.78.505

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(15)Cited-By(1)The local anti-inflammatory activity and systemic side effects of NM-135 (6α, 9-difluoro-11β-hydroxy-16α-methyl-21[[2, 3, 4, 6-tetrakis-O-(4-methylbenzoyl)-β-D-glucopyranosyl]oxy]-pregna-1, 4-diene-3, 20-dione) in croton oil-induced granuloma pouches and ear edema in rats were studied. The local anti-inflammatory activity of NM-135 was stronger than that of betamethasone 17-valerate (BV). As to systemic side effects, BV and diflucortolon valerate (DFV) caused thymolysis at the doses required for the anti-inflammatory activity. In contrast, no clear systemic side effect was observed in rats administered NM-135 at the dose producing the anti-inflammatory activity. These results suggest that NM-135 is a drug exhibiting a high degree of dissociation between the local anti-inflammatory activity and systemic side effects.

【 授权许可】

Unknown