Open AccessLocal Anti-inflammatory Activity and Systemic Side Effects of NM-135, a New Prodrug Glucocorticoid, in an Experimental Inflammatory Rat Model
Author(s) -
Takayuki Ishii,
Nobuyuki Kibushi,
Takashi Nakajima,
Tae Kakuta,
Noriko Tanaka,
Chiaki Sato,
Kei Sugai,
Isao KijimaSuda,
Hirofumi Kai,
Takeshi Miyata
Publication year - 1998
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.78.505
Subject(s) - pharmacology , chemistry , croton oil , side effect (computer science) , edema , betamethasone , carrageenan , systemic administration , inflammation , endocrinology , medicine , in vivo , biology , microbiology and biotechnology , computer science , programming language
The local anti-inflammatory activity and systemic side effects of NM-135 (6alpha,9-difluoro-11beta-hydroxy-16alpha-methyl-21[[2 ,3,4,6-tetrakis-O-(4-methylbenzoyl)-beta-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.