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Local anti-inflammatory activity and systemic side effects of NM-135, a new prodrug glucocorticoid, in an experimental inflammatory rat model.

Abstract
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.
AuthorsT Ishii, N Kibushi, T Nakajima, T Kakuta, N Tanaka, C Sato, K Sugai, I Kijima-Suda, H Kai, T Miyata
JournalJapanese journal of pharmacology (Jpn J Pharmacol) Vol. 78 Issue 4 Pg. 505-9 (Dec 1998) ISSN: 0021-5198 [Print] Japan
PMID9920209 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Inflammatory Agents
  • Glucocorticoids
  • NM 135
  • Pregnanediones
  • Prodrugs
  • diflucortolone valerate
  • Croton Oil
  • Betamethasone Valerate
  • Diflucortolone
Topics
  • Animals
  • Anti-Inflammatory Agents (adverse effects, pharmacology, therapeutic use)
  • Atrophy (chemically induced)
  • Betamethasone Valerate (pharmacology, therapeutic use)
  • Croton Oil (administration & dosage, adverse effects)
  • Diflucortolone (analogs & derivatives, pharmacology, therapeutic use)
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Ear (pathology)
  • Edema (chemically induced, drug therapy, pathology)
  • Exudates and Transudates (drug effects)
  • Glucocorticoids (adverse effects, pharmacology, therapeutic use)
  • Granuloma (chemically induced, drug therapy)
  • Inflammation (chemically induced, drug therapy)
  • Male
  • Organ Size (drug effects)
  • Pregnanediones
  • Prodrugs (adverse effects, pharmacology, therapeutic use)
  • Rats
  • Rats, Sprague-Dawley
  • Thymus Gland (drug effects, pathology)

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