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.
|
Authors | T Ishii, N Kibushi, T Nakajima, T Kakuta, N Tanaka, C Sato, K Sugai, I Kijima-Suda, H Kai, T Miyata |
Journal | Japanese journal of pharmacology
(Jpn J Pharmacol)
Vol. 78
Issue 4
Pg. 505-9
(Dec 1998)
ISSN: 0021-5198 [Print] Japan |
PMID | 9920209
(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)
|