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.
MeSH terms
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Animals
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Anti-Inflammatory Agents / adverse effects
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Anti-Inflammatory Agents / pharmacology
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Anti-Inflammatory Agents / therapeutic use*
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Atrophy / chemically induced
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Betamethasone Valerate / pharmacology
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Betamethasone Valerate / therapeutic use
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Croton Oil / administration & dosage
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Croton Oil / adverse effects
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Diflucortolone / analogs & derivatives
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Diflucortolone / pharmacology
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Diflucortolone / therapeutic use
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Disease Models, Animal
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Dose-Response Relationship, Drug
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Ear / pathology
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Edema / chemically induced
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Edema / drug therapy
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Edema / pathology
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Exudates and Transudates / drug effects
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Glucocorticoids / adverse effects
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Glucocorticoids / pharmacology
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Glucocorticoids / therapeutic use*
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Granuloma / chemically induced
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Granuloma / drug therapy
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Inflammation / chemically induced
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Inflammation / drug therapy*
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Male
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Organ Size / drug effects
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Pregnanediones
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Prodrugs / adverse effects
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Prodrugs / pharmacology
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Prodrugs / therapeutic use*
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Rats
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Rats, Sprague-Dawley
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Thymus Gland / drug effects
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Thymus Gland / pathology
Substances
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Anti-Inflammatory Agents
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Glucocorticoids
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NM 135
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Pregnanediones
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Prodrugs
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diflucortolone valerate
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Croton Oil
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Betamethasone Valerate
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Diflucortolone