Anti-inflammatory activity of rolipram in a rat ear edema model.
In the present study the anti-inflammatory activity of the phosphodiesterase inhibitor rolipram (ZK 62,711, CAS 61413-54-5) was tested in a rat model where edema was induced in the ears of the animals by the epicutaneous application of croton oil in ethanol (5%, by volume). The administration of 0.015, 0.15 and 1.5 mg rolipram per ear dose-dependently inhibited the formation of edema. Concomitantly, the body temperature of the rats was decreased. 4-14% of rolipram was percutaneously absorbed within a 5-h interval. The absorbed proportion, represented by the area under the plasma level-time curve, correlated with the inhibition of edema formation and with the decrease in body temperature.
Krause
W
W
Research Laboratories of Schering Aktiengesellschaft, Berlin, Fed. Rep. of Germany.
Kühne
G
G
D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D001831:Body Temperature / Q000187:drug effects; D003436:Croton Oil; D004305:Dose-Response Relationship, Drug; D004431:Ear, External / Q000473:pathology; D004487:Edema / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control*; D005260:Female; D009929:Organ Size / Q000187:drug effects; D011760:Pyrrolidinones / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D020889:Rolipram; D012869:Skin Absorption
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011760:Pyrrolidinones; D003436:Croton Oil; D020889:Rolipram