새로운 캅사이신유도체 DA-5018 의 피하주사 및 구소도포시 진통효과 = Analgesic Effects of DA-5018 , a New Capsaicin Derivative , after Subcutaneous Injection and Topical Apphcation

다국어 초록 (Multilingual Abstract)

The analgesic effects of DA-5018, a new capsaicin derivative, were evaluated in various experimental pain models. Drugs were administered subcutaneously or topically. When drugs were administered subcutaneously, 1) the ED_(50) values of DA-5018, morphine ·HCl, capsaicin and acetaminophen were 0.091-2.0, 0.3-4.3, 1.4-26.5 and 45.4-643 mg/kg, respectively in various pain or inflammatory models including acetic acid writhing, formalin, tail flick, Randall-Selitto, hot plate and croton oil-induced ear edema test, 2) the AD₂ values (the dose for doubling of pain threshold of vehicle control) of DA-5018, capsaicin and ketoprofen were 1.07±0.18, 23.47±4.46 and 2.97±0.43 mg/kg in Freund`s complete adjuvant (FCA)-induced arthritic pain model. And by topical application, 1) neither DA-5018 0.3% cream nor Zostrio-HP (capsaicin 0.075%) were effective in formalin test, 2) although DA-5018 0.3% cream significantly inhibited the croton oil-induced ear edema being better than Zostrix-HP and Kenofen (ketoprofen 3%). 3) Ln FCA model, DA-5018 0.3% cream reversed the decreased pain threshold of arthritic rat from 136.4 g (day 0) to 289.0 g (day 5) and 250.1 g (day 10), which was similar to Zostrix-HP, These results suggest that DA-5018 administered subcutaneously has a potent and broad analgesic spectrum than nonsteroidal antiinflammatory drugs against acute and chronic pain, and by topical application it exerts comparable analgesic and antiinffammatory effects to capsaicin cream.