KR-25018: A Novel, Orally Active Analgesic with Non-Narcotic Properties

Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the phamacological properties of KR-25018 were compared with those of morphine, capsaicin, and nonsteroidal antiinflammatory drugs (NSAIDs). The analgesic activities were evaluated in several animal models, using different stimuli, such as phenylbenzoquinone(PBQ)-induced weithing test, tail-filck test in mice and adjuvant arthritic flexion test in rat. The relationship of phamacological properties of KR-25018 to that of centrally acting opioids was assessed by the blocking test using naloxone. The analgesic potency of the KR-25018 $(MPED_{50}=0.89{\;}p.o.{\;}in{\;}PBQ-induced{\;}weithing{\;}test, {\;}MPED_{50}$=0.61$ s.c. in tail-flick test in mice0, with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.