KR-25018: A novel, orally active analgesic with non-narcotic properties
KR-25018: A novel, orally active analgesic with non-narcotic properties
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DOI：
10.1007/bf02974166
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发表时间：
1994-01-01
期刊：
影响因子：
--
通讯作者：
Kong, Jae Yang
中科院分区：
文献类型：
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作者：
Lee, Buyean;Kim, Jae Hong;Kong, Jae Yang
在新的苯乙酰胺系列中，辣椒素的衍生物之一KR-25018被发现具有很强的镇痛活性。因此，我们将KR-25018的药理学性质与吗啡、辣椒素和非甾体抗炎药（NSAIDs）进行了比较。采用不同刺激物，如苯基苯并醌（PBQ）诱导小鼠扭体实验、轻甩尾实验和大鼠佐剂关节炎屈曲实验，对其镇痛作用进行了评价。采用纳洛酮阻断试验评价kr25018与中枢作用阿片类药物的药理作用关系。与吗啡和非抗炎药作用机制不同，kr25018的镇痛效力与吗啡相当（pbq诱导扭体实验MPED-50 = 0.89 p.o.，小鼠甩尾实验MPED-50 = 0.61 s.c.）。
Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the pharmacological 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 writhing test, tail-flick test in mice and adjuvant arthritic flexion test in rat. The relationship of pharmacological 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 writhing test, MPED-50 = 0.61 s.c. in tail-flick test in mice), with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.