Effect of Morphine and Its Conjugates on the Isolated Ileal Preparation of Guinea-pig

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The present study was undertaken to reconfirm the previous conclusion that morphine-6-conjugates cause potent analgesia by themselves in mice. For this purpose, inhibitory effect of morphine and its three pairs of 3-and 6-conjugates (glucuronides, ethereal sulfates and phosphates) to nicotine-induced contraction of the isolated guinea-pig ileum was examined. The potency of these conjugates was found to decrease in the following order, morphine-6-sulfate>morphine-6-glucuronide>morphine, morphine-3-and 6-phosphate>morphine-3-glucuronide, morphine-3-sulfate, indicating fairly good accordance with order in their analgesic effects in mice. The present experiment again provided strong suggestion that the above biological effect was attributable to the conjugates themselves.
社団法人日本薬学会の論文
1977-03-25