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Opioid activity of enkephalin analogs containing the kyotorphin related structure in the amino terminus



Opioid activity of enkephalin analogs containing the kyotorphin related structure in the amino terminus



Neuropharmacology 23(4): 395-400



The pharmacological activity of 8 analogs of enkephalin [ENK] containing L-Arg or D-Arg in position 2 [Arg2-Met5-ENK, Arg2-Leu5-ENK, Arg2-Met5-ENK amide, Arg2-Leu5-ENK amide, D-Arg2-Met5-ENK, D-Arg2-Leu5-ENK, D-Arg2-Met5-ENK amide and D-Arg2-Leu5-ENK amide] were examined. All peptides showed weaker inhibitory effects than those of naturally-occurring ENK on the isolated guinea-pig ileal longitudinal muscle and the mouse vas deferens. These 8 peptides were more potent than enkephalins in the analgesic test involving intracisternal administration to mice. By the i.v. route, only D-Arg2-Met5-ENK, which induced a most potent analgesia by intracisternal injection, was effective. D-Arg2-Met5-ENK showed a similar binding affinity to that of Met5-ENK in the opioid .mu.-receptor binding assay but had a lower .delta.-receptor binding affinity than did Leu5-ENK. Administration of thiorphan, an enkephalin dipeptidyl carboxypeptidase inhibitor, did not potentiate the analgesic effect of D-Arg2-Met5-ENK while it dramatically enhanced the effect of D-Ala2-Met5-ENK when both drugs were administered concomitantly into the cisterna magna of mice.

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Accession: 006036762

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