Analgesic, receptor binding, and peripheral opioid activities of synthetic dermorphin‐dynorphin hybrid peptides

CHEWN‐LANG ‐L HO, JANE‐LING ‐L KO, LING‐LING ‐L HWANG, KUNG‐TSUNG ‐T WANG

研究成果: 雜誌貢獻文章同行評審

4 引文 斯高帕斯(Scopus)

摘要

The effects of substituting the enkephalin moiety of dynorphin with the dermorphin sequence were studied on the receptor preference, analgesic, and peripheral opioid potencies by using synthetic dermorphin‐dynorphin hybrid peptides as the probe. Replacement of the enkephalin moiety of dynorphin with the dermorphin or dermorphin1–5 sequence caused a remarkable increase in analgesic potency, and a 3‐6 fold increase in potency of binding against [3H]‐dihydromorphine. The potency of receptor binding against [3H]‐EKC was also increased by incorporation of the whole dermorphin sequence into the dynorphin molecule. In the presence of NaCl (100mM), the effect of enhancing binding against [3H]‐EKC due to dermorphin substitution disappeared, suggesting the contribution of opioid μreceptor. Peripheral opioid activities assayed by various smooth muscle preparations showed that dermorphin incorporation caused a decrease in the potency of inhibition of the contractions of the guinea pig ileum and the rabbit vas deferens, no change in potency on the mouse vas deferens, and a marked increase in the inhibition of the rat vas deferens. Among the peripheral opioid activities only that assayed with the rat vas deferens appears to correlate approximately with the analgesic and the receptor binding activities. Judging from the relative potencies obtained from all assays, it is evident that the N‐terminal dermorphin moiety, but not the C‐terminal dynorphin fragment, dominates the opioid activity and receptor preference of the hybrid peptide.

原文英語
頁(從 - 到)99-104
頁數6
期刊International Journal of Peptide and Protein Research
35
發行號2
DOIs
出版狀態已發佈 - 2月 1990
對外發佈

ASJC Scopus subject areas

  • 生物化學

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