Dynorphin(1-10)amide: A potent and selective analog of dynorphin(1-13)

Sidney Woo, Javier Garzon, Pilar Sanchez-Blazquez, F. Cankat Tulunay, Jaw Kang Chang, Horace H. Loh

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Dynorphin(1-10)amide was more potent than Dynorphin(1-13) in inhibiting the twitch of the mouse vas deferens (IC50) of Dynorphin(1-10)amide = 0.3 nM and IC50 of Dynorphin (1-13) = 4.0 nM. Binding assaays indicated that two opioid peptides had similar profiles in that they enhanced dihydromorphine (DHM) binding in picomolar concentrations but displaced DHM binding in nanomolar concentrations (IC50 for Dynorphin(1-10)amide = 5 nM). In the mouse tail-flick assay, however, Dynorphin(1-10)-amide showed a more selective action on morphine-induced analgesia. Although Dynorphin(1-10)amide had no significant analgesic activity by itself, it differed from the (1-13) analog by neither potentiating nor antagonizing morphine in naive animals. In tolerant animals, on the other hand, 50 ug of this analog administered icv shifted the ED50 of morphine from 43.0(33.0-55.9) to 17.0 (12.4-23.3). Thus, Dynorphin(1-10)amide appears to be a more potent and selective analog of Dynorphin(1-13).

Original languageEnglish (US)
Pages (from-to)1817-1820
Number of pages4
JournalLife Sciences
Volume31
Issue number16-17
DOIs
StatePublished - 1982

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