Evidence that dynorphin-(1–13) acts as an agonist on opioid κ-receptors
European Journal of PharmacologyPublished 1 January 1982
Tetsuo Oka, Kazuko Negishi, Mitsuaki Suda, Aiko Sawa, Masahiko Fujino, Mitsuhiro Wakimasu
Citations134
SJR quartileQ1
SJR score1.20
SNIP0.98
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TL;DR
The data indicate that dynorphin-(1-13) acts as an endogenous agonist on kappa-receptors, and Mr 2266 was found to be several-fold more effective than naloxone to antagonize the agonist actions of both kappa.
Abstract
The study concerned the opioid-receptor subtype on which dynorphin-(1-13) acts in in vitro isolated preparations. The potency of dynorphin-(1-13) relative to that of ethylketocyclazocine (Mr 2266), a representative kappa-receptor agonist, in inhibiting the electrically evoked contractions of the guinea-pig ileum was found to be similar to that found with either mouse was deferens or rabbit ileum. Moreover, Mr 2266 was found to be several-fold more effective than naloxone to antagonize the agonist actions of both kappa-receptor agonists such as ethylketocyclazocine, ketocyclazocine and bremazocine, and dynorphin-(1-13) either in the guinea-pig ileum, mouse vas deferens, or in rabbit ileum. Additionally, dynorphin-(1-13) was found to have a significant inhibitory action on the rabbit vas deferens which had been shown to contain kappa-receptors exclusively. The data indicate that dynorphin-(1-13) acts as an endogenous agonist on kappa-receptors.
Keywords
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