Evidence that dynorphin-(1–13) acts as an agonist on opioid κ-receptors

@article{Oka1982EvidenceTD,
  title={Evidence that dynorphin-(1–13) acts as an agonist on opioid $\kappa$-receptors},
  author={Tetsuo Oka and Kazuko Negishi and Mitsuaki Suda and Aiko Sawa and Masahiko Fujino and Mitsuhiro Wakimasu},
  journal={European Journal of Pharmacology},
  year={1982},
  volume={77},
  pages={137-141}
}
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 κ-receptor agonist, in inhibiting the electrically evoked contractions of the guinea-pig ileum was found to be similar to that found with either mouse vas deferens or rabbit ileum. Moreover, Mr 2266 was found to be several-fold more effective than naloxone to antagonize the… Expand
The choice of opioid receptor subtype in isolated preparations by dynorphins.
TLDR
The effectiveness of naloxone and Mr 2266 to antagonize the agonist action of dynorphin-(1-8) indicated that dynorphins acted as a kappa-receptor agonist in either guinea-pig ileum or rabbit ileUM whether or not peptidase inhibitors were existed. Expand
Potency of three opiate antagonists to reverse the inhibitory activity of dynorphin, enkephalins and opioid-like alkaloids on the guinea pig ileum.
TLDR
The fact that the 3 opiate antagonists evidenced similar Ke values for dynorphin and ethylketocyclazocine, but different ones for the enkephalins or normorphine supports the conclusion that Dynorphin activates preferentially K- but not mu-opiate receptors in the myenteric plexus. Expand
Evidence that endogenous 6-(Arg or Lys)-opioid peptides can interact with κ-receptors as agonists
Abstract Evidence is provided for the abilities of endogenous 6-(Arg or Lys)-opioid peptides to interact with κ-receptors as agonists. Dynorphin-(1–17) and -(1–8), α- and β-neo-endorphin, [Met 5Expand
A novel opioid peptide, leumorphin, acts as an agonist at the κ opiate receptor
Abstract The primary structure of the common precursor of porcine β-neo-endorphin and dynorphin (preproenkephalin B) has shown the existence of a third leucine-enkephalin (leu-enkephalin) sequenceExpand
The choice of opiate receptor subtype by neo-endorphins.
TLDR
The data indicate that neo-endorphins act as kappa-receptor agonists in either the guinea-pig and rabbit ileum or in the rabbit vas deferens while in the mouse vasdeferens they act on opiate receptor subtypes other than kappa - and mu-receptors. Expand
Tripeptides acting on opioid receptors in rat colon.
The tripeptides SD-34 and SD-25 induced atropine-, guanethidine-, antihistaminics-resistant but naloxone-sensitive contractions of isolated rat distal colon. They appeared to act on an opioidExpand
Dynorphin1–8 and dynorphin1–9 are ligands for the κ-subtype of opiate    receptor
It is generally accepted that there are three subtypes of opiate receptor: µ, δ and κ. The main endogenous ligands for the µ-and δ-sites are Met5-enkephalin, Leu5-enkephalin and β-endorphin, whereasExpand
Presynaptic inhibitory opioid δ- and κ-receptors in a branch of the rabbit ileocolic artery
Abstract The largest rami caecales of the ileocolic artery (a branch of the mesenteric artery) were perfused at a constant rate of flow. Either vasoconstriction or the release of previouslyExpand
Selective inactivation of opioid receptors in rat hippocampus demonstrates that dynorphin-A and -B may act on μ-receptors in the CA1 region
TLDR
The data suggest that both mu- and delta-receptors are functionally represented and provide evidence that the dynorphins or their derivatives may also be agonists at the mu-receptor. Expand
Human pharmacology of the opioid neuropeptide dynorphin A(1-13).
TLDR
The human pharmacology of dynorphin A(1-13) is evaluated and whether this peptide can modulate naloxone-precipitated withdrawal effects and the data contrast with those of previous preclinical studies showing dependence-attenuating effects of Dynorphin and fail to support its use as an antiwithdrawal agent in humans. Expand
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It is reported that the guinea pig ileum myenteric plexus contains two physically distinct classes of opiate receptors: the μ receptor, with which leu-enkephalin (or normorphine) interacts, and a separate dynorphin receptor. Expand
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The remarkable enhancement of the potency of [Leu]enkephalin by the COOH-terminal extension -Arg-Arg-Ile- Arg-Pro-Lys-Leu- lys-OH suggests new interpretations concerning the structure of opiate receptors and the function of the enkephin pentapeptides. Expand
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The results indicate that the rabbit ileum contains the new type of opiate receptor, which is not sensitive to morphine but is sensitive to enkephalins, and provides evidence that the enkphalins may function as neurotransmitters in the intestine. Expand
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