Corpus ID: 35819546

Evidence that dynorphin-(1-13) acts as an agonist on opioid kappa-receptors.

  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},
  volume={77 2-3},
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… Expand
Inactivation of dynorphin-(1-8) in isolated preparations by three peptidases.
The Ke values of three antagonists, naloxone, Mr 2266 and ICI 154129, against dynorphin-(1-8) in the presence of the three peptidase inhibitors indicated that dynorphins acted on kappa receptors in guinea-pig ileum and on both kappa and delta receptors in mouse vas deferens. Expand
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Two new opioid delta-receptor ligands, one being a highly selective agonist and the other being a potent selective antagonist in in vitro isolated preparations, were found in the present study. Expand
Generalization tests with intraventricularly applied pro-enkephalin B-derived peptides in rats trained to discriminate the opioid kappa receptor agonist ethylketocyclazocine
Studies into the receptor preference of this derivative, using the technique of “selective tolerance”, revealed that this dynorphin derivative is almost devoid of kappa-receptor activity. Expand
Opioid Receptor Effects Of Two Aminotetralin Derivatives In Guinea Pig Ileum Longitudinal Muscle And Mouse Vas Deferens Preparations
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A method to estimate the potency of the μ-component of an opioid having mixedμ-, andκ- and/orδ-agonist activities
The SC administration of either typicalμ-agonists such as morphine, pethidine, fentanyl and levorphanol or a mixedμ- andδ-agonist like [d-Ala2,d-Leu5]-enkephalin to 10-day-old rats produced loss ofExpand
Differential effects of SKF 10,047 (N-allyl-normetazocine) on peristalsis and longitudinal muscle contractions of the isolated guinea-pig ileum
It is concluded that μ- and ϰ-opioid receptors are of a greater functional significance than σ-receptors in the control of peristalsis. Expand
Possible regulatory role of dynorphin A in the urinary bladder
Dynorphin A immunoreactive material was found to be present in nerves in the rat detrusor and in prevesical ganglia, possibly via actions on K-opioid receptors and interaction with non-cholinergic nerves. Expand
Dynorphin–Still an Extraordinarily Potent Opioid Peptide
Evidence that members of this family of opioid peptides are endogenous agonists for the kappa opioid receptor is focused on and contributions to the discovery of the dynorphins are focused on. Expand