Endogenous opioid peptides: multiple agonists and receptors

@article{Lord1977EndogenousOP,
  title={Endogenous opioid peptides: multiple agonists and receptors},
  author={John A. H. Lord and Angela A. Waterfield and John Hughes and Hans W. Kosterlitz},
  journal={Nature},
  year={1977},
  volume={267},
  pages={495-499}
}
Opioid peptides were assayed by inhibition of 3H-naloxone and 3H-leu-enkephalin binding in brain homogenates and by depression of contractions of the guinea pig ileum and mouse vas deferens. We conclude that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor. 
EFFECTS OF OPIOID PEPTIDES AND KAPPA-RECEPTOR AGONISTS ON IN VITRO ISOLATED PREPARATIONS
Evidences that dynorphin-(1–13) acted as kappa-receptor agonist and that rabbit and dog ileum contained the new type of opiate receptor which was tentatively termed iota receptor, were obtained by
Opiate and opioid peptide binding in rat goldfish: further evidence for opiate receptor heterogeneity
TLDR
The binding of a series of 3H-labeled mu, kappa, sigma and delta opioid agonists and an antagonist has been examined in rat and goldfish brain membranes, showing dramatic differences both between the two species and between the different3H-ligands.
Opioid peptides and their receptors.
  • H. Kosterlitz
  • Chemistry, Medicine
    Progress in biochemical pharmacology
  • 1980
TLDR
An understanding of the pharmacokinetics of the opioid peptides will be of basic importance for the design of enkephalin analogues suitable for use as analgesics in man.
25. Functional identification of opioid receptors in vivo using β-FNA
Analgesia can be produced by activating both μ and κ opioid receptors (Tyers 1980). Receptor binding experiments indicate that many opioid drugs have comparable affinities for both μ and κ receptors,
OPIOID AGONISTS AND ANTAGONISTS: ACTION ON MULTIPLE OPIATE RECEPTORS
TLDR
Results from binding studies performed on rat vas deferens homogenates parallelled the data obtained from the isolated preparation and the high antagonistic activity of various narcotic antagonists was very similar on both preparations.
Multiple opioid ligands and receptors in the control of nociception.
TLDR
Evidence is given that antinociception induced by intracerebroventricular injection of opioids into mouse brain is mediated by receptors resembling those mediating the inhibitory action of these substances on the rat vas deferens (putative epsilon-receptors).
In vitro profile of some opioid pentapeptide analogues.
The opiate agonist potency of thirteen synthetic enkephalin pentapeptides has been examined on the electrically stimulated guinea pig ileum and mouse vas deferens preparations in comparison with
Interaction of naloxone with the opioid receptor complex in vitro
TLDR
The interaction of naloxone with the receptor complex is studied and the results further strengthens the hypothesis that leucine enkephalin binds poorly to the morphine receptor and that morphine and enkphalin receptors are allosterically coupled.
Cloning of a delta opioid receptor by functional expression.
TLDR
A complementary DNA clone encoding a functional delta opioid receptor has been identified and shows homology to G protein-coupled receptors, in particular the receptors for somatostatin, angiotensin, and interleukin-8.
Opioid peptides and their receptors
The endogenous opioid peptides belong to three groups: the endorphins, the enkephalins and the dynorphins. These three groups are clearly distinct chemical families derived from three different
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