Oxymorphazone: A long-acting opiate analgesic

  title={Oxymorphazone: A long-acting opiate analgesic},
  author={Geoffrey S. F. Ling and Steven L. Galetta and Gavril W. Pasternak},
  journal={Cellular and Molecular Neurobiology},
Summary1.Treating rat brain homogenatesin vitro with oxymorphazone, the hydrazone derivative of oxymorphone, selectively inhibited in a long-acting manner the highaffinity (mu1) binding of a number of3H-opioids. This inhibition was not affected by extensive wash procedures which did effectively reverse classical opiates such as morphine and naloxone.2.A similar, persistent inhibition of binding was observed followingin vivo administration of the drug. Both systemically and… Expand
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Effects of opioid analgesics on the action of general anaesthetics
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Opiate, enkephalin, and endorphin analgesia
These studies suggest that both opiate and opioid peptide analgesia is mediated through a single receptor subpopulation distinct from those involved with respiratory depression, and raise the possibility of specific opiate analgesics without respiratory depression. Expand
Naloxazone, a long-acting opiate antagonist: effects on analgesia in intact animals and on opiate receptor binding in vitro.
The analgetic, but not lethal, effects of morphine may be mediated by the high affinity subpopulation of opiate receptors. Expand
Naloxazone, a novel opiate antagonist: Irreversible blockade of rat brain opiate receptorsin vitro
Summary1.Naloxazone, a hydrazone derivative of naloxone which blocks mouse brain opiate receptorsin vivo for over 24 hr, produced a prolonged blockade of opiate receptor binding to rat brainExpand
The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
It has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists. Expand
The actions of naloxazone on the binding and analgesic properties of morphiceptin (NH2Tyr-Pro-Phe-Pro-CONH2), a selective mu-receptor ligand.
Naloxazone, which blocks irreversibly and selectively high affinity opiate and enkephalin binding, abolishes morphiceptin's inhibition of binding at low concentrations, suggesting that the high affinity binding of enkephalins and opiates represents a mu or morphine-type receptor. Expand
Opiates and enkephalins: a common binding site mediates their analgesic actions in rats.
Results imply that all 3H-ligands examined bind with highest affinity to a mu- like receptor while low affinity D-ala2-met5-enkephalinamide binding, with a KD of 6 nM, represents a delta-like receptor. Expand
Classification of multiple morphine and enkephalin binding sites in the central nervous system.
  • B. Wolozin, G. Pasternak
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1981
Findings suggest a common site that binds both opiates and enkephalins equally well and with highest affinity (Kd values, less than 1 nM), which appears to be the site responsible for analgesia under normal circumstances. Expand
Ontogeny of opioid pharmacology and receptors: high and low affinity site differences.
The small effect of spinal transections on morphine analgesia in 14-day old rats suggests that the change in analgesic sensitivity is at a segmental spinal level and not a result of descending pathways, and suggests an interesting correlation between high affinity binding and analgesia and between low affinitybinding and respiratory effects. Expand
Irreversible opiate agonists and antagonists: the 14- hydroxydihydromorphinone azines
Investigation into the molecular actions of the 14- hydroxydihydromorphinone hydrazones has suggested that their irreversible actions can be explained by the formation of their azines, which irreversibly block opiate binding in vitro 20- to 40-fold more potently than their corresponding hydrozones. Expand
Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors.
Naloxazone treatment blocks the analgesic effects of morphine for at least 24 hours but does not prevent death from high doses of morphine, suggesting analgesic but nonlethal opiate effects may be mediated by the high-affinity subpopulation of opiate receptors. Expand