Opioid agonist properties of two oxime derivatives of naltrexone, NPC 831 and NPC 836

  title={Opioid agonist properties of two oxime derivatives of naltrexone, NPC 831 and NPC 836},
  author={Diane L. DeHaven-Hudkins and Kathy Komer and Joshua Allen Peterson and Babu J. Mavunkel and Waclaw J. Rzeszotarski},
  journal={Pharmacology Biochemistry and Behavior},
4 Citations
Nuclear Magnetic Resonance Chemical Shift Values of Glyoxime Molecule with Experimental and Theoretical Methods
In this study, the conformational analysis was performed by the semi-empirical PM3 method to determine the molecular structure of the glyoxime molecule. Each of conformer was optimized using the


U-54494A: a unique anticonvulsant related to kappa opioid agonists.
Results suggest that U-54494A is a unique and selective anticonvulsant agent acting by a Ca++-related mechanism possibly through a subclass of kappa receptors.
A series of novel, highly potent and selective agonists for the κ‐opioid receptor
It is concluded that the seven novel compounds described are all potent and selective agonists for the κ‐opioid receptor.
Pharmacological profile of PD 117302, a selective κ‐opioid agonist
The pharmacological profile of PD 117 302 in vivo is consistent with in vitro data suggesting that PD 117302 is a selective agonist at the κ‐opioid receptor.
Supraspinal and spinal potency of selective opioid agonists in the mouse writhing test.
Although the proposed kappa-acting compounds KC and U50 were effective at relatively low doses at spinal levels, these compounds lacked activity at supraspinal sites at doses not causing sedation.
Use of beta-funaltrexamine to determine mu opioid receptor involvement in the analgesic activity of various opioid ligands.
Results seem to indicate a major role for the mu receptor in the analgesic actions of these compounds, and suggest that beta-FNA is selective for mu over kappa receptors under the conditions used in this study.
Neuroprotective actions of GR89696, a highly potent and selective κ‐opioid receptor agonist
The results indicate that the potent κ‐opioid receptor agonist, GR89696, is neuroprotective in both global and focal cerebral ischaemia models and suggest that, with this class of compound, there may be a considerable time window for pharmacological intervention.
U-50,488: a selective and structurally novel non-Mu (kappa) opioid agonist.
It is suggested that different opioid receptors mediate the analgesic effects of morphine and U-50,488, a more selective kappa agonist that causes opioid receptor-mediated sedation, diuresis and corticosteroid elevations.
U50,488, a highly selective kappa opioid: anticonvulsant profile in rats.
Results indicate that U50,488 is an efficacious, long-acting anticonvulsant against supramaximal, but not chemical threshold, seizures in rats, and suggest that this effect is mediated by non-mu (probably kappa) binding sites.
Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine.
The selective long-lasting antagonism of mu-mediated effects by beta-FNA may be of great value in the elucidation of multiple opioid receptor function.