U-50,488, a selective kappa opioid agonist: Comparison to other reputed kappa agonists

  title={U-50,488, a selective kappa opioid agonist: Comparison to other reputed kappa agonists},
  author={Philip F. Von Voigtlander and Richard A. Lewis},
  journal={Progress in Neuro-Psychopharmacology and Biological Psychiatry},

Behavioral effects of a novel kappa opioid analgesic, U-50488, in rats and rhesus monkeys

Experimental results support the previous reports in mice that U-50488 is a very selective kappa opioid agonist in rats and rhesus monkeys.

Discriminative and analgesic effects of mu and kappa opioids: in vivo pA2 analysis.

Analysis by pA2 was used to quantify interactions between the opioid antagonist quadazocine and several opioid agonists, suggesting that the discriminative stimulus and analgesic effects of kappa opioids agonists are mediated at the same opioid receptor type, which is different from the type of opioid receptor at which mu agonists produce their discriminatives stimulus and painkilling effects.

Pharmacological analysis of the rate-decreasing effects of mu and kappa opioids in pigeons

These experiments indicate that the rate-decreasing effects of morphine andl-methadone are mediated by mu opioid receptors, whereas the rate ofdecrease effects of bremazocine, U69,593 and U50,488 in pigeons differ depending on the pharmacological procedures used to assess their effects.

Antinociceptive effects of the kappa opioid, U50,488: lack of modulation by 5-HT2 antagonists

Data do not support a role for the 5-HT2 system in kappa-induced antinociception in the primate and the kappa opioid, U50,488, alone or in combination with 5HT2 antagonists, ketanserin, pirenperone and LY 53857.

Biochemical and functional interactions of a selective kappa opioid agonist with calcium.

Together these data indicate that the kappa agonist U-50488H has functionally relevant interactions with depolarization-related Ca++ mechanisms in the central nervous system.



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.

Bremazocine: a potent, long-acting opiate kappa-agonist.

Endogenous opioid peptides: multiple agonists and receptors

It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor.

4-Amino-4-arylcyclohexanones and their derivatives, a novel class of analgesics. 1. Modification of the aryl ring.

Investigation of central nervous system activity of phenylcyclohexylamines was continued by preparation of "reversed" analogues and the most potent compounds in this series showed 50% the potency of morphine.

Antagonism by naloxone of narcotic-induced respiratory depression and analgesia.

Significant differences between apparent pA2 values for respiratory depression and analgesia suggest that these two effects of the narcotic drugs are mediated by different receptor interactions.