Antagonism of bremazocine-induced urination as a test for kappa-opioid receptor antagonists within the phenylpiperidine series
✍ Scribed by Leander J. David; Dennis M. Zimmerman
- Publisher
- John Wiley and Sons
- Year
- 1984
- Tongue
- English
- Weight
- 415 KB
- Volume
- 4
- Category
- Article
- ISSN
- 0272-4391
No coin nor oath required. For personal study only.
✦ Synopsis
Antagonism of bremazocine-induced urination as a test for kappa-opioid receptor antagonists within the phenylpiperidine series. Drug Dev. Res. 4:421-427, 1984. Representative compounds from a series of phenylpiperidine-opioid antagonists were compared in their ability to antagonize the diuretic effect of 0.08 mglkg of bremazocine, a kappa-opioid receptor agonist. Three of the compounds produced dose-related antagonism of bremazocine, whereas four others did nor. The four ineffective compounds also did not exhibit any kappa agonist activity. The potency of the three effective antagonists did not correlate with their antagonist activity against morphine or in suppressing deprivation-induced drinking. These results demonstrate that several kappa receptor antagonists can be found in the phenylpiperidine series of opioid antagonists, and further emphasize the usefulness of kappa-mediated diuresis as an in vivo test for kappa-opioid receptor activity.