Reinforcing and discriminative stimulus properties of mixed agonist-antagonist opioids.
@article{Young1984ReinforcingAD, title={Reinforcing and discriminative stimulus properties of mixed agonist-antagonist opioids.}, author={Alice M. Young and Kenneth R. Stephens and David W. Hein and James H. Woods}, journal={The Journal of pharmacology and experimental therapeutics}, year={1984}, volume={229 1}, pages={ 118-26 } }
Nine mixed agonist-antagonist opioids were evaluated in macaque monkeys for their ability to serve as positive reinforcers and for their discriminative stimulus similarity to etorphine and ethylketazocine. For tests of reinforcing properties, various doses of each drug were substituted for codeine under a fixed-ratio 30 time-out 600 sec schedule of i.v. delivery. Discriminative properties were assessed in separate groups of monkeys for which etorphine and saline, or ethylketazocine and saline…
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It is indicated that dezocine shares similar stimulus effects with both mu and delta agonists, its stimulus effects are reversed by mu-selective antagonists, and its rate-decreasing effects are not mediated by activity at mu, kappa or delta opioid receptors.
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The antagonism of the stimulus and rate-altering effects of EKC was surmountable, with considerable intersubject variability in the magnitude of the EKC dose increase required to overcome the blockade.
Discriminative Stimulus Effects of the Mixed-Opioid Agonist / Antagonist Dezocine : Cross-Substitution by Mu and Delta Opioid Agonists 1
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The present findings indicate that dezocine shares similar stimulus effects with both mu and delta agonists, its stimulus effects are reversed by mu-selective antagonists, and its rate-decreasing effects are not mediated by activity at mu, kappa or delta opioid receptors.
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The results indicate that the discriminative effects of spiradoline are mediated by kappa-opioid receptors; meaningful mu-opIOid and PCP/sigma components of action were not in evidence.
Substitution and primary dependence studies in animals.
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- 2004
The results demonstrate that the discriminative stimulus effects of mu agonists in rats are more readily attenuated by drugs that block D2-like, rather than D1- like, receptors.
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The present high dose-low dose-saline discrimination procedure appears useful for assessing partial agonist activity and is consistent with partial agonists activity for pentazocine, butorphanol, nalbuphine, and buprenorphine.
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Discriminative stimulus effects of buprenorphine in the rat
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The results of this study are consistent with those of other studies showing that the discriminative effects of buprenorphine are morphine-like and mediated by the mu-opioid receptor, and extend the conditions under which this has been demonstrated to stimulus control maintained by bupenorphine itself.