Abuse liabilityDrug discrimination studies☆
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Cited by (61)
Effects of the cannabinoid CB<inf>1</inf>-receptor neutral antagonist AM4113 and antagonist/inverse agonist rimonabant on fentanyl discrimination in male rats
2022, Drug and Alcohol DependenceCitation Excerpt :The present studies evaluated how blockade of CB1 receptors with the neutral antagonist AM4113 or antagonist/inverse agonist rimonabant modified fentanyl discrimination in male rats. Consistent with previous opioid discrimination studies, the µ-opioid receptor agonists fentanyl, oxycodone, and morphine fully substituted for 0.032 mg/kg fentanyl and pretreatment with the µ-opioid receptor antagonist naltrexone blocked fentanyl discrimination (Colpaert et al., 1976; Holtzman, 1985; Shannon and Holtzman, 1976; Walker et al., 1994). Like naltrexone, AM4113 was effective in blocking fentanyl discrimination without disrupting response rates.
In vitro and in vivo pharmacology of kratom
2022, Advances in PharmacologyCitation Excerpt :The reinforcing strength can be compared using an i.v. drug self-administration procedure using progressive-ratio schedules of drug reinforcement (Roberts & Bennett, 1993) and choice procedures (Townsend, Schwienteck, Robinson, Lawson, & Banks, 2021). Whereas drug discrimination assays are not directly employed to assess the abuse potential of test compounds, these assays have considerable pharmacological selectivity and can be used to identify the receptor mechanism of action of test compounds by comparing their effects to reference compounds (i.e., training drugs) that have a well-established receptor mechanism of action (e.g., Holtzman, 1985; Katz et al., 2017; Schuster & Johanson, 1988). An experimental animal is placed in an operant conditioning chamber typically with two levers on which the animal is conditioned to press for delivery of food or water.
Discriminative stimulus effects of carfentanil in rats discriminating fentanyl: Differential antagonism by naltrexone
2021, Drug and Alcohol DependenceCitation Excerpt :This study evaluated antagonism of the discriminative stimulus effects of carfentanil, fentanyl, and heroin by the opioid receptor antagonist naltrexone. Drug discrimination is a pharmacologically-selective procedure where behavior can be used as a readout of pharmacological activity (Glennon et al., 1983; Holtzman, 1985). Animals are trained to respond on one lever after receiving an injection of a specific dose of a drug and on another lever after receiving an injection of saline.
Distinct cognitive and discriminative stimulus effects of ketamine enantiomers in rats
2020, Pharmacology Biochemistry and BehaviorCitation Excerpt :However, all studies utilized phencyclidine (PCP), not ketamine as a training drug. In these studies, both (S)- and (R)- ketamine fully substituted for phencyclidine (PCP) (Brady and Balster, 1982; Zukin et al., 1984) as did the racemic mixture (Holtzman, 1985) indicating that the two isomers produce equivalent contributions to the discriminative stimulus effects of PCP. In both reports, (R)-ketamine was about 2× less potent than (S)-ketamine in producing discriminative stimulus effects comparable to PCP.
mGlu2/3 receptor antagonism: A mechanism to induce rapid antidepressant effects without ketamine-associated side-effects
2020, Pharmacology Biochemistry and BehaviorCitation Excerpt :When substituted for LY3020371, neither d-amphetamine (Fig. 12, middle panel) nor PCP (Fig. 12, right panel) produced significant LY3020371-like discriminative stimulus effects. Drug discrimination methods are used as one approach to predicting the subjective effects produced by drugs and by way of connection, their abuse liability (Holtzman, 1985). This is the only reported data in which an mGlu2/3 receptor antagonist was trained as a discriminative stimulus.
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Supported in part by USPHS Grant DA00541 and Research Scientist Development Award K02 DA00008, both from National Institute on Drug Abuse.