Fixed-proportion mixtures with the α2-adrenergic agonist clonidine or lofexidine do not alter fentanyl self-administration in non-opioid-dependent male and female rats

与α2-肾上腺素能激动剂可乐定或洛非西定按固定比例混合,不会改变非阿片类药物依赖的雄性和雌性大鼠的芬太尼自我给药行为。

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Abstract

Illicitly manufactured fentanyl has increasingly been adulterated with other chemical substances such as α2-adrenergic agonists. Although xylazine was the initial α-2 agonist reported to be in the illicit fentanyl supply, other α-2 agonists are increasingly being identified, suggesting that xylazine adulteration of illicit fentanyl is intentional to augment fentanyl effects. The aim of the present study was to determine the interactions between 2 clinically available α-2 agonists, clonidine and lofexidine, and fentanyl on reinforcement endpoints in male and female rats. Three drug self-administration experiments were conducted. First, clonidine and lofexidine self-administration dose-effect functions were determined under a fixed-ratio 5 schedule to assess whether clonidine or lofexidine functioned as reinforcers in rats. Second, behavioral economic demand functions were determined for fentanyl alone, α-2 agonists alone, or several fixed-proportion fentanyl/α-2 agonist mixtures. Lastly, fentanyl/α-2 agonist interactions were determined under a concurrent schedule of fixed-proportion fentanyl/α-2 agonist mixture and food availability. Neither clonidine nor lofexidine functioned as reinforcers under the fixed-ratio 5 schedule, even at the largest doses examined, which produced behavioral sedation. The present results demonstrate that clonidine and other α-2 agonists do not function as reinforcers under limited-access conditions in nonopioid-dependent rats. Furthermore, fentanyl self-administration was not significantly altered by increasing fixed-proportion mixtures of clonidine or lofexidine under either behavioral economic demand or fentanyl versus food choice procedures. Overall, these results demonstrate that α-2 agonists do not modulate fentanyl reinforcement in nonopioid-dependent rats and suggest that other potential reasons need to be explored for α-2 agonist adulteration of illicitly manufactured fentanyl. SIGNIFICANCE STATEMENT: Illicitly manufactured fentanyl continues to be adulterated with α-2 agonists. The present results demonstrate that clonidine and lofexidine neither enhance nor attenuate fentanyl self-administration under either behavioral economic demand or drug-choice procedures. These results suggest other factors than reinforcement modulation should be examined regarding the premise for α-2 agonist adulteration of illicitly manufactured fentanyl.

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