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, 234 (8), 1237-1245

Locomotor Activity and Discriminative Stimulus Effects of a Novel Series of Synthetic Cathinone Analogs in Mice and Rats

Affiliations

Locomotor Activity and Discriminative Stimulus Effects of a Novel Series of Synthetic Cathinone Analogs in Mice and Rats

Michael B Gatch et al. Psychopharmacology (Berl).

Abstract

Rationale: Recent years have seen an increase in the recreational use of novel, synthetic psychoactive substances. There are little or no data on the abuse liability of many of the newer compounds.

Objectives: The current study investigated the discriminative stimulus and locomotor effects of a series of synthetic analogs of cathinone: α-pyrrolidinopropiophenone (α-PPP), α-pyrrolidinohexiophenone (α-PHP), α-pyrrolidinopentiothiophenone (α-PVT), 3,4-methylenedioxybutiophenone (MDPBP), and ethylone.

Methods: Locomotor activity was assessed in an open-field assay using Swiss-Webster mice. Discriminative stimulus effects were assessed in Sprague-Dawley rats trained to discriminate either cocaine or methamphetamine from vehicle.

Results: Each of the compounds produced an inverted-U dose-effect on locomotor activity. Maximal effects were similar among the test compounds, but potencies varied with relative potencies of MDPBP > α-PPP = α-PHP > ethylone > α-PVT. Each of the test compounds substituted fully for the discriminative stimulus effects of methamphetamine. α-PPP, α-PHP, and ethylone fully substituted for cocaine. α-PVT produced a maximum of 50% cocaine-appropriate responding, and MDPBP produced an inverted-U-shaped dose-effect curve with maximum effects of 67%.

Conclusions: These data provide initial evidence that these structurally similar, emerging novel psychoactive substances demonstrate potential for abuse and may be utilized for their stimulant-like effects, given their ability to stimulate locomotor activity and their substitution for the discriminative stimulus effects of the classical psychostimulants cocaine and/or methamphetamine.

Keywords: Abuse; Cathinones; Drug discrimination; Locomotor activity; Mouse; Rat.

Figures

Figure 1
Figure 1
Structures of compounds tested
Figure 2
Figure 2. Time course of locomotor stimulant effects
Average horizontal activity counts/10min (ambulation counts) as a function of time and dose for α-PHP, α-PPP, α-PVT, MDPBP, and ethylone. Each panel shows the effects of one dose of compound versus the vehicle; n=8 for each dose. The gray bar shows the time range of peak effect. *indicates stimulant effects (p<0.05) against vehicle control at any time period.
Figure 3
Figure 3. Dose effect of locomotor activity
Average horizontal activity counts/10 min (±SE) during the 30 min of peak effect as a function of dose for each of the five cathinones. The top panel shows the effects of the three alpha compounds, α-PHP, α-PPP, and α-PVT. The bottom panel shows the effects of the compounds with a methylenedioxy ring, MDPBP and ethylone. n=8 for each dose. Ctrl indicates vehicle control. * indicates stimulant effects (p<0.05) against vehicle control.
Figure 4
Figure 4. Substitution for the discriminative stimulus effects of cocaine or methamphetamine
The top graph in each panel shows the percentage of total responses made on the drug-appropriate lever. The bottom graph shows the rate of responding in responses per second (r/s). Panel A shows the effects of the three alpha compounds, α-PHP, α-PPP and α-PVT in cocaine-trained rats. Panel B shows the effects of α-PHP, α-PPP and α-PVT in methamphetamine-trained rats. Panel C shows the effects of the compounds with a methylenedioxy ring, MDPBP and ethylone, in cocaine-trained rats. Panel D shows the effects of MDPBP and ethylone in methamphetamine-trained rats. n=6 for each compound. Ctrl indicates vehicle and training drug controls. * indicates rate effects (p<0.05) against vehicle control

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