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Locomotor activity and discriminative stimulus effects of a novel series of synthetic cathinone analogs in mice and rats.
Psychopharmacology (Berl). 2017 04; 234(8):1237-1245.P

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.

Authors+Show Affiliations

Center for Neuroscience Discovery, University of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth, TX, 76107-2699, USA. michael.gatch@unthsc.edu.Center for Neuroscience Discovery, University of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth, TX, 76107-2699, USA.Center for Neuroscience Discovery, University of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth, TX, 76107-2699, USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28210779

Citation

Gatch, Michael B., et al. "Locomotor Activity and Discriminative Stimulus Effects of a Novel Series of Synthetic Cathinone Analogs in Mice and Rats." Psychopharmacology, vol. 234, no. 8, 2017, pp. 1237-1245.
Gatch MB, Dolan SB, Forster MJ. Locomotor activity and discriminative stimulus effects of a novel series of synthetic cathinone analogs in mice and rats. Psychopharmacology (Berl). 2017;234(8):1237-1245.
Gatch, M. B., Dolan, S. B., & Forster, M. J. (2017). Locomotor activity and discriminative stimulus effects of a novel series of synthetic cathinone analogs in mice and rats. Psychopharmacology, 234(8), 1237-1245. https://doi.org/10.1007/s00213-017-4562-4
Gatch MB, Dolan SB, Forster MJ. Locomotor Activity and Discriminative Stimulus Effects of a Novel Series of Synthetic Cathinone Analogs in Mice and Rats. Psychopharmacology (Berl). 2017;234(8):1237-1245. PubMed PMID: 28210779.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Locomotor activity and discriminative stimulus effects of a novel series of synthetic cathinone analogs in mice and rats. AU - Gatch,Michael B, AU - Dolan,Sean B, AU - Forster,Michael J, Y1 - 2017/02/16/ PY - 2016/11/16/received PY - 2017/02/02/accepted PY - 2017/2/18/pubmed PY - 2017/12/2/medline PY - 2017/2/18/entrez KW - Abuse KW - Cathinones KW - Drug discrimination KW - Locomotor activity KW - Mouse KW - Rat SP - 1237 EP - 1245 JF - Psychopharmacology JO - Psychopharmacology (Berl.) VL - 234 IS - 8 N2 - 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. SN - 1432-2072 UR - https://www.unboundmedicine.com/medline/citation/28210779/Locomotor_activity_and_discriminative_stimulus_effects_of_a_novel_series_of_synthetic_cathinone_analogs_in_mice_and_rats_ L2 - https://dx.doi.org/10.1007/s00213-017-4562-4 DB - PRIME DP - Unbound Medicine ER -