ArticlesCathinone: An Investigation of Several N-Alkyl and Methylenedioxy-Substituted Analogs
Section snippets
Drug Discrimination Studies
Nine male Sprague–Dawley rats (ca. 250–300 g), housed individually, were reduced in body weight to approximately 80% of their free-feeding weight. During the entire course of the study, the animals’ body weights were maintained at this level by partial food deprivation; in their home cages, the animals were allowed drinking water ad lib. The animals were trained (15-min training session) to discriminate intraperitoneal injections (15-min presession injection interval) of 1.0 mg/kg of
Results
N-Monoethylcathinone (N-Et CAT; ED50 = 0.77 mg/kg), N-mono-n-propylcathinone (N-Pr CAT; ED50 = 2.03 mg/kg), racemic N,N-dimethylcathinone and its (−)-isomer [(±)Di Me CAT, ED50 = 0.61 mg/kg; (−)Di Me CAT, ED50 = 0.44 mg/kg], and (+)N,N-dimethylamphetamine [(+)Di Me AMPH; ED50 = 2.92 mg/kg] all resulted in stimulus generalization when administered to (+)amphetamine-trained animals (ED50 = 0.33 mg/kg) (Table 1). In some cases [N-Pr CAT, (+)Di Me AMPH)], the animals’ response rates were decreased
Discussion
As appears to be the case with amphetamine 9, 34, 36, 37, N-monomethylation of cathinone results (at least) in retention of potency [19], but any further increase in alkyl chain length results in a progressive decrease in potency (Table 1). The ED50 values for racemic cathinone, its N-methyl (i.e., methcathinone), N-ethyl (i.e., N-Et CAT), and N-n-propyl (i.e., N-Pr CAT) derivatives are 0.71, 0.37, 0.77, and 2.03 mg/kg) (see Table 3). These results, then, are not unexpected and represent
Acknowledgements
This work was supported, in part, by NIH Grant DA-01642. We would like to thank Dr. M. Gabryszuk for his assistance with some of the stimulus generalization studies.
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