Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 6, Pages 623-627Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500113s
Keywords
Dopamine uptake inhibitors; serotonin releasers; serotonin receptor; cocaine; methamphetamine
Categories
Funding
- National Institute on Drug Abuse [DA12970]
- National Institute on Drug Abuse, NIH
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As part of our program to study neurotransmitter releasers, we report herein a class of hybrid dopamine reuptake inhibitors that display serotonin releasing activity. Hybrid compounds are interesting since they increase the design. potential of transporter related compounds and hence represent a novel and unexplored strategy for therapeutic drug discovery. A series of N-alkylpropiophenones was synthesized and assessed for uptake inhibition and release activity using rat brain synaptosomes. Substitution on the aromatic ring yielded compounds that maintained hybrid activity, with the two disubstituted analogues (PAL-787 and PAL-820) having the most potent hybrid activity.
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