Distinctions between dopamine transporter antagonists could be just around the bend.

Henry LK, Blakely RD
Mol Pharmacol. 2008 73 (3): 616-8

PMID: 18156312 · DOI:10.1124/mol.107.044586

Abuse of psychostimulants such as cocaine and amphetamines has a tremendous social and economic impact. Although replacement therapies are offered for addiction to opioids, nicotine, and alcohol, there is no approved replacement treatment for psychostimulant addiction. Recent studies on an emerging group of benztropine- and rimcazole-based compounds provide hope that replacement therapies for cocaine and amphetamine addiction may come in the near future. A new study (p. 813) now investigates the molecular interaction of the benztropine and rimcazole compounds with their target, the dopamine transporter, and provides an intriguing explanation as to why use of these compounds, unlike cocaine, do not lead to locomotor stimulation and drug discrimination behaviors in animal models.

MeSH Terms (15)

Animals Benztropine Carbazoles Cocaine Discrimination Learning Dopamine Plasma Membrane Transport Proteins Dopamine Uptake Inhibitors Dose-Response Relationship, Drug Inhibitory Concentration 50 Mice Models, Molecular Motor Activity Protein Conformation Protein Structure, Secondary Rats

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