title: Distinctions between dopamine transporter antagonists could be just around the bend.
abstract: 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.
authors.affiliation: Department of Pharmacology, Physiology, and Therapeutics, University of North Dakota School of Medicine and Health Sciences, Grand Forks, ND 58203, USA. khenry@medicine.nodak.edu
authors.forename: L Keith
authors.initials: LK
authors.lastname: Henry
authors.forename: Randy D
authors.initials: RD
authors.lastname: Blakely
mesh_terms: D000818:Animals; D001590:Benztropine / Q000494:pharmacology; D002227:Carbazoles / Q000494:pharmacology; D003042:Cocaine / Q000494:pharmacology; D004193:Discrimination Learning / Q000187:drug effects; D050483:Dopamine Plasma Membrane Transport Proteins / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*; D018765:Dopamine Uptake Inhibitors / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D020128:Inhibitory Concentration 50; D051379:Mice; D008958:Models, Molecular; D009043:Motor Activity / Q000187:drug effects; D011487:Protein Conformation / Q000187:drug effects; D017433:Protein Structure, Secondary; D051381:Rats
chemical_list: D002227:Carbazoles; D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors; D001590:Benztropine; C034931:rimcazole; D003042:Cocaine