Abstract
Because much evidence implicates the dopamine transporter in the reinforcing effects of cocaine, development of potential medications for cocaine dependence has included the dopamine transporter as a target. The present overview covers progress in the drug development area regarding several classes of dopamine uptake inhibitors, with an emphasis on structure-activity relationships that enhance potency and selectivity at transporters for dopamine compared with those for serotonin or norepinephrine. The following categories of compounds are covered: tropane, benztropine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR), methylphenidate, mazindol, and phencyclidine analogs. Activity at transporters as well as on behavior is highlighted.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
-
Review
MeSH terms
-
Animals
-
Cocaine-Related Disorders / drug therapy*
-
Cocaine-Related Disorders / metabolism
-
Dopamine Plasma Membrane Transport Proteins
-
Dopamine Uptake Inhibitors / administration & dosage*
-
Dopamine Uptake Inhibitors / chemistry
-
Dopamine Uptake Inhibitors / metabolism
-
Drug Delivery Systems / methods*
-
Humans
-
Membrane Glycoproteins*
-
Membrane Transport Modulators*
-
Membrane Transport Proteins / antagonists & inhibitors*
-
Membrane Transport Proteins / metabolism
-
Nerve Tissue Proteins / antagonists & inhibitors*
-
Nerve Tissue Proteins / metabolism
Substances
-
Dopamine Plasma Membrane Transport Proteins
-
Dopamine Uptake Inhibitors
-
Membrane Glycoproteins
-
Membrane Transport Modulators
-
Membrane Transport Proteins
-
Nerve Tissue Proteins