Cocaine and several sigma receptor ligands inhibit dopamine uptake in rat caudate-putamen.
Cocaine and several sigma receptor ligands inhibit dopamine uptake via a common site. This is evidenced by a concentration-dependent inhibition of dopamine uptake and displacement of the binding of [3H]WIN 35,428 (also called CFT), a cocaine analog with high affinity for the dopamine transporter. Since several sigma receptor ligands have been shown to block the stimulant effects of cocaine, this site may serve as a target for future drug development to treat cocaine abuse.
Izenwasser
S
S
Psychobiology Section, NIDA Addiction Research Center, Baltimore, MD 21224.
Newman
A H
AH
Katz
J L
JL
D000345:Affinity Labels; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002352:Carrier Proteins / Q000378:metabolism; D002421:Caudate Nucleus / Q000187:drug effects / Q000378:metabolism*; D003042:Cocaine / Q000031:analogs & derivatives / Q000494:pharmacology*; D004298:Dopamine / Q000378:metabolism*; D050483:Dopamine Plasma Membrane Transport Proteins; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins / Q000378:metabolism; D011699:Putamen / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism; D017480:Receptors, sigma / Q000187:drug effects*
D000345:Affinity Labels; D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D011954:Receptors, Dopamine; D017480:Receptors, sigma; C021279:(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester; D003042:Cocaine; D004298:Dopamine