[3H]beta-CIT: a radioligand for dopamine transporters in rat brain tissue.
[3H]2-beta-carbomethoxy-3-beta-[4'-iodophenyl]tropane (beta-CIT) was prepared and evaluated. With rat forebrain tissue, [3H]beta-CIT showed high affinity for dopamine transporters (DAT), with selectivity for DAT over norepinephrine transporters, but not serotonin transporters, as well as DAT-stereoselectivity with beta-CIT, amphetamine and methylphenidate. Affinity and selectivity for 53 compounds assayed with [3H]beta-CIT and standard DAT radioligand [3H]GBR-12935 were highly correlated (r0.95). [3H]beta-CIT is proposed as a useful, high-affinity DAT radioprobe.
Kula
N S
NS
Mailman and Addiction Research Centers, McLean Division of Massachusetts General Hospital, Belmont, MA 02478, USA.
Baldessarini
R J
RJ
Tarazi
F I
FI
Fisser
R
R
Wang
S
S
Trometer
J
J
Neumeyer
J L
JL
D000661:Amphetamine / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D002352:Carrier Proteins / Q000378:metabolism; D003042:Cocaine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism; D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors / Q000494:pharmacology; D008297:Male; D008562:Membrane Glycoproteins / Q000378:metabolism; D026901:Membrane Transport Proteins; D008774:Methylphenidate / Q000737:chemistry / Q000378:metabolism; D009419:Nerve Tissue Proteins; D010879:Piperazines / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology; D013237:Stereoisomerism; D014316:Tritium
D000661:Amphetamine; D002352:Carrier Proteins; D003042:Cocaine; D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D008774:Methylphenidate; D009419:Nerve Tissue Proteins; D010879:Piperazines; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; D014316:Tritium; C493216:Slc6a3 protein, rat; C493232:Slc6a4 protein, rat; C069723:2beta-carbomethoxy-3beta-(4-iodophenyl)tropane; C043425:vanoxerine; C044630:1-(2 (diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine