[H-3]beta-CIT: a radioligand for dopamine transporters in rat brain tissue

[H-3]2-beta-carbomethoxy-3-beta-[4'-iodophenyl]tropane (beta-CIT) was prepa red and evaluated. With rat forebrain tissue, [H-3]beta-CIT showed high aff inity for dopamine transporters (DAT), with selectivity for DAT over norepi nephrine transporters, but not serotonin transporters, as well as DAT-stere oselectivity with beta-CIT, amphetamine and methylphenidate. Affinity and s electivity for 53 compounds assayed with [H-3]beta-CIT and standard DAT rad ioligand [H-3]GBR-12935 were highly correlated (r > 0.95). [H-3]beta-CIT is proposed as a useful, high-affinity DAT radioprobe. (C) 1999 Elsevier Scie nce B.V. All rights reserved.