[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.
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