Hl. Kimmel et al., Dopamine transporter synthesis and degradation rate in rat striatum and nucleus accumbens using RTI-76, NEUROPHARM, 39(4), 2000, pp. 578-585
Intracerebroventricular injections of the irreversible dopamine transporter
(DAT) inhibitor, RTI-76 (3 beta-(3-p-chlorophenyl) tropan-2 beta-carboxyli
c acid p-isothiocyanatophenylethyl ester hydrochloride), decreased DAT bind
ing in both the striatum and nucleus accumbens as measured by both [H-3]GBR
12935 and by [H-3]WIN35,428. This decrease was dose-related, with 100 nmol
RTI-76 producing approximately a 50% decrease in both regions. The maximal
inhibition of DAT binding was observed 24 h after RTI-76 injection, and bin
ding was fully restored 7 days after injection. The DAT protein half-life d
etermined under these conditions was about 2 days. [H-3]Nisoxetine binding
at norepinephrine transporters in the cortex was not altered by RTI-76 admi
nistration at any time point or dose examined. (C) 2000 Elsevier Science Lt
d. All rights reserved.