CTDP-32476 is a potent and selective dopamine transporter (DAT) inhibitor and a competitive inhibitor of cocaine binding to the DAT with Ki of 12 nM.
CTDP-32476 demonstrates 20-fold higher affinity for the DAT than cocaine.
CTDP-32476 is more potent than methylphenidate in blocking [3H]-cocaine binding.
Systemic administration of CTDP-32476 alone produced a slow-onset, long-lasting increase in extracellular nucleus accumbens DA, locomotion, and brain-stimulation reward, inhibited cocaine self-administration, cocaine-associated cue-induced relapse to drug seeking, and cocaine-enhanced extracellular DA in the nucleus accumbens.
