SRI-32743 is a novel allosteric modulator of dopamine transporter (DAT), attenuates HIV-1 Tat protein-induced inhibition of the dopamine transporter.
SRI-32743 shares the binding residues inside the pocket of DAT with Tat binding.
SRI-32743 (50 nM) attenuated Tat-induced inhibition of [3H]DA uptake and decreased the cocaine-mediated dissociation of [3H]WIN35,428 binding in CHO cells expressing hDAT.
SRI-32743 ameliorates Tat-induced cognitive deficits and potentiation of cocaine reward.
SRI-32743 reverses HIV-1 Tat-induced increase in dopamine release in the caudate putamen of inducible Tat transgenic mice.
