TABLE 6.

A summary of the evidence for allosteric modulation of DAT by SoRI compounds Cocaine competitively inhibits [³H]DA uptake (Zhu and Hexum, 1992) and DAT binding (Reith et al., 1992; Pariser et al., 2008).

Drug	[3H]DA Uptake	DAT Binding ([125I]RTI-55)	Effect on [125I]RTI-55 Dissociation from DAT	Effect on d-Amph-Induced DAT-Mediated Efflux of [3H]MPP+	Effect on d-Amph-Induced DAT-Mediated DA Release
Cocaine	“Normal” competitive inhibitor	Normal competitive inhibitor	No effecta	Slows d-Amph-induced efflux by changing apparent rate constants	Competitive inhibitor
SoRI-9804	Partial inhibitor decreases Vmaxa	Partial inhibitor decreases Bmaxa	Slowed dissociation ratea	Slows d-Amph-induced efflux without changing apparent rate constants	Partial inhibitor “agonist-like”
SoRI-20040	Partial inhibitor decreases Vmax	Partial inhibitor decreases Bmax	Slowed dissociation rate	Not determined; direct effects at high concentrations	Partial inhibitor agonist-like
SoRI-20041	Partial inhibitor decreases Vmax	Partial inhibitor decreases Bmax	Slowed dissociation rate	Not determined; direct effects at high concentrations	No effect “antagonist-like”
SoRI-2827	Partial inhibitor decreases Vmax, but less so than SoRI-20040 and SoRI-20041	Partial inhibitor decreases Bmax	No effect on dissociation rate	Not studied; nonspecific effects	Not studied; nonspecific effects

^aUnpublished data