Table 1.

Preference of the DAT conformation, effects on locomotor activity and substitution for cocaine under cocaine discrimination or self-administration procedures.

Compound [reference]	DAT conformation (μM)	Locomotor activity (μmol/kg, I.P.)	Substitution for cocaine in cocaine discrimination (μmol/kg, I.P.)	Substitution for cocaine in cocaine self-administration (mg/kg/injection, I.V.)
Cocaine [3,5]	Outward-facing (100)	Increased (30–100) Increased (20 or 40 mg/kg, I.P.)	Substituted (30)	Substituted (0.1 and 0.32)
JHW 007 [2,3]	Inward-facing (1)	Inactive (0.3–3.0 mg/kg, I.P.)	Not substituted (0.17–5.6 mg/kg, I.P.)	Not substituted (0.032–1.0)
RTI-336 [3]	Outward-facing (1)	Increased (10–56 mg/kg, I.P.)	Substituted (56 mg/kg, I.P.)	Substituted (0.1 and 0.32)
RTI-337 [3]	Outward-facing (1)	Increased (100 mg/kg, I.P.)	Partially substituted (10–100 mg/kg, I.P.)	Not substituted (0.1–3.2)
LX-10 [5]	Outward-facing (10)	Increased (3 and 10)	Substituted (10)	N.T.
LX-11 [5]	Outward-facing (20)	Inactive (3–56)	Not substituted (17)	N.T.
LX-12 [5]	Outward-facing (20)	Inactive (3–300)	Not substituted (0.3–10)	N.T.
LX-13 [5]	Outward-facing (10)	Increased (10 and 30)	Not substituted (3–17)	N.T.
LX-15 [5]	No change (20)	Inactive (3–100)	Not substituted (0.3–10)	N.T.
LX-16 [5]	Outward-facing (10)	Increased (3–100)	Partially substituted (0.3–3)	N.T.
LX-19 [5]	Outward-facing (10)	Increased (30–100)	Partially substituted (0.3–10)	N.T.
LX-20 [5]	No change (20)	Inactive (30)	Not substituted (0.3–3)	N.T.
LX-21 [5]	Outward-facing (10)	Inactive (0.56–170)	Not substituted (0.3–3)	N.T.
LX-22 [5]	Outward-facing (20)	Inactive (0.56–300)	Not substituted (0.3–10)	N.T.
LX-23 [5]	Outward-facing (10)	Inactive (0.56–56)	Not substituted (0.3–5.6)	N.T.
LX-24 [5]	Outward-facing (20)	Inactive (1.7–56)	Not substituted (0.3–5.6)	N.T.

NT: Not Tested