RTI-13951-33 poorly inhibits SERT (IC50: 25.1 ± 2.7 μM). RTI-13951-33 elevates [35S]-GTPγS binding (EC50: 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice. RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; Ki, 2.29 μM), vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and moderate affinity at serotonin transporter (SERT; Ki, 0.75 μM) [1].

RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently reduces alcohol lever responses in a rat model of alcohol self-administration. RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t1/2 of 48 min and 87 min in rat plasma and brain [1].