An NTS1 agonist; selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively); inactive in an NTS1 calcium flux assay (EC50 = >80 μM); a positive allosteric modulator that increases binding of radiolabaled neurotensin to NTS1 in a concentration-dependent manner; reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice at 20 and 10-30 mg/kg, respectively; reduces methamphetamine self-administration in rats at 30 mg/kg,