N-oleoyl-dopamine (OLDA) belongs to a novel class of lipophilic dopamine (DA) derivatives, identified in the brain. OLDA is an agonist of the vanilloid VR1 receptor but physiological consequences of its interaction with this and other receptor sysytems are unclear. In this study we posed a question of whether OLDA could display DA-like effects on locomotor performance. We addressed the issue by examining locomotor activity, expressed as a distance traveled by a freely moving rat in a 2 h test, before and after i.p. injection of 10 and 20 mg/kg OLDA. In additional experimental groups pretreatment with Haloperidol (0.1 and 0.2 mg/kg), a D2 receptor antagonist, was used as a means of assessing the involvement of the DA system in OLDA action. We found that locomotor activity increased promptly after OLDA injection. It peaked at 15 min, starting waning toward the baseline level afterward. Overall, the mean distance traveled by the rats in the 2 h test period increased, from 403 ±89 (SE) cm in the vehicle-treated to 1213 ±196 cm in the OLDA-treated rats (P<0.05). The increase in locomotor activity was reduced dose-dependently by Haloperidol. In separate in vitro assays, we confirmed the undivided integrity of the OLDA compound over the 2 h test time. We conclude that OLDA enhanced locomotor performance due to interaction with the DA neurotransmission.