We examined the effects of a potent glutamate transporter inhibitor, (2S,3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate (TFB-TBOA), on the expression of methamphetamine-induced behavioral sensitization in rats. Rats were intraperitoneally treated with 2 mg/kg methamphetamine for 5 days and then challenged with 1 mg/kg methamphetamine. Intracerebroventricular administration of TFB-TBOA (0.1 nmol) 10 min before the challenge significantly facilitated the expression of behavioral sensitization. On the other hand, it had no effect on the locomotor activation elicited by the challenge with methamphetamine in repeated-saline-treated (non-sensitized) rats. These results suggest that central glutamate transporters may play an inhibitory role in the expression of behavioral sensitization to methamphetamine.