Taurine, a beta-amino acid, plays an important role as a neuromodulator and is necessary for the normal development of the brain. Since de novo synthesis of taurine in the brain is minimal and in vivo studies suggest that taurine does not cross the blood-brain barrier, we examined whether the choroid plexus, the blood-cerebrospinal fluid barrier, plays a role in taurine transport in the central nervous system. The uptake of [3H]taurine into ATP-depleted choroid plexus from rabbit was substantially greater in the presence of an inwardly directed Na+ gradient, whereas in the absence of a Na+ gradient taurine accumulation was negligible. A transient inside-negative potential gradient enhanced the Na(+)-driven uptake of taurine into the tissue slices, suggesting that the transport process is electrogenic. Na(+)-driven taurine uptake was saturable with an estimated Vmax of 111 +/- 20.2 nmol/g per 15 min and a Km of 99.8 +/- 29.9 microM. The estimated coupling ratio of Na+ and taurine was 1.80 +/- 0.122. Na(+)-dependent taurine uptake was significantly inhibited by beta-amino acids, but not by alpha-amino acids, indicating that the transporter is selective for beta-amino acids. Na(+)-dependent taurine uptake showed some selectivity for anions: the accumulation was comparable in the presence of Cl-, Br- and thiocyanate whereas I-, SO4(2-) and gluconate did not stimulate the uptake significantly. Collectively, our results demonstrate that taurine is transported in the choroid plexus via a Na(+)-dependent, saturable and apparently beta-amino acid selective mechanism. This process may be functionally relevant to taurine homeostasis in the brain.