740873-06-7

In rats Naluzotan shows 11% oral bioavailability with a serum t_1/2 of 2?3.5 h when administrated po, attaining a C_max level of 24 ± 13 ng/mL (3 mg/kg, po). Naluzotan shows significant brain penetration, achieving a brain:serum concentration ratio of approximately 0.5 in the rat at 1 h following either intravenous or oral administration and reaching brain concentration approximately equivalent to that of buspirone. In dogs the pharmacokinetic profile of naluzotan shows 16% oral bioavailability, a serum t_1/2 of 1.1 h po, and a C_max level of 174 ± 141 ng/mL (3 mg/kg, po)^[1]. PRX-00023 (0.01-0.05 mg/kg, i.p.) significantly reduces USV rates, but done of these doses produce sedation in rats^[2].