in rats: On day 1 and following an overnight fast, animals were weighed (body weight range: 258–307 g) and each formulation was administered to a group of four male and four female rats. The i.v. formulation was administered by jugular venipuncture at a dose volume of 2 ml kg−1. The oral formulation was administered by gavage at a dose volume of 2 ml kg−1. Following dose administration, blood samples (0.25–0.40 ml) were collected from each animal by jugular venipuncture under isoflurane anesthesia. Blood samples were collected (using lithium heparin as the anticoagulant) at pre-dose and again at 0.08 (i.p. only), 0.25 (oral only), 0.33 (i.p. only), 0.5 (oral only), 1, 2, 4, 8, and 24 h post-dose.

Binding of 3H-JNJ-5207852 to rat H3 receptor were studied. Membranes from rat brain were incubated with increasing concentrations of 3H-JNJ-5207852 (0-70 nM)