When given orally, a dose range of 100 mg to 1000 mg (approximately 1 to 15 mg/kg free base per dose) can be given to a patient.

FlpIn Chinese hamster ovary (CHO) cells stably expressing adenosine A1 receptors were used for activity evaluation. Membrane homogenates (15 mkg) were equilibrated with [3H]CCPA (2 nM) in a 1-ml total volume of assay buffer for 90 min at 30°C. R-PIA (10 mkM), alone or in the presence of T62, VCP520, or VCP333, was then added at various time points to prevent the reassociation of [3H]CCPA with the receptor. In subsequent experiments designed to investigate the effect of a range of modulator concentrations on [3H]CCPA dissociation rate, a “two-point kinetic” experimental paradigm was used in which the effect of increasing concentrations of allosteric ligand on [3H]CCPA dissociation was determined at 20 and 90 min.