TABLE 2

Kp,uu,lumbar CSF values of test compounds in the presence or absence of concomitant treatment with zosuquidar in cynomolgus monkeys

Test CompoundsUnbound Plasma AUCaCSF AUCaKp,uu,lumbar CSFKp,uu,lumbar CSF Ratio
Zosuquidar (−)bZosuquidar (+)cZosuquidar (−)bZosuquidar (+)cZosuquidar (−)bZosuquidar (+)cZosuquidar (+)/(−)
Antipyrine2980 ± 11802870 (3120, 2650)3110 ± 11303080 (3290, 2870)1.05 ± 0.041.07 (1.05, 1.08)1.0
Ondansetron586 ± 180508 (752, 484)493 ± 110653 (728, 578)0.861 ± 0.0961.08 (0.968, 1.19)1.3
Desloratadine515 ± 39587 (619, 692)77.0 ± 8.5163 (164, 163)0.151 ± 0.0260.250 (0.264, 0.235)1.7
Quinidine483 ± 181363 (515, 332)114 ± 39412 (472, 351)0.239 ± 0.0110.987 (0.916, 1.06)4.1
  • a Unit, ng·h/ml.

  • b Mean ± S.D. of three animals.

  • c Mean of two animals with individual values in the parenthesis.