TABLE A1

Appendix I: Pharmacokinetic parameters of compounds used in the present investigation

Units for CL and Vd are ml/min/kg and l/kg, respectively.


Compound

Rat

Dog

Monkey

Human
CL
Vd
CL
Vd
CL
Vd
CL
Vd
αVβ3 antagonista,29 47.0 1.5 5.4 0.9 9.0 0.3 1.0 0.2
Amiodarone3,36,38 14.7 72.3 14.7 4.6 10.7b 5.1b 1.9 66.0
Biperiden27 68.0 14.0 27.0 9.5 21.9b 3.6b 15.3 6.2
Chlorpromazine7,33 61.0 29.1 53.0 16.3 24.6b 8.0b 4.3 11.2
Diltiazem4,26,36,41 82.3 3.6 59.0 21.4 34.5b 3.5b 12.0 3.1
Epiroprim23 45.0 4.6 10.7 8.3 30.6 5.1 3.5 2.5
Felodipine2,10 84.7 12.4 19.5 7.8 15.7b 2.2b 11.1 9.7
Flindokalner20 29.9 3.4 3.1 3.2 40.2 5.4 7.63 2.35
Garenoxacin16 12.1 0.9 2.4 1.3 3.4 1.0 1.2 1.0
Haloperidol5,34,36 86.2 10.4 32.9b 37.0b 7.8 6.6 11.8 18.0
Methadone13,22,36 59.3 7.58 41.4 7.6 29.4b 8.2b 1.4 3.8
Midazolam1,6,12 67.0 1.6 27.0 3.0 24.2 1.5 6.6 1.1
Mifepristone8 50.0 4.3 15.6b 10.5b 24.2 32.5 0.33 0.30
Nifedipine11,15,36 4.5 0.127 12.3 1.15 10.0b 0.5b 7.0 0.78
Ofloxacin14,18,19,28,39 26.3 1.66 2.65 1.15 7.5c 1.6c 4.53 1.78
PNU-9639140 46.7 1.5 36.7 2.5 33.3 1.4 7.2 2.2
Propafenone9,30 62.0 5.2 30.8 3.0 44.1b 8.2b 8.8 2.29
Remoxipride37 170.0 4.5 4.9 1.6 11.8b 1.1b 1.7 0.7
Semaxanib32,35 45.0 1.6 52.0 1.4 25.7 1.45 14.0 0.98
Verapamil24,25 40.4 2.99 62.2 4.47 37.1b 4.5b 13.7 5.5
Vinorelbine17,21,31
31.7
24.4
20.0
49.6
23.6b
11.4b
21.0
75.6
  • a 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)propyl-imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)propionic acid

  • b Parameter derived from data generated in this laboratory

  • c Data specifically for S-Ofloxacin