Table 1

Pharmacokinetic parameters for R-2HMP and major metabolites after s.c. administration to the rat of 10 mg/kg R-2HMP

Tissue/ CompoundAUC0–240AUC0–∞CmaxTmaxAbsorption/FormationRedistributionElimination
C γ t1/2 A α t1/2 B β t1/2
Brain
 R-2HMP2985233328726204  ± 91215383510.107375030.067108480.0059117
 R-2HMA4775651483704  ± 19415163770.06610160440.061113330.009474
 R-2HPA1715318593286  ± 363094620.0461594090.04316530.0069100
 R-2HA3730544532  ± 13303600.051133360.04615240.0047149
Liver
 R-2HMP2635844279772755  ± 306301413410.054131402340.0521311070.0032220
 R-2HMA3124451940420  ± 893090430.0431689770.03917660.0020350
 R-2HPA1230314343191  ± 241550700.0581250300.05313400.0054129
 R-2HA* 1308314193114  ± 19302130.050142130.01354
Plasma
 R-2HMP35338408861125  ± 409513063.920.211280.068101780.0068101
 R-2HMA1594017688194  ± 16152680.292.51500.030231180.008681
 R-2HPA4980536354  ± 1115690.362200.02528490.01066
 R-2HA* 1493206113  ± 75123.710.2120.0069100
  • Values were calculated by MOR with a triexponential model, followed by variance-weighted nonlinear regression.

  • ∗, biexponential model was used.

  • Units: AUC, nanogram · minutes per gram; A, B, C,Cmax, nanograms per gram; α, β, γ, min.−1; Tmax, t1/2, min.