TABLE 3

Derived pharmacokinetic parameters of the seven model compounds and the observed brain half-lives


Compound

kout a

kel b

t1/2eq c

t1/2eq,in d

Obs.t1/2eqe
h-1 h
Caffeine 18 0.75 0.040 0.039 0.1
CP-141938 2.7 0.33 0.29 0.26 1
Fluoxetine 0.70 0.23 1.5 1.0 1
NFPS 0.14 0.21 N.A.f 5.0 >24
Propranolol 5.1 0.74 0.16 0.14 0.1
Theobromine 10 0.11 0.071 0.070 0.1
Theophylline
17
0.20
0.041
0.040
0.1
  • a kout = PS · fu,brain/Vb

  • b kel = Clp/Vp except for fluoxetine. The kel of fluoxetine was calculated from Clp, Cld, Vp, and Vsp using eq. 8

  • c t1/2eq = ln2/(koutkel)

  • d t1/2eq,in = ln2/kout

  • e Estimated visually from the BP time course in Fig. 2

  • f Not applicable due to kout < kel