TABLE 1

Uptake parameter values (observed and predicted) for six lipophilic amine drugs with or without pretreatment with FCCP

Substrate
Kp,U1,max
Kp,min
KU1
Kp,max
Kp,min,av a
Kp,max/Kp,min
Predicted Kp,maxb
-FCCP
+FCCP
-FCCP
+FCCP
μM
Dextromethorphanc 35 15 70 50 15 3.3 54.9
Quinine 96 46 57 27 1 143 36 3.9 125
Propranolold 171 69 30 240 69 3.5 239
Imipramined 210 150 10 360 150 2.4 514
Fluvoxamine 389 181 188 157 1 577 169 3.4 579
Fluoxetine
1280
909
732
396
3
2010
564
3.6
1920

  • ↵ a Average Kp,min in the absence and presence of FCCP.

  • ↵ b Using eq. 5.

  • ↵ c Witherow and Houston (1999).

  • ↵ d Hallifax and Houston (2006).