TABLE 1

Uptake of 11C-dLop in Composite Neocortex at Baseline and After Pharmacologic Inhibition of P-Glycoprotein

ConditionAUC10–30 (SUV⋅min)K1 (mL⋅cm−3⋅min−1)k2 (min−1)VT (mL⋅cm−3)
Baseline (n = 14)2.94 ± 0.660.014 ± 0.0020.012 ± 0.0021.20 ± 0.16
Tariquidar
 4 mg/kg concurrent (n = 2)14.61 ± 2.31
 2 mg/kg concurrent (n = 10)15.34 ± 5.25*
 1,500 mg oral (n = 3)2.06 ± 0.07
 4 mg/kg delayed (n = 4)5.26 ± 2.26†0.026 ± 0.0090.010 ± 0.0012.56 ± 0.64
 6 mg/kg delayed (n = 3)10.05 ± 3.25‡0.049 ± 0.0110.013 ± 0.0013.88 ± 0.71
Disulfiram
 500 mg (n = 3)3.13 ± 0.430.012 ± 0.0010.011 ± 0.0011.14 ± 0.03
 2,500 mg (n = 3)2.44 ± 0.120.012 ± 0.0070.008 ± 0.0031.53 ± 0.66

  • ↵* P < 0.0001 vs. baseline.

  • ↵† P = 0.06 vs. baseline.

  • ↵‡ P = 0.003 vs. baseline.

  • K1 = rate constant for brain entry; k2 = rate constant for brain efflux.

  • Data are mean ± SD.