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. 2015 Jun 17;35(11):1827–1835. doi: 10.1038/jcbfm.2015.133

Table 2. Kinetic rate constants estimated with a 2-TCMi at baseline and after PF-04457845 with 60 minutes of scan data.

60 minutes K1 (mL/cm3/min) k2 (1/min) k3 (1/min) Ki (mL/cm3/min) λk3 (mL/cm3/min)
Prefrontal cortex
 Baseline 0.28 (0.03) 0.11 (0.02) 0.061 (0.009) 0.102 (0.010) 0.159 (0.015)
 PF 1 mg 0.35 (0.02) 0.12 (0.01) 0.007 (0.002) 0.018 (0.004) 0.019 (0.005)
 PF 4 mg 0.31 (0.02) 0.10 (0.01) 0.003 (0.001) 0.010 (0.002) 0.010 (0.003)
 PF 20 mg 0.30 (0.06) 0.10 (0.01) 0.006 (0.001) 0.015 (0.001) 0.016 (0.001)
           
Temporal cortex
 Baseline 0.29 (0.03) 0.11 (0.01) 0.062 (0.006) 0.106 (0.010) 0.168 (0.018)
 PF 1 mg 0.34 (0.01) 0.11 (0.01) 0.007 (0.002) 0.018 (0.004) 0.020 (0.005)
 PF 4 mg 0.32 (0.01) 0.10 (0.01) 0.003 (0.001) 0.011 (0.001) 0.011 (0.001)
 PF 20 mg 0.31 (0.07) 0.10 (0.01) 0.005 (0.002) 0.015 (0.002) 0.016 (0.003)
           
Occipital cortex
 Baseline 0.28 (0.04) 0.11 (0.01) 0.061 (0.009) 0.101 (0.013) 0.159 (0.021)
 PF 1 mg 0.35 (0.04) 0.12 (0.02) 0.006 (0.001) 0.016 (0.003) 0.016 (0.004)
 PF 4 mg 0.31 (0.03) 0.10 (0.01) 0.004 (0.001) 0.011 (0.001) 0.011 (0.001)
 PF 20 mg 0.30 (0.07) 0.10 (0.01) 0.006 (0.001) 0.015 (0.001) 0.015 (0.001)
           
Parietal cortex
 Baseline 0.31 (0.04) 0.11 (0.01) 0.063 (0.009) 0.110 (0.012) 0.172 (0.019)
 PF 1 mg 0.37 (0.01) 0.12 (0.01) 0.007 (0.002) 0.020 (0.003) 0.021 (0.004)
 PF 4 mg 0.33 (0.01) 0.10 (0.01) 0.005 (0.001) 0.014 (0.002) 0.015 (0.002)
 PF 20 mg 0.33 (0.08) 0.10 (0.01) 0.005 (0.001) 0.016 (0.002) 0.017 (0.002)
           
A. cingulate
 Baseline 0.26 (0.02) 0.11 (0.01) 0.068 (0.009) 0.098 (0.007) 0.159 (0.014)
 PF 1 mg 0.31 (0.02) 0.11 (0.01) 0.004 (0.001) 0.010 (0.002) 0.010 (0.003)
 PF 4 mg 0.29 (0.01) 0.10 (0.01) 0.004 (0.002) 0.011 (0.004) 0.012 (0.004)
 PF 20 mg 0.26 (0.07) 0.09 (0.01) 0.002 (0.001) 0.006 (0.003) 0.006 (0.003)
           
Insular cortex
 Baseline 0.27 (0.03) 0.11 (0.02) 0.066 (0.009) 0.106 (0.008) 0.173 (0.015)
 PF 1 mg 0.34 (0.01) 0.12 (0.01) 0.007 (0.004) 0.019 (0.008) 0.021 (0.009)
 PF 4 mg 0.30 (0.01) 0.09 (0.01) 0.004 (0.002) 0.013 (0.006) 0.013 (0.006)
 PF 20 mg 0.30 (0.06) 0.10 (0.01) 0.005 (0.001) 0.015 (0.002) 0.016 (0.002)
           
Cerebellar cortex
 Baseline 0.28 (0.02) 0.10 (0.01) 0.057 (0.007) 0.105 (0.010) 0.168 (0.017)
 PF 1 mg 0.33 (0.01) 0.10 (0.01) 0.004 (0.002) 0.013 (0.003) 0.013 (0.004)
 PF 4 mg 0.28 (0.02) 0.08 (0.01) 0.002 (0.001) 0.008 (0.001) 0.008 (0.001)
 PF 20 mg 0.31 (0.05) 0.10 (0.01) 0.005 (0.001) 0.014 (0.001) 0.014 (0.001)
           
Hippocampus
 Baseline 0.19 (0.03) 0.09 (0.02) 0.071 (0.018) 0.087 (0.009) 0.160 (0.016)
 PF 1 mg 0.23 (0.01) 0.09 (0.02) 0.009 (0.005) 0.019 (0.008) 0.021 (0.009)
 PF 4 mg 0.20 (0.01) 0.08 (0.01) 0.006 (0.001) 0.015 (0.003) 0.017 (0.004)
 PF 20 mg 0.21 (0.04) 0.08 (0.01) 0.007 (0.001) 0.017 (0.003) 0.018 (0.003)
           
Amygdala
 Baseline 0.16 (0.02) 0.08 (0.05) 0.069 (0.032) 0.073 (0.010) 0.136 (0.020)
 PF 1 mg 0.19 (0.01) 0.08 (0.01) 0.008 (0.003) 0.017 (0.006) 0.019 (0.008)
 PF 4 mg 0.17 (0.01) 0.07 (0.01) 0.004 (0.002) 0.010 (0.005) 0.011 (0.005)
 PF 20 mg 0.16 (0.03) 0.07 (0.01) 0.007 (0.002) 0.015 (0.001) 0.016 (0.002)
           
Caudate
 Baseline 0.29 (0.04) 0.11 (0.03) 0.057 (0.016) 0.100 (0.018) 0.155 (0.030)
 PF 1 mg 0.33 (0.03) 0.10 (0.01) 0.004 (0.001) 0.014 (0.003) 0.014 (0.003)
 PF 4 mg 0.31 (0.01) 0.09 (0.01) 0.001 (0.001) 0.005 (0.003) 0.005 (0.003)
 PF 20 mg 0.29 (0.03) 0.09 (0.01) 0.003 (0.001) 0.010 (0.002) 0.010 (0.002)
           
Putamen
 Baseline 0.31 (0.03) 0.10 (0.01) 0.056 (0.009) 0.110 (0.015) 0.171 (0.028)
 PF 1 mg 0.36 (0.01) 0.10 (0.01) 0.004 (0.002) 0.015 (0.007) 0.015 (0.007)
 PF 4 mg 0.34 (0.01) 0.09 (0.01) 0.003 (0.001) 0.010 (0.004) 0.011 (0.004)
 PF 20 mg 0.32 (0.06) 0.09 (0.01) 0.003 (0.001) 0.012 (0.006) 0.012 (0.007)
           
Thalamus
 Baseline 0.31 (0.03) 0.10 (0.01) 0.061 (0.009) 0.117 (0.009) 0.189 (0.017)
 PF 1 mg 0.36 (0.02) 0.09 (0.01) 0.005 (0.001) 0.017 (0.004) 0.018 (0.005)
 PF 4 mg 0.31 (0.02) 0.07 (0.01) 0.001 (0.001) 0.005 (0.003) 0.005 (0.003)
 PF 20 mg 0.33 (0.04) 0.08 (0.01) 0.003 (0.001) 0.011 (0.002) 0.012 (0.003)

2-TCMi, irreversible two tissue compartment model; A. cingulate, anterior cingulate cortex; PF, PF-04457845. Data are in mean (s.d.) of n=6 for the baseline and n=2 each after PF-04457845 dosing at 1 mg, 4 mg, and 20 mg, respectively.