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Table 1 CNS PET tracer dataset a

From: Identification of positron emission tomography (PET) tracer candidates by prediction of the target-bound fraction in the brain

   Target In vitrodata PET data
  Bmax Kd Vu,brain ftb BPND ftb
  (nM)b (nM) (mL/g brain)    
[18 F]2-FA-85380 Yes nAChr a4b2 0.7 0.145 1.7 0.74 1.8 0.64
[11C]AFM Yes SERT 38 1.04 46 0.44 1.4 0.58
[18 F]Altanserin Yes 5HT2a 89 0.32 122 0.70 1.06 0.51
[11C]AZ10419369 Yes 5HT1b 9.8c 0.37 30 0.47 1.3 0.57
[11C]AZD2184 Yes Amyloid 1,407 4.9 33 0.90 1.1 0.52
[11C]AZD2995 Yes Amyloid 1,407 6.2 7 0.97 0.6 0.38
[18 F]AZD4694 Yes Amyloid 1,407 2.3 205 0.75 1.2 0.55
[11C]CP-126998 Yes AchE 211 0.48 41 0.92   
[11C]DASB Yes SERT 38 3.5 31 0.26 1.6 0.62
[18 F]Fallypridef Yes D2 27 0.03 18 0.98 22.2 0.96
[18 F]Fallyprideg Yes D2 0.9 0.03 18 0.63 2.11 0.68
[18 F]FE-PE2I Yes DAT 212 12 62 0.22 4.1 0.80
[18 F]FEPPA[iv] Yes TSPO 58 0.07 15 0.98 4.4 0.81
[11C]FLB457 Yes D2 0.9 0.02 26 0.63 2.6 0.72
[11C]Flumazenil Yes GABA 71 0.7 3.2 0.97 5.8 0.85
[18 F]FP-CIT Yes DAT 212 33 36 0.15 1.0 0.50
[11C]GR103545 Yes KOR 3.75c 0.048 41 0.66 2.18 0.69
[11C]GR205171 Yes NK1 55 0.016 57 0.98 14.5 0.94
[11C]GSK189254A Yes H3 8.4 0.08 8.5 0.93 1.3 0.57
[11C]Harmine Yes MAO-A 270 5 25 0.68 1.7 0.63
[11C]MADAM Yes SERT 38 0.06 90 0.88 1.4 0.58
[11C]McN5652 Yes SERT 38 0.2 238 0.44 0.50 0.33
[11C]MDL100907 Yes 5HT2a 89 0.24 17 0.96 1.3 0.57
[11C]MePPEP Yes CB1r 47 0.1 296 0.61 5.5 0.85
[18 F]MPPF Yes 5HT1a 350 3.3 14 0.89 1.6 0.62
[11C]NNC112 Yes D1 93 0.18 70 0.88 2.85 0.74
[11C]PBR28 Yes TSPO 58 1.8 11 0.75 3.99 0.80
[11C]PE2I Yes DAT 212 4.9 39 0.53 8.0 0.89
[11C]PHNO Yes D2/D3 26.5d 0.56 11 0.81 2.5 0.71
[11C]PIB Yes Amyloid 1,407 2.5 250 0.69 0.85 0.46
[11C]PK11195 Yes TSPO 58 4.3 59 0.19 0.18 0.15
[11C]Raclopride Yes D2 27 2.5 9.4 0.53 2.6 0.72
[18 F]Spiperone Yes D2 27 0.028 147 0.87   
[11C]SB207145 Yes 5HT4 21 0.037 4.4 0.99 3.4 0.77
[11C]SCH23390 Yes D1 93 2.1 32 0.58 1.8 0.64
[11C]WAY100635 Yes 5HT1a 350 1.1 14 0.96 7.4 0.88
[11C]Citalopram No SERT 38 4.8 60 0.12 0.1 0.09
[11C]Clomipramine No SERT 38 0.15 863 0.23 0.1 0.09
[11C]CPEB[iv] No ORL-1 13.5e 1.1 143 0.08 0.1 0.09
[11C]Desipramine No NET 5 0.63 264 0.03 0.1 0.09
[11C]Diazepam No GABA 71 7 20 0.34 0.1 0.09
[11C]MeNER No NET 5c 2.5 31 0.06 0.3 0.23
[11C]NE100 No Sigma 23e 1.2 96 0.17 0.1 0.09
[11C]Nisoxetine No NET 5 0.73 58 0.11 0.1 0.09
[18 F]Paroxetine No SERT 38 0.065 876 0.40 0.1 0.09
[11C]Remoxipride No D2 27 270 6.3 0.02 0.1 0.09
[11C]Sertraline No SERT 38 0.15 4,184 0.06 0.1 0.09
[11C]Venlafaxine No SERT 38 7.5 10 0.33 0.1 0.09
  1. aAn extended version of this table is provided as supporting information (Additional file 1: Table S1), which includes literature references to Bmax, Kd, and BPND for each tracer, details of Vu,brain determination, calculated molecular descriptors and CNS PET MPO score, and the region of brain tissue interest.
  2. bData refers to human brain tissue unless otherwise specified.
  3. cMonkey.
  4. dDog.
  5. eRat.
  6. fBmax value refers to caudate.
  7. gBmax value refers to thalamus.