Skip to main content

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.