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Table 2 Overview of specific NET binding of the radioligand [11C]Me@HAPTHI vs. Me@HAPTHI and FMeNER-D2 on rat and human tissue origin

From: Radiosynthesis and first preclinical evaluation of the novel norepinephrine transporter pet-ligand [11C]ME@HAPTHI

n ≥ 3

[11C]Me@HAPTHI

% BL-competitor

fmol

Rat heart

 FMeNER 1 μM

88.8 ± 11.2

<0.01

 FMeNER 100nM

99.00 ± 0.07

<0.01

 Me@HAPTHI 1 μM

92.5 ± 7.5*

<0.01

 Me@HAPTHI 100nM

104.5 ± 4.5

<0.01

Human cortex

 FMeNER 1 μM

71.9 ± 7.9*

0.86

 FMeNER 100nM

86.3 ± 11.2*

<0.01

 Me@HAPTHI 1 μM

66.3 ± 5.9*

1.32

 Me@HAPTHI 100nM

82.1 ± 13.9*

0.02

Human thalamus

 FMeNER 1 μM

68.36 ± 2.11

0.71

 FMeNER 100nM

77.6 ± 9.8

0.47

 Me@HAPTHI 1 μM

85.9 ± 18.5

0.09

 Me@HAPTHI 100nM

92.5 ± 17.3

0.26

Human hypothalamus

 FMeNER 1 μM

77.4 ± 14.5

0.02

 FMeNER 100 nM

97.8 ± 14.6

0.11

 Me@HAPTHI 1 μM

62.0 ± 3.6*

0.04

 Me@HAPTHI 100 nM

83.7 ± 1.7*

0.05

Human hippocampus

 FMeNER 1 μM

67.3 ± 8.2

<0.01

 FMeNER 100 nM

97.1 ± 10.3

<0.01

 Me@HAPTHI 1 μM

68.3 ± 5.3

<0.01

 Me@HAPTHI 100 nM

84.1 ± 9.3

<0.01

Human nucleus caudatus

  

 FMeNER 1 μM

107.6 ± 17.7

n.d.

 FMeNER 100nM

102.6 ± 14.5

n.d.

 Me@HAPTHI 1 μM

110.0 ± 21.0

n.d.

 Me@HAPTHI 100nM

93.5 ± 12.5

nd

Human cerebellum

  

 FMeNER 1 μM

108.2 ± 17.3

n.d.

 FMeNER 100nM

103.9 ± 12.2

n.d.

 Me@HAPTHI 1 μM

107.2 ± 20.8

n.d.

 Me@HAPTHI 100nM

124.7 ± 10.8

n.d.

  1. fmol values reflect calculated relative concentration (fmol/mm2) of transporter protein). Limit of detection = 0.01 fmol; BL=baseline
  2. n.d. not determined
  3. *p < 0.05