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Table 1 Binding affinity (Ki) of compounds 1–3 for 5-HT1A receptors and other biogenic amines, neurotransmitter receptors, and transporters

From: Synthesis, in vitro and in vivo evaluation of 11C-O-methylated arylpiperazines as potential serotonin 1A (5-HT1A) receptor antagonist radiotracers

 

(1)

(2)

(3)

Target

Ki(nM)

Ki(nM)

Ki(nM)

5-HT1A

22

7.7

5.8

5-HT1B

> 10,000

> 10,000

> 10,000

5-HT1E

> 10,000

> 10,000

> 10,000

5-HT1D

> 10,000

> 10,000

1176

5-HT2A

> 10,000

> 10,000

> 10,000

5-HT2B

403

516

137

5-HT2C

> 10,000

> 10,000

> 10,000

5-HT3

> 10,000

> 10,000

> 10,000

5-HT4

> 10,000

> 10,000

> 10,000

5-HT5a

> 10,000

> 10,000

1805

5-HT6

> 10,000

> 10,000

> 10,000

5-HT7R

76

830

530

Alpha1A

129

46

23

Alpha1B

1080

254

142

Alpha1D

213

53

19

Alpha 2A

453

> 10,000

> 10,000

Alpha2B

670

> 10,000

2215

Alpha2C

835

> 10,000

1984

D2R

777

> 10,000

800

D3R

369

2552

133

D4R

137

88

153

D1, D5

> 10,000

> 10,000

> 10,000

DAT

> 10,000

> 10,000

> 10,000

NET

> 10,000

> 10,000

> 10,000

SERT

> 10,000

> 10,000

> 10,000

Adenosine receptors

> 10,000

> 10,000

> 10,000

AMPA

> 10,000

> 10,000

> 10,000

Beta Receptors

> 10,000

> 10,000

> 10,000

CB1, CB2

> 10,000

> 10,000

> 10,000

DOR, KOR, MOR

> 10,000

> 10,000

> 10,000

H1-H4

> 10,000

> 10,000

> 10,000

Muscarinic receptors

> 10,000

> 10,000

> 10,000

NMDA

> 10,000

> 10,000

> 10,000

NOP

> 10,000

> 10,000

> 10,000

PBR

> 10,000

> 10,000

> 10,000

Sigma 2

> 10,000

> 10,000

> 10,000

Sigma1R

520

> 10,000

> 10,000