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EJNMMI Research

Table 2 In vitro properties of TASP0390136, TASP0410457, and TASP0434988

From: Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors

 

Affinity for H3Rs

Off-target binding

Log D7.4

Efflux ratio (MDR1)

Rat, IC50

Monkey, IC50

Sigma 1, IC50

Adrenergic α2c, IC50

nM (n = 3)

nM (n = 3)

nM

nM

TASP0390136

2.74

1.06

167

>1000

1.36

6.29

TASP0410457

2.34

1.80

379

>1000

1.79

1.64

TASP0434988

0.783

0.565

257

528

2.22

2.14

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