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Table 1 Potential for saxagliptin to antagonize binding of radioligands to cardiovascular-related receptors, ion channels, and enzymes

From: Nonclinical and clinical pharmacology evidence for cardiovascular safety of saxagliptin

Target

L type Ca2+

GABA-A

α1B2γ2

Cardiac

hNAV1.5

Adrenergic α1β

Muscarinic

M2

ACE

PDE

IC50 or EC50, μM

>25

>30

>30

>30

>30

>60

>30

  1. ACE acetylcholinesterase, GABA-A gamma-aminobutyric acid type A, PDE phosphodiesterase