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Table 3 Molecular target binding profiles

From: KEA-1010, a ketamine ester analogue, retains analgesic and sedative potency but is devoid of Psychomimetic effects

Molecular Target
(Assay Type)
KetamineKEA-1010KEA-1025
IC50 [Percent Inhibition at 10 μM]
Ca2+ Channel L-Type
(Radioligand Binding)
>  10 μM
[24%]
>  10 μM
[−]
>  10 μM
[−]
GABAA Receptor
(Radioligand Binding)
>  10 μM
[−]
>  10 μM
[−]
>  10 μM
[−]
δ1 Opiate Receptor
(Radioligand Binding)
>  10 μM
[−]
>  10 μM
[−]
>  10 μM
[−]
μ Opiate Receptor
(Radioligand Binding)
>  10 μM
[−]
>  10 μM
[−]
>  10 μM
[−]
Norepinephrine Uptake Site
(Functional Uptake Assay)
>  10 μM
[23%]
>  10 μM
[−]
>  10 μM
[−]
HCN1 K+ Channel
(Patch-Clamp Functional Assay)
>  100 μM
[15%]
>  100 μM
[20%]
>  100 μM
[−]
  1. Percent Inhibition at 10 μM only quoted where inhibition > 15%
  2. Percent Inhibition in patch-clamp assay quoted at 100 μM, not 10 μM, as that was top dose employed