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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)

Ketamine

KEA-1010

KEA-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