Table 1 Effects on intracellular Ca2+ level and AMPA-R-mediated currents in the presence or absence of AMPA in rat primary hippocampal neurons.

From: Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement

 

Intracellular Ca2+ level *

AMPA-R currents #

Potentiation EC50 (μM)

Agonistic effect @30 μM (%)

Potentiation EC50 (μM)

Agonistic effect @30 μM (%)

TAK-653

0.93

4.8

4.4

1.7

TAK-137

0.42

7.6

1.4

6.4

LY451646

0.78

88

1.9

39

  1. *% of 5 μM AMPA + 10 μM HBT1 response.
  2. # % of AMPA (100 μM)-induced steady-state response.
  3. EC50 value was calculated from dose-response curve in the presence of 5 μM AMPA for intracellular Ca2+ levels or 1 μM AMPA for AMPA-R currents using a nonlinear regression.
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