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. Author manuscript; available in PMC: 2022 Jan 6.
Published in final edited form as: ACS Chem Neurosci. 2020 Dec 16;12(1):79–98. doi: 10.1021/acschemneuro.0c00561

Table 2.

Effect of EU1180–55 and EU1180–154 Enantiomers on the Glutamate Response Time Course

amplitude (pA)a deactivation τW (ms)b
control (S)-EU1180–55 foldc N control (S)-EU1180–55 foldc N
GluN1/GluN2A 768 ± 141 1604 ± 297 2.1d 11 80 ± 9.7 250 ± 24 3.1d 9
GluN1/GluN2B 454 ± 172 1290 ± 436 2.8d 7 569 ± 45 934 ± 47 1.6d 10
GluN1/GluN2C 152 ± 42 879 ± 213 5.8d 7 513 ± 25 716 ± 40 1.4d 16
GluN1/GluN2D 204 ± 51 856 ± 215 4.2d 7 5510 ± 329 6500 ± 357 1.2d 12
amplitude (pA)a deactivation τW (ms)b
control (R)-EU1180–55 foldc N control (R)-EU1180–55 foldc N
GluN1/GluN2A 1020 ± 241 1560 ± 364 1.5d 12 55 ± 4.5 89 ± 6.3 1.6d 8
GluN1/GluN2B 452 ± 143 561 ± 179 1.2d 8 628 ± 39 822 ± 73 1.3d 15
GluN1/GluN2C 158 ± 34 811 ± 145 5.1d 7 576 ± 28 827 ± 42 1.4d 10
GluN1/GluN2D 291 ± 102 1120 ± 264 3.8d 6 6830 ± 279 8010 ± 318 1.2d 13
amplitude (pA)a deactivation τW (ms)b
control (S)-EU1180–154 foldc N control (S)-EU1180–154 foldc N
GluN1/GluN2A 754 ± 196 1080 ± 337 1.4d 7 79 ± 9.2 148 ± 22 2.0d 8
GluN1/GluN2B 600 ± 301 1040 ± 418 1.7d 8 670 ± 31 1001 ± 71 1.5d 10
GluN1/GluN2C 206 ± 58 589 ± 170 2.9d 6 433 ± 30 609 ± 65 1.4d 6
GluN1/GluN2D 201 ± 34 580 ± 101 2.9d 7 5540 ± 156 6660 ± 395 1.2d 9
amplitude (pA)a deactivation τW (ms)b
control (R)-EU1180–154 foldc N control (R)-EU1180–154 foldc N
GluN1/GluN2A 841 ± 146 1130 ± 219 1.3d 10 56 ± 5.5 66 ± 5.9 1.3 15
GluN1/GluN2B 422 ± 221 442 ± 228 1.0 6 616 ± 36 720 ± 44 1.2d 12
GluN1/GluN2C 185 ± 48 296 ± 77 1.6d 13 411 ± 14 522 ± 23 1.3d 8
GluN1/GluN2D 227 ± 25 313 ± 38 1.4d 15 5980 ± 384 6360 ± 192 1.1 7
a

Steady-state current response to 100 μM glutamate plus vehicle and the response amplitude following a direct switch to glutamate plus 15 μM (S)- or (R)-EU1180–55 or 5 μM (S)- or (R)-EU1180–154 were measured using whole cell current recordings from transfected HEK cells. Data shown are mean ± SEM; 30 μM glycine was present in all solutions and recordings were made at −70 mV.

b

Agonist-evoked currents were recorded in response to rapid application of 100 μM glutamate plus 30 μM glycine for 1.5 s. (S)- or (R)-EU1180–55 (15 μM) or (S)- or (R)-EU1180–154 (5 μM) was added to the glycine-containing wash, and the glutamate/glycine-containing solution and recordings were repeated in the same cell. Recordings were made at −70 mV.

c

Fold is the ratio of parameter in drug to control.

d

p < 0.05 by paired t test of amplitude and weighted tau (τW). Power to detect an effect size of 1.5 was 0.8–0.99 for steady-state amplitude and for weighted tau.