Table 3 Fitting of macroscopic GluN1/GluN2A current response and effect of UBP684.

From: A single-channel mechanism for pharmacological potentiation of GluN1/GluN2A NMDA receptors

Rates

Experiment

Macroscopic Fit

Control

UBP684

Control

UBP684

b+

—

—

30

37

b−

—

—

25

84

d1+

—

—

1.00

8.2

d1−

—

—

0.30

2.0

d2+

—

—

22

165

d2−

—

—

46

107

Residual

—

—

2.67 × 10−6

8.85 × 10−5

glutamate EC 50 or K d

4.62 ± 0.32

3.12 ± 0.52

0.84

2.2

P O (peak)

0.54 ± 0.04

0.13 ± 0.03

0.55

0.13

MOT

2.276

5.093

2.1

0.453

  1. The normalized residual sum of squares (indicated as Residual) were derived from the macroscopic fitting with the gating rates fixed to those derived from MIL fits (Fig. 4); the desensitization (d) and agonist binding (b+) and unbinding (b−) rates were set as free parameters. The agonist binding rates are in µM−1 s−1 and all other rate constants are s−1. The K d is in µM and calculated as b−/b+. The desensitization rates were constrained to 5-fold ± rates derived from MIL fits (Fig. 4). Open probability (P o ), mean open time (MOT).
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