Table 1 Affinity and activity of ifenprodil and 3-benzazepines 1–7

From: A common mechanism allows selective targeting of GluN2B subunit-containing N-methyl-D-aspartate receptors

Compound

affinity

TEVC activity

 

Ki + SEM [nM]

IC50 ± SE [nM]

A2 ± SE [%]

p

n

ifenprodil

10 ± 1b

264 ± 27

94 ± 2

0.97

24

rac-1

84 ± 18a

94 ± 8

93 ± 2

1.25

24

(R)-1

30 ± 8a

53 ± 3

93 ± 1

1.11

24

(S)-1

740 ± 61a

206 ± 23

95 ± 2

0.98

24

2

111 ± 53b

91 ± 7

97 ± 2

1.08

24

3

10 ± 3b

3367 ± 926

92 ± 8

0.93

18

4

681 ± 133b

1305 ± 483

100 ± 9

0.70

18

5

225 ± 3b

9 ± 2%c

–

–

3

6

29 ± 2b

2629 ± 296

93d

0.70

12

7

39 ± 6b

7211 ± 1774

93d

0.62

12

  1. Ki values were determined by displacement of [³H]ifenprodil in three independent experiments. Activity was determined by TEVC at holding potential of −70 mV using GluN1-1a/GluN2B expressing oocytes and is given as IC50 value. A2 represents the maximum inhibition of compound derived from dose-response curve, while p represents the slope of the dose-response curve. n represents the number of independent oocytes, which were used to generate the dose-response curve
  2. aKi values were previously published34
  3. bNewly recorded Ki values
  4. cInhibition (% ± SEM) of ion flux at a compound concentration of 30 µM
  5. dDue to non-saturating inhibition, A2 was set as identical with rac-1
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