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. Author manuscript; available in PMC: 2020 Jun 19.
Published in final edited form as: ACS Chem Neurosci. 2019 May 24;10(6):2989–3007. doi: 10.1021/acschemneuro.9b00205

Table 5.

Binding Affinities of 3q-s1−4 at Native NMDA Receptors and Functional Characterization as Antagonists at Cloned GluN1/GluN2A-D Receptorsa

graphic file with name nihms-1034786-t0014.jpg
Ki
compd 2,3-trans configuration Abs stereochem or d.r. at ε-carbon NMDA (binding affinity) GluN1/GluN2A GluN1/GluN2B GluN1/GluN2C GluN1/GluN2D
3q-s1 (−)-Abs (n.d.) 96:4 28 [4.56 ± 0.06] − − − −
3q-s2 (−)-Abs (n.d.) 4:96 1.3 [5.89 ± 0.09] 1.2 ± 0.1 2.8 ± 0.1 6.5 ± 0.6 15 ± 2
3q-s3,4 (+)-Abs (n.d.) 1:2 0.25 [6.61 ± 0.07] 0.61 ± 0.02 2.7 ± 0.1 12 ± 1 62 ± 9
a

All values in μM. Binding data are mean values of at least three individual experiments performed in triplicate. For NMDA: Ki values with mean pKi ± SEM in brackets. For GluN1/GluN2A-D, Ki values are reported as the mean ± SEM from six oocytes and were estimated from IC50 values using the Cheng−Prusoff relationship (see Methods). −: not tested; n.d.: not determined.