Figure 1.
NVP-AAM077 discriminates poorly between NR2A- and NR2B-containing receptors. Concentration–response curves showing NVP-AAM077 inhibition of rodent NR1a/NR2A and NR1a/NR2B receptors expressed in Xenopus oocytes, as described by Perin-Dureau et al. (2002), are shown. NMDAR currents were elicited at −60 mV using glycine at a saturating concentration (100 μm) and glutamate at a concentration close to EC50 (5 μm for NR1a/NR2A and 2 μm for NR1a/NR2B receptors). NVP-AAM077 was applied during an application of glutamate plus glycine. The inhibition was quantified once the response in NVP-AAM077 had reached steady state. The curves represent least-square fits to the data points using the following equation: Irel = 100 − 100/(1 + (IC50/[NVP-AAM077])n). The estimated values of IC50 and n values are: 23 nm and 1.10 for NR1a/NR2A receptors and 213 nm and 1.07 for NR1a/NR2B receptors. Each point is the mean value obtained form five to eight cells. NVP-AAM077 stock solutions (1 mm and 100 μm) were prepared by progressive dilutions with bidistilled water of a solution containing 10 mm NVP-AAM077 in 100 mm NaCl. Error bars represent SD.
