Table 5. Chemical Structures and Pharmacological Profile of Isatin Oxime Analogues 5.1−5.3a.
GluA1 |
GluA2 | GluK1 |
GluK2 |
||||
---|---|---|---|---|---|---|---|
cmpd | bind. | func. | bind. | bind. | func. | bind. | func. |
5.1 (NS 102) | −b | −b | −b | −b | 6c | 1.4d | −b |
5.2 (NS 257)e | −b | 0.97 | −b | −b | −b | −b | 2.3 |
5.3 ((R/S)-NS 1209) | 0.12g | −b | 0.030g | 0.74g | 0.63f | 6.2g | 65f |
All values in [μM].
Not tested.
KB value for inhibition of Ca2+ influx in rat dorsal root ganglion (DRG) neurons; from ref (49),.
Displacement of [3H]KA radioligand; from ref (65).
IC50 values for inhibition of KA-induced depolarization in the appropriate mRNA-injected Xenopus oocytes; from ref (67).
IC50 values for inhibition of domoate-induced currents in HEK293 cells; from ref (68).
Displacement of [3H]AMPA radioligand; from ref (69).