Ligand | α1 | α1K104A | α1F108A | α1T112A | ||||
---|---|---|---|---|---|---|---|---|
IC50 | n | IC50 | n | IC50 | n | IC50 | n | |
Strychnine | 2-15016.0 ± 2.0 | (6) | 172.0 ± 8.8 | (5) | 293.1 ± 5.7 | (2) | 1605 ± 100 | (2) |
Nipecotic a. | #0.82 ± 0.1 | (13) | 3.62 ± 0.54 | (9) | 3.09 ± 0.27 | (5) | 7.11 ± 0.99 | (6) |
Isonipecotic a. | #0.23 ± 0.03 | (5) | 0.61 ± 0.1 | (7) | n.d. | 2.35 ± 0.5 | (5) | |
Isobutyric a. | #2.9 ± 0.5 | (3) | 20.4 ± 1.28 | (4) | n.d. | n.d. | ||
5,7CIQA | †19.4 ± 5.1 | (5) | 26.0 ± 1.0 | (2) | n.d. | n.d. | ||
β-AIBA | #0.8 ± 0.1 | (3) | 2.37 ± 0.45 | (4) | n.d. | n.d. |
Inhibition of glycine currents by antagonists was analyzed in oocytes injected with the mutant α1 cRNAs. IC50 values were determined using a glycine concentration corresponding to the respective EC50 value (see Table 1). Data represent mean ± S.E.M. of n experiments and are given for strychnine in nM, 5,7CIQA in μM, and nipecotic acid, isonipecotic acid, isobutyric acid, and β-AIBA in mM, respectively.
n.d., not determined.
↵2-150 ,#,† Data taken from Schmieden et al., 1989, Schmieden and Betz, 1995, and Schmieden et al., 1996, respectively.