TABLE 5.
Quantification of effects of single point mGlu5 mutations on pharmacological characteristics of allosteric modulators
Data represent the mean ± S.E.M. from at least three independent determinations. Parameters are as defined for Table 2.
| Cell Line | MPEP, pKB | VU29 |
CPPHA |
||
|---|---|---|---|---|---|
| pKB | logβ | pKB | logβ | ||
| Wild-type | 8.58 ± 0.17 | 6.87 ± 0.19 | 0.40 ± 0.03 | 5.62 ± 0.16 | 0.78 ± 0.14 |
| F585I | 8.28 ± 0.15 | N.D. | N.D. | 5.14 ± 0.15 | 0.61 ± 0.07 |
| Y658V | 6.57 ± 0.13* | N.D. | N.D. | N.D. | N.D. |
| L743V | 8.04 ± 0.10* | 6.52 ± 0.17 | 1.04 ± 0.09* | N.D. | N.D. |
| A809V | 6.52 ± 0.12* | 5.31 ± 0.26* | 0.58 ± 0.10 | N.D. | N.D. |
N.D., not determined.
*
Significantly different (P < 0.05) from wild-type value, with one-way analysis of variance and Dunnett's post hoc test.