Table 4. Effects of pretreatment with kinase inhibitors on SKF-82958-induced desensitization of DOPR in CHO-FLAG-hDOPR/HA-D1R cells.
EC50 and Emax values of DPDPE in stimulating [35S]GTPγS binding to membranes of CHO-FLAG-hDOPR/HA-D1R cells pretreated with or without the inhibitors were calculated. Each value represents the mean ± s.e.m. of three to four independent experiments performed in duplicate.
| EC50 (nM) | Emax (fmol/mg protein) | ||
|---|---|---|---|
| Control | vehicle | 20.3 ± 2.1 | 59.6 ± 5.9 |
| SKF | 35.3 ± 10.7 | 31.6 ± 3.6* | |
|
| |||
| PKC inhibitor GF 109203X | vehicle | 20.3 ± 6.5 | 57.2 ± 3.8 |
| SKF | 16.7 ± 4.1 | 34.3 ± 4.7* | |
|
| |||
| MEK1 inhibitor PD 98059 | vehicle | 22.6 ± 6.0 | 57.9 ± 4.4 |
| SKF | 22.2 ± 5.1 | 60.5 ± 4.2 | |
|
| |||
| PI3K inhibitor wortmannin | vehicle | 17.1 ± 2.9 | 60.5 ± 4.7 |
| SKF | 21.3 ± 8.8 | 47.5 ± 3.2 | |
|
| |||
| PKA inhibitor Rp-cAMP-SH | vehicle | 20.3 ± 2.1 | 66.8 ± 7.8 |
| SKF | 17.5 ± 4.8 | 56.9 ± 3.1 | |
*
P<0.05, compared to the vehicle control by two tailed t test.