Inhibition of [3H]-SR31747 binding to recombinant SI by various drugs
| Drug | Enzyme | ||
|---|---|---|---|
| mSI | hSI | ySI | |
| SR31747 | 2.6 ± 0.2 | 1.5 ± 0.1 | 2.8 ± 0.2 |
| Tamoxifen | 1.9 ± 0.2 | 3.6 ± 0.4 | >3200 |
| cis-Flupentixol | 2.2 ± 0.1 | 1.8 ± 0.1 | >1000 |
| Trifluoperazine | 33 ± 3 | 18 ± 1 | >1000 |
| 7-Ketocholestanol | 7.2 ± 1.1 | 30 ± 0.2 | 300 ± 40 |
| SKF-525A | >1000 | 150 ± 0.9 | >1000 |
| Emopamil1-a | >1000 | >1000 | >1000 |
| Ifenprodil | 49 ± 4 | 29 ± 7 | 16 ± 2 |
| Verapamil | >3200 | >10,000 | >10,000 |
| Fenpropimorph | 44 ± 1 | 29 ± 8 | 0.10 ± 0.01 |
| Tridemorph | 1.6 ± 0.1 | 0.82 ± 0.07 | 0.18 ± 0.01 |
| (+)-Pentazocine | >10,000 | >10,000 | >10,000 |
| DTG | >10,000 | >10,000 | >10,000 |
| Haloperidol | >10,000 | >10,000 | 1.3 ± 0.1 |
↵1-a Inhibition of [3H]SR31747 binding to mSI, hSI and ySI by 1 mM emopamil was 0%, 34% and 43%, respectively.
IC50 values are expressed in nM.