Table 2.
Profile of Inverse Agonists in HERK Treated Membranes
| Drug | EC50 (nM±SD) |
EMAX (Percent±SD) |
|---|---|---|
| LTC-274 | 1.6±0.4 | -37±2 |
| 6-β-Naltrexamide | 2.6±0.5 | -67±2 |
| BNTX | 3.1±0.43 | -82±2 |
| Diprenorphine | 0.26±0.06 | -84±3 |
| NorBNI | 32±6 | -86±3 |
| CTAP | 38±5 | -89±2 |
| Naltrexone | 0.96±0.13 | -90±2 |
| NTB | 6.6±1.3 | -90±3 |
| Naloxone | 1.8±0.1 | -91±1 |
| NTI | 17±4 | -94±4 |
| 6-β-naltrexol | 1.2±0.12 | -98±1 |
| KC-2-009 | 6.7±0.4 | -100±1 |
Inverse agonist dose-response curves (10 points per curve) were generated as described in Methods. The EMAX is normalized with 100% being the inhibition of [35S]-GTP-γ-S binding produced by 5 μM KC-2-009. The data of 3 experiments were meaned and the best-fit estimates of the EC50 and EMAX determined using nonlinear least squares curve fitting programs. Each value is ±SD.