Table 4.
Compound | IC50, nM | μ versus δ selectivity | |
---|---|---|---|
Binding versus [3H]DPDPE | Binding versus [3H]CTOP | ||
1. Somatostatin | 15,000a | 20,000a | 0.7 |
2. D-Phe-c[Cys-Phe-D-Trp-Lys-Thr-Pen]Thr-OH | 20,000a | 1,000b | 20 |
3. D-Phe-c[Pen-Phe-D-Trp-Lys-Thr-Pen]Thr-OH | 9,800a | 10,800b | none |
4. D-Phe-c[Cys-Tyr-D-Trp-Lys-Thr-Pen]Thr-OH | 3,800a | 290b | 13 |
5. D-Phe-c[Cys-Tyr-D-Trp-Lys-Thr-Pen]Thr-NH2 | 950a | 3.5b | 270 |
6. D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Pen]Thr-NH2 | 2,000 | 5.5 | 360 |
7. D-Phe-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]Thr-NH2 (CTAP) | 4,500 | 3.5 | 1,300 |
8. D-Phe-c[Cys-Trp-D-Trp-Orn-Thr-Pen]Thr-NH2 (CTOP) | 13,500 | 2.8 | 4,800 |
9. D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 | 1,300 | 1.2 | 1,100 |
10. D-Tic-c[Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 | 16,000 | 1.4 | 11,300 |
vs[3H]DADLE.
vs[3H]naloxone.
Abbreviations: DADLE, [D-Ala2,D-Leu5]enkephalin; DPDPE, c[D-Pen2,D-Pen5]enkephalin.