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. Author manuscript; available in PMC: 2016 Oct 25.
Published in final edited form as: Annu Rev Pharmacol Toxicol. 2013;53:557–580. doi: 10.1146/annurev-pharmtox-010510-100456

Table 4.

Binding affinity assays of somatostatin-like analogs with opioid receptors

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
a

vs[3H]DADLE.

b

vs[3H]naloxone.

Abbreviations: DADLE, [D-Ala2,D-Leu5]enkephalin; DPDPE, c[D-Pen2,D-Pen5]enkephalin.