Binding affinities of delta compounds to WT and mutant delta receptors Competition experiments were carried out on HEK 293 cell membrane preparations expressing receptors either stably (WT, M262T, C328R) or transiently (Y308H) and using variable concentrations of unlabeled ligands to displace [3H]diprenorphine. Data are means ± S.E.M. from n experiments performed in triplicate (Kd) or in duplicate (Ki) using at least two different membrane preparations.
Compounds | WT | M262T | Y308H | C328R | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ki | n | Ki | n | Ki | n | Ki | n | |||||
| nM | nM | nM | nM | |||||||||
| [3H]Diprenorphine (Kd) | 0.39 ± 0.06 | 2 | 0.72 ± 0.21 | 2 | 8.00 ± 1.22 | 5 | 0.44 ± 0.06 | 3 | ||||
| SNC 80 | 9.41 ± 3.07 | 3 | 9.62 ± 2.59 | 3 | 438 ± 21 | 5 | 5.73 ± 1.84 | 4 | ||||
| ICI 174864 | 434 ± 61 | 4 | 1308 ± 247 | 3 | >4800 | 2 | 567 ± 53 | 6 | ||||
| NLX | 66.20 ± 0.71 | 3 | 59.11 ± 2.92 | 2 | ||||||||
| NTI | 0.30 ± 0.15 | 3 | 0.12 ± 0.02 | 3 | ||||||||
| BNTX | 3.22 ± 0.58 | 3 | 6.10 ± 1.48 | 3 | ||||||||
| NTB | 0.10 ± 0.02 | 3 | 0.23 ± 0.04 | 3 | ||||||||
| TIPP | 2.90 ± 0.66 | 3 | 7.03 ± 3.05 | 3 | ||||||||
| TICP[ψ] | 4.62 ± 0.64 | 3 | 3.91 ± 0.27 | 3 | 21.82 ± 1.53 | 4 | 7.20 ± 1.14 | 6 | ||||
| H-Dmt-Tic-OH | 13.13 ± 1.71 | 3 | 5.20 ± 1.85 | 3 | 200 ± 7 | 4 | 13.74 ± 4.12 | 7 | ||||
| H-Dmt-Tic-NH2 | 9.41 ± 1.13 | 3 | 9.43 ± 1.16 | 3 | ||||||||
| N,N(CH3)2-Dmt-Tic-NH2 | 2.50 ± 0.76 | 3 | 1.81 ± 0.66 | 3 | 18.23 ± 3.48 | 4 | 1.90 ± 0.41 | 4 | ||||
| HS-378 | 0.40 ± 0.01 | 2 | 0.90 ± 0.03 | 3 | ||||||||
| HS-414 | 2.10 ± 0.72 | 3 | 4.13 ± 1.04 | 3 | ||||||||
| HS-464 | 0.11 ± 0.03 | 3 | 0.40 ± 0.09 | 3 | ||||||||
| HS-510A | 0.12 ± 0.03 | 3 | 0.41 ± 0.15 | 3 | ||||||||
| HS-531 | 0.42 ± 0.08 | 2 | 0.80 ± 0.09 | 2 | ||||||||
| HS-595 | 0.22 ± 0.01 | 2 | 0.41 ± 0.05 | 2 |
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