|
Inhibitory concentrations 50% (IC50) ± SE of receptorphin competition on different opioid sites, assayed by displacement binding of a variety of opioid ligands. |
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| Opioid Source |
DPDPE or DSLET |
DAGO |
EKC |
Diprenorphin |
EKC +DADLE |
Diprenorphin +DADLE |
|
|
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| MCF7 |
3.25 ± 0.42 × 10-9 |
1.43 ± 0.20 × 10-10 |
6.65 ± 1.01 × 10-11 |
5.78 ± 0.64 × 10-13 |
1.59 ± 0.14 × 10-10 |
>10-12 |
| T47D |
ND |
ND |
5.14 ± 0.74 × 10-10 |
>10-12 |
5.41 ± 0.57 × 10-11 |
>10-12 |
| DU145 |
ND |
6.52 ± 0.58 × 10-11 |
2.34 ± 0.55 × 10-11 |
ND |
2.87 ± 0.22 × 10-11 |
ND |
| PC3 |
ND |
4.30 ± 0.97 × 10-11 |
>10-6 |
ND |
>10-6 |
ND |
| Rat |
8.25 ± 0.81 × 10-8 |
1.81 ± 0.23 × 10-7 |
*1.85 ± 0.11 × 10-10 |
**5.77 ± 0.87 × 10-10 |
- |
1.85 ± 0.43 × 10-10 |
| Brain |
2.65 ± 0.13 × 10-9 |
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|
*[3H]U60-593 was used as a selective kappa1 opioid ligand **Displacement curves were best fitted with a two-site model. See text for details. IC50s (in Moles/L) were calculated by sigmoidal fitting of displacement experiments. ND = not detected. Mean ± SE of three different experiments performed in duplicate. | ||||||
Kampa et al. BMC Pharmacology 2001 1:9 doi:10.1186/1471-2210-1-9 |
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