In vitro effects of N/OFQ and UFP-102 at recombinant and native NOP receptors
Data are the mean ± S.E.M. of at least four experiments. Maximal effects were expressed as stimulation factor (binding of [-35S]GTPγS in the presence of ligand divided by that under basal conditions) in [-35S]GTPγS experiments, as percentage inhibition of forskolin-stimulated response in cAMP studies, as percentage inhibition of control twitch in mouse and rat vas deferens and guinea pig ileum experiments, as percentage of 10 μM carbachol-induced contraction in mouse colon studies, and as percentage of K+ -evoked 5-HT overflow in mouse cerebral cortex synaptosomes studies.
N/OFQ | UFP-102 | CR | |||||
|---|---|---|---|---|---|---|---|
| pEC50 (CL95%) | Emax | pEC50 (CL95%) | Emax | ||||
| GTPγ[35S]/CHOhNOP | 8.70 | 10.71 ± 0.73 | 10.12 | 12.26 ± 0.39 | 26 | ||
| (8.51-8.89) | (10.0-10.24) | ||||||
| cAMP/CHOhNOP | 9.86 | -103 ± 1% | 10.17 | -104 ± 1% | 2 | ||
| (9.43-10.28) | (9.93-10.41) | ||||||
| Mouse vas deferens | 7.76 | -88 ± 3% | 9.44 | -92 ± 3% | 48 | ||
| (7.65-7.87) | (9.28-9.60) | ||||||
| Guinea pig ileum | 7.94 | -69 ± 7% | 9.24 | -65 ± 7% | 20 | ||
| (7.70-8.18) | (9.09-9.39) | ||||||
| Rat vas deferens | 7.24 | -83 ± 3% | 8.57 | -85 ± 2% | 21 | ||
| (7.11-7.37) | (8.40-8.74) | ||||||
| Mouse colon | 8.92 | 54 ± 4% | 9.19 | 61 ± 7% | 2 | ||
| (8.71-9.13) | (8.84-9.54) | ||||||
| Mouse cerebral cortex synaptosomes | 8.64 | 66 ± 3% | 9.42 | 67 ± 4% | 7 | ||
|
| (8.35-8.68) |
| (9.22-9.50) |
|
| ||
CR, concentration ratio.