In vitro pharmacological profile of NOP selective agonists
| human NOP | rodent NOP | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| receptor binding | NOP/G-protein | [35S]GTPγS | Ca2+ mobilization | mVD | rVD | |||||||
| pKi | Selectivity | pEC50 | α | pEC50 | α | pEC50 | α | pEC50 | α | pEC50 | α | |
| N/OFQ | 9.91a | >1000 | 8.44b | 1.00 | 8.75a | 1.00 | 9.54c | 1.00 | 7.47d | 1.00 | 6.83e | 1.00 |
| N/OFQ(1-13)-NH2 | 10.24a | 276 | 8.46b | 1.00 | 9.28a | 0.86 | 9.30c | 0.96 | 7.40f | 1.01 | 6.90f | 0.99 |
| UFP-112 | 10.55e | >1000 | 9.35b | 0.98 | 10.55e | 1.03 | 9.05c | 1.04 | 9.24d | 0.97 | 8.34e | 1.14 |
| PWT2-N/OFQ | 10.30g | >1000 | 9.17b | 1.10 | 10.12g | 1.14 | 8.83g | 0.98 | 7.92g | 0.99 | 7.23h | 1.03 |
| [F/G] | 8.00i | 67 | 7.85b | 0.72 | 8.05j | 0.67 | 8.03c | 0.54 | slight transient effect pA2 6.75f | Inactive pA2 6.83f | ||
| UFP-113 | 10.26e | >500 | 9.35b | 0.45 | 9.72e | 0.79 | 7.97c | 0.62 | variable agonist effects pA2 9.10e | variable agonist effects pA2 9.22e | ||
| Ac-RYYRWK-NH2 | 9.01l | >1000 | 8.76h | 0.78 | 8.67l | 0.57 | 8.68c | 0.58 | 8.07m | 0.71 | 7.93h | 0.78 |
| Ro 64-6198 | 9.41n | >100 | 7.76h | 1.01 | 8.09a | 0.89 | 7.98c | 1.07 | 6.84° | 1.05 | 7.24° | 0.95 |
| Ro 65-6570 | 8.25p | 10 | 7.77b | 0.96 | 7.73h | 1.01 | 7.95q | 1.05 | 6.80q | 1.15 | 7.11q | 1.0 |
a (McDonald et al., 2003b), b (Malfacini et al., 2014), c (Camarda et al., 2009), d (Rizzi et al., 2007c), e (Arduin et al., 2007a), f (Bigoni et al., 1999), g (Rizzi et al., 2014), h unpublished results, i(Varani et al., 1999), J (Wright et al., 2003), l (Dooley et al., 1997), m (Rizzi et al., 2002a), n (Jenck et al., 2000), o (Rizzi et al., 2001c), p (Hashiba et al., 2001), q (Molinari et al., 2012), r (Varty et al., 2008). α is the ratio between the Emax of the agonist and the Emax of N/OFQ.