Table 1.
Multiple effects of NOP receptor-related ligands on regulating pain processing.
| NOP receptor-related ligands | Findings in rodents | Findings in primates |
|---|---|---|
| NOP Receptor Agonists (Peptides) | ||
| N/OFQ | Spinal, Acute pain ↓ (Xu et al., 1996) (Erb et al., 1997) (King et al., 1997) (Yamamoto et al., 1997a) |
Spinal, Acute pain ↓ (Ko et al., 2006) (Ko & Naughton, 2009) |
| Spinal, Acute pain ↑ (Inoue et al., 1999) (Sakurada et al., 1999) |
||
| Spinal, Inflammatory pain ↓ (Yamamoto et al., 1997b) (Hao et al., 1998) (Chen & Sommer, 2007) |
||
| Spinal, Neuropathic pain ↓ (Yamamoto & Nozaki-Taguchi, 1997) (Corradini et al., 2001) (Courteix et al., 2004) |
||
| Supraspinal, Acute pain ↑ (Meunier et al., 1995) (Reinscheid et al., 1995) |
Supraspinal, Acute pain ↓ (Ding et al., 2015b) |
|
| Supraspinal, Inflammatory pain ↑ (Zhu et al., 1997) (Wang et al., 1999a) |
||
| [Phe1ψ(CH2-NH)Gly2]N/OFQ-(1–13)-NH2 | Supraspinal, Acute pain ↑ (Calo et al., 1998) (Wang et al., 1999b) |
|
| Supraspinal, Inflammatory pain ↑ (Bertorelli et al., 1999) |
||
| UFP-112 | Spinal, Acute pain ↓ (Rizzi et al., 2007) (Calo et al., 2011) |
Spinal, Acute pain ↓ (Hu et al., 2010) |
| Spinal, Capsaicin-induced allodynia ↓ (Hu et al., 2010) |
||
| PWT2-N/OFQ | Spinal, Acute pain ↓ (Rizzi et al., 2015) |
Spinal, Acute pain ↓ (Rizzi et al., 2015) |
| Spinal, Neuropathic pain ↓ (Rizzi et al., 2015) |
||
| NOP Receptor Agonists (Non-peptides) | ||
| Ro64-6198 | Spinal, Neuropathic pain ↓ (Obara et al., 2005) |
|
| Systemic, Acute pain ↓ (Reiss et al., 2008) |
Systemic, Acute pain ↓ (Ko et al., 2009) |
|
| Systemic, Acute pain ↑ (Reiss et al., 2008) |
Systemic, Inflammatory pain ↓ (Sukhtankar et al., 2014) |
|
| Systemic, Capsaicin-induced allodynia ↓ (Ko et al., 2009) |
||
| Ro65-6570 | Supraspinal, Neuropathic pain ↓ (Schiene et al., 2013) |
|
| Systemic, Inflammatory pain ↓ (Schiene et al., 2013) |
||
| Supraspinal, Neuropathic pain ↓ (Schiene et al., 2013) |
||
| GRT-TA2210 | Supraspinal, Neuropathic pain ↓ (Linz et al., 2013) |
|
| Systemic, Inflammatory pain ↓ (Linz et al., 2013) ` |
||
| SCH 221510 | Systemic, Inflammatory pain ↓ (Sobczak et al., 2013) (Sobczak et al., 2014) |
Systemic, Acute pain ↓ (Cremeans et al., 2012) |
| Systemic, Inflammatory pain ↓ (Wladischkin et al., 2012) |
||
| Systemic, Capsaicin-induced allodynia ↓ (Wladischkin et al., 2012) |
||
| NOP Receptor Antagonist | ||
| UFP-101 | Supraspinal, Acute pain ↓ (Rizzi et al., 2006) |
|
| Supraspinal, Inflammatory pain ↓ (Scoto et al., 2009) |
||
| Supraspinal, Neuropathic pain ↓ (Scoto et al., 2009) |
||
| Mixed NOP/MOP Receptor Agonists | ||
| [Dmt1]N/OFQ(1–13)-NH2 | Spinal, Acute pain ↓ (Calo et al., 2012) |
Spinal, Acute pain ↓ (Molinari et al., 2013) |
| SR16435 | Spinal, Inflammatory pain ↓ (Sukhtankar et al., 2013) |
|
| Spinal, Neuropathic pain ↓ (Sukhtankar et al., 2013) |
||
| Systemic, Acute pain ↓ (Khroyan et al., 2009) |
||
| SR14150 | Systemic, Neuropathic pain ↓ (Khroyan et al., 2011b) |
|
| SR16835 | Systemic, Neuropathic pain ↓ (Khroyan et al., 2011b) |
|
| BU08028 | Spinal, Inflammatory pain ↓ (Sukhtankar et al., 2013) |
|
| Spinal, Neuropathic pain ↓ (Sukhtankar et al., 2013) |
||
| Systemic, Acute pain ↓ (Khroyan et al., 2011a) |
Systemic, Acute pain ↓ (Ding et al., 2015a) |
|
| Systemic, Capsaicin-induced allodynia ↓ (Ding et al., 2015a) |
||
| Cebranopadol | Systemic, Acute pain ↓ (Linz et al., 2014) |
|
| Systemic, Inflammatory pain ↓ (Linz et al., 2014) |
||
| Systemic, Neuropathic pain ↓ (Linz et al., 2014) |
||
↓, antinociception or antihypersensitivity; ↑, pronociception or hypersensitivity