Anti-nociceptive and anti-allodynic effects of a high affinity NOP hexapeptide [Ac-RY(3-Cl)YRWR-NH2] (Syn 1020) in rodents.

摘要: There has been a flurry of activity to develop agonists and antagonists for the member opioid receptor family, NOP (also known as ORL1), in part understand its role pain. Modifications hexapeptide originally identified from combinatorial library have led discovery high affinity agonist Ac-RY(3-Cl)YRWR-NH2 (Syn 1020). In following experiments we characterized anti-nociceptive effects Syn 1020 tail-flick model acute pain diabetic neuropathy chronic mice rats, respectively. Acute antinociception was assessed using assay which animals received intracerebroventricular (i.c.v.) or subcutaneous (s.c.) injections alone with morphine were tested latencies. model, induced by streptozotocin rats. Tactile allodynia measured, von Frey hair filaments, intraperitoneal (i.p.) gabapentin (positive control). mice, i.c.v. did not any pro- effects, however, reversed similar potency N/OFQ (the natural ligand NOP). S.c. also produced analgesic effects. i.p, anti-allodynic Thus, 1020, directed peptide, administered systemically both models rats