Nociceptin receptor

Next to these three classical receptor families a additional opioid receptor has been identified. This receptor is known as the nociceptin receptor or ORL 1 receptor. Its natural ligand is known... 

Dautzenberg, F.M., Wichmann, J., Higelin, J., Py-Lang, G., Kratzeisen, C., Malherbe, P., Kilpatrick, G.J., Jenck, F. Pharmacological characterization of the novel nonpetide orphanin FQ / nociceptin receptor agonist Ro 64-6198 Rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance in vivo, J. Pharmacol. Exp. Ther. 2001, 298, 812-819. 

Kyle, D., Goehring, R.R., Shao, B. (Euroceltique) Benzimidazole compounds having nociceptin receptor affinity, WO0139775 (2001). 

Manabe, T., Noda, Y., Mamiya, T., Katagiri, H., Houtani, T., Nishi, M., Noda, T., Takahashi, T., Sugimoto, T., Nabeshima, T., Takeshima, H. Facilitation of long-term potentiation and memory in mice lacking nociceptin receptors. Nature 1998, 394, 577-581. 

Meunier, J.-C. The potential therapeutic value of nociceptin receptor agonists and antagonists, Exp. Opin. Ther. Patents 2000, 10, 371-388. 

Thomsen, C. and Hohlweg, R. (8-Naphthalen-1-ylmethyl-4-oxo-1-phenyl-1,3,8-triaza-spiro[4.5]dec-3-yl)-acetic acid methyl ester (NNC 63-0532) is a novel potent nociceptin receptor agonist, Br. J. Pharmacol. 2000, 131, 903-908. 

Ueda, H., Yamaguchi, T., Tokuyama, S., Inoue, M., Nishi, M., Takeshima, H. Partial loss of tolerance liability to morphine analgesia in mice lacking the nociceptin receptor gene, Neuroscience Lett. 1997, 237, 136-138. 

Varani K, Calo G, Rizzi A, Merighi S, Toth G, Guerrini R, Salvadori S, Borea PA, Regoli D (1998) Nociceptin receptor binding in mouse forebrain membranes thermodynamic characteristics and structure activity relationships. Br J Pharmacol 125(7) 1485-1490... 

Guerrini R, Calo G, Rizzi A et al (1998) A new selective antagonist of the nociceptin receptor. Brit J Pharmacol 123 163-5... 

Bigoni R, Guiliani S, Cato G et at. (1999) Characterization of nociceptin receptors in the periphery In vitro and in vivo studies. Naunyn-Schmiedeberg s Arch Pharmacol 359 160-167... 

Nociceptin (orphanin FQ) is a novel neuropeptide whose actions have yet to be completely elucidated. However, stimulation of the nociceptin receptor has been implicated in the modulation of many neurobehavioral processes, including pain, substance dependence, sexual behavior, anxiety, locomotor activity, learning capacity, memory, and adaptation to stressful stimulus [1-6]. Continued research in this area has the potential to lead to a new class of drugs for pain medicine and beyond. 

Syntheses and structure-activity reiationships of 3-di-substituted 8-benzhydryi-nortropane anaiogs as nociceptin receptor iigands... 

Recently, it has been demonstrated that the fear gene, oprll, that produces the nociceptine receptor, is involved in post-traumatic stress. Laboratory assays prove that nociceptine and its agonist molecules, that stimulate this receptor. 

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