Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: Research tools and potential therapeutic agents

Life Sciences

Volumn 73, Issue 6, 2003, Pages 663-678

  Zaveri, Nurulain ^a  

^a SRI INTERNATIONAL   (United States)

Author keywords

Analgesia; Anxiety; Nociceptin; Nociceptin analog; ORL1; ORL1 agonist; ORL1 antagonist; ORL1 ligands; Orphanin FQ; Piperidines

Indexed keywords

1 (1 CYCLOOCTYLMETHYL 3 HYDROXYMETHYL 4 PIPERIDYL) 3 ETHYL 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; ANILIDOPIPERIDINE; BUPRENORPHINE; ETORPHINE; FENTANYL DERIVATIVE; LOFENTANIL; MORPHINAN DERIVATIVE; MORPHINAN NALOXONE BENZOYLHYDRAZONE; N (4 AMINO 2 METHYL 6 QUINOLINYL) 2 (4 ETHYLPHENOXYMETHYL)BENZAMIDE; NALFURAFINE; NNC 630532; NOCICEPTIN RECEPTOR; OPIATE AGONIST; OPIATE ANTAGONIST; ORIPAVINE; PENTOXYVERINE; PIMOZIDE; RIMCAZOLE; RO 646198; RO 656570; SPIROXATRINE; UFP 101; UNCLASSIFIED DRUG;

AGONIST; AMIDATION; AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; ANALGESIC ACTIVITY; ANTINOCICEPTION; CHO CELL; CONFERENCE PAPER; DRUG POTENCY; IC 50; STRUCTURE ACTIVITY RELATION;

EID: 0037498440     PISSN: 00243205     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0024-3205(03)00387-4     Document Type: Conference Paper

References (114)

1. Adam, G., Cesura, A.M., Galley, G., Jenck, F., Monsama, F., Rover, S., Wichmann, J., 1998. New 8-substituted 1,3,8-triazaspiro[4,5]decan-4-one derivatives. European Patent. EP 0856514. Hoffmann-La Roche.
2. Adam, G., Dautzenberg, F.M., Kolczewski, S., Rover, S., Wichmann, J., 2000a. Spiro[piperidine-4,1′-pyrrolo[3,4-C]pyrrole] derivatives. United States Patent. US 6075034. Hoffmann-La Roche, Nutley, N.J.
3. Adam, G., Cesura, A.M., Jenck, F., Kolczewski, S., Rover, S., Wichmann, J., 2000b. Diaza-spiro[3,5] nonane derivatives. United States Patent. US 6113527. Hoffmann-La Roche, Nutley, N.J.
4. Adam, G., Cesura, A.M., Galley, C., Jenck, F., Rover, S., Wichmann, J., 2000c. Piperidine derivatives. United States Patent. US 6166209. Hoffmann-La Roche, Nutley, N.J.
5. Ambo A., Hamazaki N., Yamada Y., Nakata E., Sasaki Y. Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nociceptin peptides. Journal of Medicinal Chemistry. 44:2001;4015-4018.
6. Barlocco, D., Cignarella, G., Giardina, G., Grugni, M., Ronzoni, S., 2000. Novel compounds. International PCT Application. WO 00/27815. SmithKline Beecham SPA.
7. Becker J.A., Wallace A., Garzon A., Ingallinella P., Bianchi E., Cortese R., Simonin F., Kieffer B.L., Pessi A. Ligands for kappa-opioid and ORL1 receptors identified from a conformationally constrained peptide combinatorial library. Journal of Biological Chemistry. 274:1999;27513-27522.
8. Berger H., Bigoni R., Albrecht E., Richter R.M., Krause E., Bienert M., Calo G. The nociceptin/orphanin FQ receptor ligand acetyl-RYYRIK-amide exhibits antagonistic and agonistic properties. Peptides. 21:2000;1131-1139.
9. Bigoni R., Giuliani S., Calo G., Rizzi A., Guerrini R., Salvadori S., Regoli D., Maggi C.A. Characterization of nociceptin receptors in the periphery: in vitro and in vivo studies. Naunyn Schmiedebergs Archives of Pharmacology. 359:1999;160-167.
10. Bigoni R., Rizzi A., Rizzi D., Becker J.A., Kieffer B.L., Simonin F., Regoli D., Calo G. In vitro pharmacological profile of peptide III-BTD: a novel ligand for nociceptin/orphanin FQ and opioid receptors. Life Sciences. 68:2000;233-239.
11. Bigoni R., Calo G., Rizzi A., Guerrini R., De Risi C., Hashimoto Y., Hashiba E., Lambert D.G., Regoli D. In vitro characterization of J-113397, a non-peptide nociceptin/orphanin FQ receptor antagonist. Naunyn Schmiedebergs Archives of Pharmacology. 361:2000;565-568.
12. Bigoni R., Rizzi D., Rizzi A., Camarda V., Guerrini R., Lambert D.G., Hashiba E., Berger H., Salvadori S., Regoli D., Calo G. Pharmacological characterisation of [(pX)Phe(4)]nociceptin(1-13)amide analogues1. In vitro studies. Naunyn Schmiedebergs Archives of Pharmacology. 365:2002;442-449.
13. Bigoni R., Cao G., Rizzi A., Okawa H., Regoli D., Smart D., Lambert D.G. Effects of naloxone benzoylhydrazone on native and recombinant nociceptin/orphanin FQ receptors. Canadian Journal of Physiology and Pharmacology. 80:2002;407-412.
14. Bunzow J.R., Saez C., Mortrud M., Bouvier C., Williams J.T., Low M., Grandy D.K. Molecular cloning and tissue distribution of a putative member of the rat opioid receptor gene family that is not a mu, delta or kappa opioid receptor type. FEBS Letters. 347:1994;284-288.
15. Burnside J.L., Rodriguez L., Toll L. Species differences in the efficacy of compounds at the nociceptin receptor (ORL1). Peptides. 21:2000;1147-1154.
16. Butour J.L., Moisand C., Mazarguil H., Mollereau C., Meunier J.C. Recognition and activation of the opioid receptor-like ORL 1 receptor by nociceptin, nociceptin analogs and opioids. European Journal of Pharmacology. 321:1997;97-103.
17. Calo G., Guerrini R., Bigoni R., Rizzi A., Bianchi C., Regoli D., Salvadori S. Structure-activity study of the nociceptin(1-13)-NH2 N-terminal tetrapeptide and discovery of a nociceptin receptor antagonist. Journal of Medicinal Chemistry. 41:1998;3360-3366.
18. Calo G., Guerrini R., Rizzi A., Salvadori S., Regoli D. Pharmacology of nociceptin and its receptor: a novel therapeutic target. British Journal of Pharmacology. 129:2000;1261-1283.
19. Calo G., Bigoni R., Rizzi A., Guerrini R., Salvadori S., Regoli D. Nociceptin/orphanin FQ receptor ligands. Peptides. 21:2000;935-947.
20. Calo G., Guerrini R., Bigoni R., Rizzi A., Marzola G., Okawa H., Bianchi C., Lambert D.G., Salvadori S., Regoli D. Characterization of [Nphe(1)]nociceptin(1-13)NH(2), a new selective nociceptin receptor antagonist. British Journal of Pharmacology. 129:2000;1183-1193.
21. Calo G., Rizzi A., Bigoni R., Guerrini R., Salvadori S., Regoli D. Pharmacological profile of nociceptin/orphanin FQ receptors. Clinical and Experimental Pharmacology and Physiology. 29:2002;223-228.
22. Calo G., Rizzi A., Rizzi D., Bigoni R., Guerrini R., Marzola G., Marti M., McDonald J., Morari M., Lambert D.G., Salvadori S., Regoli D. [Nphe(1),Arg(14),Lys(15)]nociceptin-NH(2), a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor. British Journal of Pharmacology. 136:2002;303-311.
23. Carpenter K.J., Dickenson A.H. Evidence that [Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord. British Journal of Pharmacology. 125:1998;949-951.
24. Cesura, A.M., Hoffmann, T., Rover, S., Wichmann, J., 2000. Piperidine derivatives. International PCT Application, WO 00/14067, Hoffmann-La Roche.
25. Chiou L.C., Fan S.H., Guerrini R., Calo G. [Nphe(1)]N/OFQ-(1-13)-NH(2) is a competitive and selective antagonist at nociceptin/orphanin FQ receptors mediating K(+) channel activation in rat periaqueductal gray slices. Neuropharmacology. 42:2002;246-252.
26. Chiou L.C., Fan S.H. CompB (J-113397), selectively and competitively antagonizes nociceptin activation of inwardly rectifying K(+) channels in rat periaqueductal gray slices. Neuropharmacology. 42:2002;987-992.
27. Chung K.F., Chang A.B. Therapy for cough: active agents. Pulmonary Pharmacology and Therapeutics. 15:2002;335-338.
28. Ciccocioppo R., Biondini M., Antonelli L., Wichmann J., Jenck F., Massi M. Reversal of stress- and CRF-induced anorexia in rats by the synthetic nociceptin/orphanin FQ receptor agonist, Ro 64-6198. Psychopharmacology (Berl). 161:2002;113-119.
29. Dautzenberg F.M., Wichmann J., Higelin J., Py-Lang G., Kratzeisen C., Malherbe P., Kilpatrick G.J., Jenck F. Pharmacological characterization of the novel nonpeptide orphanin FQ/nociceptin receptor agonist Ro 64-6198: rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance in vivo. Journal of Pharmacology and Experimental Therapeutics. 298:2001;812-819.
30. Di Giannuario A., Pieretti S., Catalani A., Loizzo A. Orphanin FQ reduces morphine-induced dopamine release in the nucleus accumbens: a microdialysis study in rats. Neuroscience Letters. 272:1999;183-186.
31. Di Giannuario A., Rizzi A., Pieretti S., Guerrini R., Bertorelli R., Salvadori S., Regoli D., Calo G. Studies on the antinociceptive effect of [Nphe1]nociceptin(1-13)NH2 in mice. Neuroscience Letters. 316:2001;25-28.
32. Dooley C.T., Houghten R.A. Orphanin FQ: receptor binding and analog structure activity relationships in rat brain. Life Sciences. 59:1996;L23-L29.
33. Dooley C.T., Spaeth C.G., Berzetei-Gurske I.P., Craymer K., Adapa I.D., Brandt S.R., Houghten R.A., Toll L. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. Journal of Pharmacology and Experimental Therapeutics. 283:1997;735-741.
34. Fukuda K., Kato S., Mori K., Nishi M., Takeshima H., Iwabe N., Miyata T., Houtani T., Sugimoto T. cDNA cloning and regional distribution of a novel member of the opioid receptor family. FEBS Letters. 343:1994;42-46.
35. Gistrak M.A., Paul D., Hahn E.F., Pasternak G.W. Pharmacological actions of a novel mixed opiate agonist/antagonist: naloxone benzoylhydrazone. Journal of Pharmacology and Experimental Therapeutics. 251:1989;469-476.
36. Griebel G., Perrault G., Sanger D.J. Orphanin FQ, a novel neuropeptide with anti-stress-like activity. Brain Research. 836:1999;221-224.
37. Grisel J.E., Farrier D.E., Wilson S.G., Mogil J.S. [Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 acts as an agonist of the orphanin FQ/nociceptin receptor in vivo. European Journal of Pharmacology. 357:1998;R1-R3.
38. Groneberg D.A., Fischer A. Endogenous opioids as mediators of asthma. Pulmonary Pharmacology and Therapeutics. 14:2001;383-389.
39. Guerrini R., Calo G., Rizzi A., Bianchi C., Lazarus L.H., Salvadori S., Temussi P.A., Regoli D. Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide. Journal of Medicinal Chemistry. 40:1997;1789-1793.
40. Guerrini R., Calo G., Rizzi A., Bigoni R., Bianchi C., Salvadori S., Regoli D. A new selective antagonist of the nociceptin receptor. British Journal of Pharmacology. 123:1998;163-165.
41. Guerrini R., Calo G., Bigoni R., Rizzi A., Varani K., Toth G., Gessi S., Hashiba E., Hashimoto Y., Lambert D.G., Borea P.A., Tomatis R., Salvadori S., Regoli D. Further studies on nociceptin-related peptides: discovery of a new chemical template with antagonist activity on the nociceptin receptor. Journal of Medicinal Chemistry. 43:2000;2805-2813.
42. Guerrini R., Calo G., Bigoni R., Rizzi D., Rizzi A., Zucchini M., Varani K., Hashiba E., Lambert D.G., Toth G., Borea P.A., Salvadori S., Regoli D. Structure-activity studies of the Phe(4) residue of nociceptin(1-13)-NH(2): identification of highly potent agonists of the nociceptin/orphanin FQ receptor. Journal of Medicinal Chemistry. 44:2001;3956-3964.
43. Hashiba E., Harrison C., Galo G., Guerrini R., Rowbotham D.J., Smith G., Lambert D.G. Characterisation and comparison of novel ligands for the nociceptin/orphanin FQ receptor. Naunyn Schmiedebergs Archives of Pharmacology. 363:2001;28-33.
44. Hashiba E., Lambert D.G., Jenck F., Wichmann J., Smith G. Characterisation of the non-peptide nociceptin receptor agonist, Ro64-6198 in Chinese hamster ovary cells expressing recombinant human nociceptin receptors. Life Sciences. 70:2002;1719-1725.
45. Hashimoto Y., Calo G., Guerrini R., Smith G., Lambert D.G. Antagonistic effects of [Nphe1]nociceptin(1-13)NH2 on nociceptin receptor mediated inhibition of cAMP formation in Chinese hamster ovary cells stably expressing the recombinant human nociceptin receptor. Neuroscience Letters. 278:2000;109-112.
46. Hawkinson J.E., Acosta-Burruel M., Espitia S.A. Opioid activity profiles indicate similarities between the nociceptin/orphanin FQ and opioid receptors. European Journal of Pharmacology. 389:2000;107-114.
47. Hohlweg, R., Watson, B., Thomsen, C., 2001. 1,3,8-Triazaspiro[4,5]decanones with high affinity for opioid receptor subtypes. United States Patent. US 6277991. Novo Nordisk A/S.
48. Ichikawa D., Ozaki S., Azuma T., Nambu H., Kawamoto H., Iwasawa Y., Takeshima H., Ohta H. In vitro inhibitory effects of J-113397 on nociceptin/orphanin FQ-stimulated. Neuroreport. 12:2001;1757-1761.
49. Ito, F., 1998. Morphinan hydroxamic acid compounds. United States Patent. US 5834478 Pfizer, Inc.
50. Ito, F., 2002. 2-Benzimidazolylamine compounds as ORL-1 receptor agonists. United States Patent. US 6340681 B1. Pfizer, Inc.
51. Ito, F., Ohashi, Y., 2000. 1,3,8-Triazaspiro[4,5]decanone compounds as ORL1-receptor agonists. European Patent Application, EP 0997464 A1. Pfizer, Inc.
52. Ito, F., Noguchi, H., Ohashi, Y., Kondo, H., Yamagishi, T., 1999. 4-(2-Keto-1-benzimidazolinyl)piperidine compounds as ORL1-receptor agonists. International Patent. WO 99/36421. Pfizer, Inc.
53. Ito, F., Noguchi, H., Kondo, H., 2001a. 2-Substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists. United States Patent. US 6172067 B1. Pfizer, Inc.
54. Ito, F., Noguchi, H., Ohashi, Y., Shimokawa, H., 2001b. Benzimidazole compounds as ORL-1 receptor agonists. European Patent Application. EP 1122257 A1. Pfizer, Inc.
55. Jenck F., Moreau J.L., Martin J.R., Kilpatrick G.J., Reinscheid R.K., Monsma F.J. Jr., Nothacker H.P., Civelli O. Orphanin FQ acts as an anxiolytic to attenuate behavioral responses to stress. Proceedings of the National Academy of Sciences U. S. A. 94:1997;14854-14858.
56. Jenck F., Wichmann J., Dautzenberg F.M., Moreau J.L., Ouagazzal A.M., Martin J.R., Lundstrom K., Cesura A.M., Poli S.M., Roever S., Kolczewski S., Adam G., Kilpatrick G. A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat. Proceedings of the National Academy of Sciences U. S. A. 97:2000;4938-4943.
57. Jinsmaa Y., Takahashi M., Fukunaga H., Yoshikawa M. Retro-nociceptin methylester, a peptide with analgesic and memory-enhancing activity. Life Sciences. 67:2000;3095-3101.
58. Kapusta D.R., Calo G., Kenigs V.A. Peripheral administration of partial agonists of the nociceptin/orphanin FQ peptide (NOP) receptor produce water diuresis in conscious rats. FASEB Journal. 16:2002;A841.
59. Kapusta D.R., Kenigs V.A., Vinge M.M., Hansen C., Meier E., Thokildsen C., Petersen J.S. ZP120C is a peripherally acting nociceptin/orphanin FQ (N/OFQ) analogue with water diuretic and potassium sparing properties. FASEB Journal. 16:2002;A841.
60. Kawamoto H., Ozaki S., Itoh Y., Miyaji M., Arai S., Nakashima H., Kato T., Ohta H., Iwasawa Y. Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397). Journal of Medicinal Chemistry. 42:1999;5061-5063.
61. Kawamoto, H., Ozaki, S., Ito, Y., Iwazawa, Z., 2000. 4-Oxoimidazolidine-5-spiro-nitrogen-containing heterocyclic compound. Patent Abstracts of Japan. Application. JP 2000169476. Banyu Pharmaceutical Co. (Japan).
62. Kobayashi T., Ikeda K., Togashi S., Itoh N., Kumanishi T. Effects of sigma ligands on the nociceptin/orphanin FQ receptor co-expressed with the G-protein-activated K+ channel in Xenopus oocytes. British Journal of Pharmacology. 120:1997;986-987.
63. Kotlinska J., Wichmann J., Legowska A., Rolka K., Silberring J. Orphanin FQ/nociceptin but not Ro 65-6570 inhibits the expression of cocaine-induced conditioned place preference. Behavioural Pharmacology. 13:2002;229-235.
64. Kyle, D., Goehring, R.R., Shao, B., 2001. Benzimidazole compounds having nociceptin receptor affinity. International PCT Application. WO 01/39775 A1. EuroCeltique, S. A. (Luxembourg).
65. Kyuhou S., Gemba H. Injection of orphanin FQ/nociceptin into the periaqueductal gray suppresses the forebrain-elicited vocalization in the guinea pig. Neuroscience Letters. 260:1999;113-116.
66. Larsen, B.D., 1999. Pharmacologically active peptide conjugates having a reduced tendency towards enzymatic hydrolysis. International Patent. WO 99/46283.
67. Larsen, B.D., 2001. Novel peptide conjugates. International Patent. WO 01/98324.
68. 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. 394:1998;577-581.
69. McDonald J., Barnes T.A., Calo G., Guerrini R., Rowbotham D.J., Lambert D.G. Effects of [(pF)Phe(4)]nociceptin/orphanin FQ-(1-13)NH(2) on GTPgamma35S binding and cAMP formation in Chinese hamster ovary cells expressing the human nociceptin/orphanin FQ receptor. European Journal of Pharmacology. 443:2002;7-12.
70. Meunier J.C., Mollereau C., Toll L., Suaudeau C., Moisand C., Alvinerie P., Butour J.L., Guillemot J.C., Ferrara P., Monsarrat B., Mazarguil H., Vassart G., Parmentier M., Constentin J. Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor. Nature. 377:1995;532-535.
71. Meunier J.C. Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor. European Journal of Pharmacology. 340:1997;1-15.
72. Mogil J.S., Grisel J.E., Reinscheid R.K., Civelli O., Belknap J.K., Grandy D.K. Orphanin FQ is a functional anti-opioid peptide. Neuroscience. 75:1996;333-337.
73. Mollereau C., Mouledous L. Tissue distribution of the opioid receptor-like (ORL1) receptor. Peptides. 21:2000;907-917.
74. Mollereau C., Parmentier M., Mailleux P., Butour J.L., Moisand C., Chalon P., Caput D., Vassart G., Meunier J.C. ORL1, a novel member of the opioid receptor family. Cloning, functional expression and localization. FEBS Letters. 341:1994;33-38.
75. Murphy N.P., Ly H.T., Maidment N.T. Intracerebroventricular orphanin FQ/nociceptin suppresses dopamine release in the nucleus accumbens of anaesthetized rats. Neuroscience. 75:1996;1-4.
76. Murphy N.P., Lee Y., Maidment N.T. Orphanin FQ/nociceptin blocks acquisition of morphine place preference. Brain Research. 832:1999;168-170.
77. Noda Y., Mamiya T., Nabeshima T., Nishi M., Higashioka M., Takeshima H. Loss of antinociception induced by naloxone benzoylhydrazone in nociceptin receptor-knockout mice. Journal of Biological Chemistry. 273:1998;18047-18051.
78. Okada K., Sujaku T., Chuman Y., Nakashima R., Nose T., Costa T., Yamada Y., Yokoyama M., Nagahisa A., Shimohigashi Y. Highly potent nociceptin analog containing the Arg-Lys triple repeat. Biochemical and Biophysical Research Communications. 278:2000;493-498.
79. Ozaki, S., Kawamoto, H., Ito, Y., Hayashi, K., Iwasawa, Y., Hirano, K., 1998. New 2-oxoimidazole derivatives are nociceptin receptor binding inhibitors useful, e.g. as analgesics and for ameliorating brain function. International Patent. WO 98/54168-A1. Banyu Pharmaceutical Co.
80. Ozaki S., Kawamoto H., Itoh Y., Miyaji M., Iwasawa Y., Ohta H. A potent and highly selective nonpeptidyl nociceptin/orphanin FQ receptor (ORL1) antagonist: J-113397. European Journal of Pharmacology. 387:2000;R17-R18.
81. Ozaki S., Kawamoto H., Itoh Y., Miyaji M., Azuma T., Ichikawa D., Nambu H., Iguchi T., Iwasawa Y., Ohta H. In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. European Journal of Pharmacology. 402:2000;45-53.
82. Ozaki, S., Kawamoto, H., Ito, Y., Hirano, K., Hayashi, K., Iwasawa, Y., 2001. 2-Oxoimidazole derivatives. United States Patent. US 6258825 B1. Banyu Pharmaceutical Co.
83. Polidori C., Calo G., Ciccocioppo R., Guerrini R., Regoli D., Massi M. Pharmacological characterization of the nociceptin receptor mediating hyperphagia: identification of a selective antagonist. Psychopharmacology (Berl). 148:2000;430-437.
84. Pomonis J.D., Billington C.J., Levine A.S. Orphanin FQ, agonist of orphan opioid receptor ORL1, stimulates feeding in rats. Neuroreport. 8:1996;369-371.
85. Redrobe J.P., Calo G., Guerrini R., Regoli D., Quirion R. [Nphe(1)]-Nociceptin (1-13)-NH(2), a nociceptin receptor antagonist, reverses nociceptin-induced spatial memory impairments in the Morris water maze task in rats. British Journal of Pharmacology. 131:2000;1379-1384.
86. Reinscheid R.K., Nothacker H.P., Bourson A., Ardati A., Henningsen R.A., Bunzow J.R., Grandy D.K., Langen H., Monsma F.J. Jr., Civelli O. Orphanin FQ: a neuropeptide that activates an opioidlike G protein-coupled receptor. Science. 270:1995;792-794.
87. Reinscheid R.K., Ardati A., Monsma F.J. Jr., Civelli O. Structure-activity relationship studies on the novel neuropeptide orphanin FQ. Journal of Biological Chemistry. 271:1996;14163-14168.
88. Rizzi A., Bigoni R., Marzola G., Guerrini R., Salvadori S., Regoli D., Calo G. The nociceptin/orphanin FQ receptor antagonist, [Nphe1]NC(1-13)NH2, potentiates morphine analgesia. Neuroreport. 11:2000;2369-2372.
89. Rizzi A., Bigoni R., Marzola G., Guerrini R., Salvadori S., Regoli D., Calo G. Characterization of the locomotor activity-inhibiting effect of nociceptin/orphanin FQ in mice. Naunyn Schmiedebergs Archives of Pharmacology. 363:2001;161-165.
90. Rizzi D., Bigoni R., Rizzi A., Jenck F., Wichmann J., Guerrini R., Regoli D., Calo G. Effects of Ro 64-6198 in nociceptin/orphanin FQ-sensitive isolated tissues. Naunyn Schmiedebergs Archives of Pharmacology. 363:2001;551-555.
91. Rizzi D., Rizzi A., Bigoni R., Camarda V., Marzola G., Guerrini R., De Risi C., Regoli D., Calo G. [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. Journal of Pharmacology and Experimental Therapeutics. 300:2002;57-63.
92. Rizzi A., Salis B., Ciccocioppo R., Marzola G., Bigoni R., Guerrini R., Massi M., Madeddu P., Salvadori S., Regoli D., Calo G. Pharmacological characterisation of [(pX)Phe(4)]nociceptin(1-13)NH(2) analogues2. In vivo studies. Naunyn Schmiedebergs Archives of Pharmacology. 365:2002;450-456.
93. Rizzi A., Rizzi D., Marzola G., Regoli D., Larsen B.D., Petersen J.S., Calo G. Pharmacological characterization of the novel nociceptin/orphanin FQ receptor ligand, ZP120: in vitro and in vivo studies in mice. British Journal of Pharmacology. 137:2002;369-374.
94. Rover S., Adam G., Cesura A.M., Galley G., Jenck F., Monsma F.J. Jr., Wichmann J., Dautzenberg F.M. High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor. Journal of Medicinal Chemistry. 43:2000;1329-1338.
95. Rover S., Wichmann J., Jenck F., Adam G., Cesura A.M. ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl- 1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones. Bioorganic and Medicinal Chemistry Letters. 10:2000;831-834.
96. Sandin J., Georgieva J., Schott P.A., Ogren S.O., Terenius L. Nociceptin/orphanin FQ microinjected into hippocampus impairs spatial learning in rats. European Journal of Neuroscience. 9:1997;194-197.
97. Satoh, A., Kawamoto, H., Ozaki, S., Ito, Y., Iwasawa, Y., 2000. 4-Oxoimidazolidine-2-spiro-nitrogenous heterocyclic compounds. International Patent. WO 00/34280. Banyu Pharmaceutical Co.
98. Satoh, A., Kato, T., Iwasawa, Y., Ooi, N., 2001. 4-Oxoimidazolidine-2-spiro-nitrogenous heterocyclic compounds. International Patent. WO 01/96337. Banyu Pharmaceutical Co.
99. Schlicker E., Morari M. Nociceptin/orphanin FQ and neurotransmitter release in the central nervous system. Peptides. 21:2000;1023-1029.
100. Seki T., Awamura S., Kimura C., Ide S., Sakano K., Minami M., Nagase H., Satoh M. Pharmacological properties of TRK-820 on cloned mu-, delta- and kappa- opioid receptors and nociceptin receptor. European Journal of Pharmacology. 376:1999;159-167.
101. Shinkai, H., Ito, T., Yamada, H., 1999. Amide derivatives and nociceptin antagonists. International Patent. WO 99/48492.
102. Shinkai H., Ito T., Iida T., Kitao Y., Yamada H., Uchida I. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. Journal of Medicinal Chemistry. 43:2000;4667-4677.
103. Siniscalchi A., Rodi D., Beani L., Bianchi C. Inhibitory effect of nociceptin on [3H]-5-HT release from rat cerebral cortex slices. British Journal of Pharmacology. 128:1999;119-123.
104. Thomsen C., 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. British Journal of Pharmacology. 131:2000;903-908.
105. Tulshian, D., Ho, G.D., Silverman, L.S., Matasi, J.J., McLeod, R.L. Hey, J.A., Chapman, R.W., Bercovici, A., Cuss, F.M., 2001a. High affinity ligands for nociceptin receptor ORL-1. United States Patent. US 6262066 B1. Schering Corporation, Kenilworth, N.J.
106. Tulshian, D., Ho, G.D., Silverman, L.S., Matasi, J.J., McLeod, R.L., Hey, J.A., Chapman, R.W., Bercovici, A., Cuss, F.M., 2001b. Nociceptin receptor ORL-1 agonists for use in treating cough. International PCT Application. WO 01/07050. Schering Corporation, Kenilworth, N.J.
107. Varani K., Rizzi A., Calo G., Bigoni R., Toth G., Guerrini R., Gessi S., Salvadori S., Borea P.A., Regoli D. Pharmacology of [Tyr1]nociceptin analogs: receptor binding and bioassay studies. Naunyn Schmiedebergs Archives of Pharmacology. 360:1999;270-277.
108. Wang J.B., Johnson P.S., Imai Y., Persico A.M., Ozenberger B.A., Eppler C.M., Uhl G.R. cDNA cloning of an orphan opiate receptor gene family member and its splice variant. FEBS Letters. 348:1994;75-79.
109. Wichmann J., Adam G., Rover S., Cesura A.M., Dautzenberg F.M., Jenck F. 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists. Bioorganic and Medicinal Chemistry Letters. 9:1999;2343-2348.
110. Wichmann J., Adam G., Rover S., Hennig M., Scalone M., Cesura A.M., Dautzenberg F.M., Jenck F. Synthesis of (1S,3aS)-8-(2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one, a potent and selective orphanin FQ (OFQ) receptor agonist with anxiolytic-like properties. European Journal of Medicinal Chemistry. 35:2000;839-851.
111. Xu I.S., Wiesenfeld-Hallin Z., Xu X.J. [Phe1psi(CH2-NH)Gly2]-nociceptin-(1-13)NH2, a proposed antagonist of the nociceptin receptor, is a potent and stable agonist in the rat spinal cord. Neuroscience Letters. 249:1998;127-130.
112. Yamada H., Nakamoto H., Suzuki Y., Ito T., Aisaka K. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. British Journal of Pharmacology. 135:2002;323-332.
113. Yamamoto T., Sakashita Y., Nozaki-Taguchi N. Antagonism of ORLI receptor produces an algesic effect in the rat formalin test. Neuroreport. 12:2001;1323-1327.
114. Zaveri N., Polgar W.E., Olsen C.M., Kelson A.B., Grundt P., Lewis J.W., Toll L. Characterization of opiates, neuroleptics, and synthetic analogs at ORL1 and opioid receptors. European Journal of Pharmacology. 428:2001;29-36.