Utilizing functional genomics to identify new pain treatments: The example of nociceptin

American Journal of PharmacoGenomics

Volumn 3, Issue 2, 2003, Pages 117-130

  Meunier, Jean Claude ^a  

^a INSTITUT DE PHARMACOLOGIE ET DE BIOLOGIE STRUCTURALE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

1 (1 CYCLOOCTYLMETHYL 3 HYDROXYMETHYL 4 PIPERIDYL) 3 ETHYL 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 4,6 DIAMINOQUINOLINE DERIVATIVE; 8 (2,3,3A,4,5,6 HEXAHYDRO 1H PHENALEN 1 YL) 1 PHENYL 1,3,8 TRIAZASPIRO[4.5]DECAN 4 ONE; [8 (1 NAPHTHYLMETHYL) 4 OXO 1 PHENYL 1,3,8 TRIAZASPIRO[4.5]DEC 3 YL]ACETIC ACID METHYL ESTER; ANALGESIC AGENT; ANTINOCICEPTIVE AGENT; BENZIMIDAZOPIPERIDINE DERIVATIVE; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; N (4 AMINO 2 METHYL 6 QUINOLINYL) 2 (4 ETHYLPHENOXYMETHYL)BENZAMIDE; NOCICEPTIN; ORPHAN OPIOID RECEPTOR LIKE 1 RECEPTOR; ORPHAN OPIOID RECEPTOR LIKE 1 RECEPTOR AGONIST; ORPHAN OPIOID RECEPTOR LIKE 1 RECEPTOR ANTAGONIST; PEPTIDE DERIVATIVE; SPIROPIPERIDINE DERIVATIVE; UFP 101; UNCLASSIFIED DRUG; ZP 120;

ALLODYNIA; ANALGESIA; CHRONIC PAIN; GENOMICS; HUMAN; HYPERALGESIA; INFLAMMATION; KNOCKOUT MOUSE; MOLECULAR CLONING; NOCICEPTION; NONHUMAN; PAIN; PRIORITY JOURNAL; REVIEW; TRANSGENIC MOUSE;

ANIMALS; GENOMICS; HUMANS; OPIOID PEPTIDES; PAIN; RECEPTORS, OPIOID;

ANIMALIA; MUS MUSCULUS; RODENTIA;

EID: 0038014065     PISSN: 11752203     EISSN: None     Source Type: Journal    
DOI: 10.2165/00129785-200303020-00005     Document Type: Review

References (182)

1. Debouck C, Metcalf B. The impact of genomics on drug discovery. Ann Rev Pharmacol Toxicol 2000; 40: 193-207
2. Stadel JM, Wilson S, Bergsma DJ. Orphan G protein-coupled receptors: a neglected opportunity for pioneer drug discovery. Trends Pharmacol Sci 1997; 18: 430-7
3. Howard AD, McAllister G, Feighner SD, et al. Orphan G protein-coupled receptors and natural ligand discovery. Trends Pharmacol Sci 2001; 22: 132-40
4. Meunier J-C, Mollereau C, Toll L, et al. Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor. Nature 1995; 377: 532-5
5. Reinscheid RK, Nothacker HP, Bourson A, et al. Orphanin FQ: a neuropeptide that activates an opioid-like G protein-coupled receptor. Science 1995; 270: 792-4
6. Florin S, Suaudeau C, Meunier J-C, et al. Nociceptin stimulates locomotion and exploratory behaviour in mice. Eur J Pharmacol 1996; 317: 9-13
7. Devine DP, Taylor L, Reinscheid R. et al. Rats rapidly develop tolerance to the locomotor-inhibitory effects of the novel neuropeptide orphanin FQ. Neurochem Res 1996; 21: 1387-96
8. Jenck F, Moreau JL, Martin JR, et al. Orphanin FQ acts as an anxiolytic to attenuate behavioral responses to stress. Proc Natl Acad Sci U S A 1997; 94: 14854-8
9. Griebel G, Perrault G, Sanger DJ. Orphanin FQ, a novel neuropeptide with antistress-like activity. Brain Res 1999; 836: 221-4
10. Koster A, Montkowski A, Schulz S, et al. Targeted disruption of the orphanin FQ/nociceptin gene increases stress susceptibility and impairs stress adaptation in mice. Proc Natl Acad Sci USA 1999; 96: 10444-9
11. Reinscheid RK, Civelli O. The orphanin FQ/nociceptin knockout mouse: a behavioral model for stress responses. Neuropeptides 2002; 36: 72-6
12. Mogil JS, Grisel JE, Reinscheid RK, et al. Orphanin FQ is a functional anti-opioid peptide. Neuroscience 1996; 75: 333-7
13. Mogil JS, Grisel JE, Zhangs G, et al. Functional antagonism of mu-, delta- and kappa-opioid antinociception by orphanin FQ. Neurosci Lett 1996; 214: 131-4
14. Pomonis JD, Billington CJ, Levine AS. Orphanin FQ, agonist of orphan opioid receptor ORL1, stimulates feeding in rats. Neuroreport 1996; 8: 369-71
15. Stratford TR, Holahan MR, Kelley AE. Injections of nociceptin into nucleus accumbens shell or ventromedial hypothalamic nucleus increase food intake. Neuroreport 1997; 8: 423-6
16. Polidori C, de Caro G, Massi M. The hyperphagic effect of nociceptin/orphanin FQ in rats. Peptides 2000; 21: 1051-62
17. Sandin J, Georgieva J, Schott PA, et al. Nociceptin/orphanin FQ microinjected into hippocampus impairs spatial learning in rats. Eur J Neurosci 1997; 9: 194-7
18. Manabe T, Noda Y, Mamiya T, et al. Facilitation of long-term potentiation and memory in mice lacking nociceptin receptors. Nature 1998; 394: 577-81
19. Noda Y, Mamiya T, Manabe T, et al. Role of nociceptin systems in learning and memory. Peptides 2000; 21: 1063-9
20. Kapusta DR. Neurohumoral effects of orphanin FQ/nociceptin: relevance to cardiovascular and renal functions. Peptides 2000; 21: 1081-99
21. Peiser C, Undem BJ, Fischer A. Nociceptin effects in the airways. Peptides 2000; 21: 995-8
22. Osinski MA, Brown DR. Orphanin FQ/nociceptin: a novel neuromodulator of gastrointestinal function. Peptides 2000; 21: 999-1005
23. Lecci A, Giuliani S, Meini S, et al. Nociceptin and the micturition reflex. Peptides 2000; 21: 1007-21
24. Gumusel B, Hao Q, Hyman A, et al. Nocicepfin: an endogenous agonist for central opioid like 1 (ORL1) receptors possesses systemic vasorelaxant properties. Life Sci 1997; 60: PL141-5
25. Kapusta DR, Sezen SF, Chang JK, et al. Diuretic and antinatriuretic responses produced by the endogenous opioid-like peptide, nociceptin (orphanin FQ). Life Sci 1997; 60: PL15-21
26. McLeod RL, Bolser DC, Jia Y, et al. Antitussive effect of nociceptin/orphanin FQ in experimental cough models. Pulm Pharmacol Ther 2002; 15: 213-6
27. Giuliani S, Lecci A, Tramontana M, et al. The inhibitory effect of nociceptin on the micturition reflex in anaesthetized rats. Br J Pharmacol 1998; 124: 1566-72
28. Devine DP, Reinscheid RK, Monsma Jr FJ, et al. The novel neuropeptide orphanin FQ fails to produce conditioned place preference or aversion. Brain Res 1996; 727: 225-9
29. Murphy NP, Lee Y, Maidment NT. Orphanin FQ/nociceptin blocks acquisition of morphine place preference. Brain Res 1999; 832: 168-70
30. Ciccocioppo R, Panocka I, Polidori C, et al. Effect of nociceptin on alcohol intake in alcohol-preferring rats. Psychopharmacol (Berl) 1999; 141: 220-4
31. Evans CJ, Keith DE, Morrison H, et al. Cloning of a delta-opioid receptor by functional expression. Science 1992; 258: 1952-5
32. Kieffer BL, Befort K, Gaveriaux-Ruff C, et al. The delta-opioid receptor: isolation of a cDNA by expression cloning and pharmacological characterization. Proc Natl Acad Sci USA 1992; 89: 12048-52
33. Kieffer B. Molecular aspects of opioid receptors. In: Dickenson A, Besson J-M, editors. Pain, handbook of experimental pharmacology. Berlin: Springer-Verlag, 1997; 130: 281-303
34. Libert F, Parmentier M, Lefort A, et al. Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science 1989; 244: 569-72
35. Mollereau C, Parmentier M, Mailleux P, et al. ORL1, a novel member of the opioid receptor family: cloning, functional expression and localization. FEBS Lett 1994; 341: 33-8
36. Fukuda K, Kato S, Mori K, et al. cDNA cloning and regional distribution of a novel member of the opioid receptor family. FEBS Lett 1994; 343: 42-6
37. Chen Y, Fan Y, Liu J, et al. Molecular cloning, tissue distribution and chromosomal localization of a novel member of the opioid receptor gene family. FEBS Lett 1994; 347: 279-83
38. Bunzow JR, Saez C, Mortrud M, et al. 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 Lett 1994; 347: 284-8
39. Wang JB, Johnson PS, Imai Y, et al. cDNA cloning of an orphan opiate receptor gene family member and its splice variant. FEBS Lett 1994; 348: 75-9
40. Wick MJ, Minnerath SR, Lin X, et al. Isolation of a novel cDNA encoding a putative membrane receptor with high homology to the cloned mu-, delta-, and kappa-opioid receptors. Brain Res Mol Brain Res 1994; 27: 37-44
41. Lachowicz JE, Shen Y, Monsma Jr FJ, et al. Molecular cloning of a novel G protein-coupled receptor related to the opiate receptor family. J Neurochem 1995; 64: 34-40
42. Nishi M, Takeshima H, Mori M, et al. Structure and chromosomal mapping of genes for the mouse kappa-opioid receptor and an opioid receptor homologue (MOR-C). Biochem Biophys Res Commun 1994; 205: 1353-7
43. Halford WP, Gebhardt BM, Car DJ. Functional role and sequence analysis of a lymphocyte orphan opioid receptor. J Neuroimmunol 1995; 59: 91-101
44. Wick MJ, Minnerath SR, Roy S, et al. Expression of alternate forms of brain opioid orphan receptor mRNA in activated human peripheral blood lymphocytes and lymphocytic cell lines. Brain Res Mol Brain Res 1995; 32: 342-7
45. Pan YX, Xu J, Pasternak GW. Structure and characterization of the gene encoding a mouse kappa 3-related opioid receptor. Gene 1996; 171: 255-60
46. Anton B, Fein J, To T, et al. Immunohistochemical localization of ORL-1 in the central nervous system. J Comp Neurol 1996; 368: 229-51
47. Monteillet-Agius G, Fein J, Anton B, et al. ORL-1 and mu opioid receptor antisera label different fibers in areas involved in pain. J Comp Neurol 1998; 399: 373-83
48. Okuda-Ashitaka E, Tachibana S, Houtani T, et al. Identification and characterization of an endogenous ligand for opioid receptor homologue ROR-C: its involvement in allodynic response to innocuous stimulus. Brain Res Mol Brain Res 1996; 43: 96-104
49. Saito Y, Maruyama K, Saido TC, et al. N23K, a gene transiently up-regulated during neural differentiation, encodes a precursor protein for a newly identified neuropeptide nociceptin. Biochem Biophys Res Commun 1995; 217: 539-45
50. Mollereau C, Simons MJ, Soularue P, et al. Structure, tissue distribution, and chromosomal localization of the prepronociceptin gene. Proc Natl Acad Sci USA 1996; 93: 8666-70
51. Nothacker HP, Reinscheid RK, Mansour A, et al. Primary structure and tissue distribution of the orphanin FQ precursor. Proc Natl Acad Sci USA 1996; 93: 8677-82
52. Okuda-Ashitaka E, Minami T, Tachibana S, et al. Nocistatin, a peptide that blocks nociceptin action in pain transmission. Nature 1998; 392: 286-9
53. Florin S, Suaudeau C, Meunier JC, et al. Orphan neuropeptide Noc 11, a putative pronociceptin maturation product, stimulates locomotion in mice. Neuroreport 1997; 8: 705-7
54. Xie GX, Ito E, Maruyama K, et al. The promoter region of human prepronociceptin gene and its regulation by cyclic AMP and steroid hormones. Gene 1999; 238: 427-36
55. Houtani T, Nishi M, Takeshima H, et al. Structure and regional distribution of nociceptin/orphanin FQ precursor. Biochem Biophys Res Commun 1996; 219: 714-9
56. Neal CR, Mansour A, Reinscheid RK, et al. Localization of orphanin FQ (nociceptin) peptide and messenger RNA in the central nervous system of the rat. J Comp Neurol 1999; 406: 503-47
57. Boom A, Mollereau C, Meunier J-C. et al. Distribution of the nociceptin and nocistatin precursor transcript in the mouse central nervous system. Neuroscience 1999; 91: 991-1007
58. Riedl M, Shuster S, Vulchanova L, et al. Orphanin FQ/nociceptin-immunoreactive nerve fibers parallel those containing endogenous opioids in rat spinal cord. Neuroreport 1996; 7: 1369-72
59. Schulz S, Schreff M, Nuss D, et al. Nociceptin/orphanin FQ and opioid peptides show overlapping distribution but not co-localization in pain-modulatory brain regions. Neuroreport 1996; 7: 3021-5
60. Cheng ZJ, Fan GH, Zhao J, et al. Endogenous opioid receptor-like receptor in human neuroblastoma SK-N-SH: activation of inhibitory G protein and homologous desensitization. Neuroreport 1997; 8: 1913-8
61. Mathis JP, Ryan-Moro J, Chang A, et al. Biochemical evidence for orphanin FQ/nociceptin receptor heterogeneity in mouse brain. Biochem Biophys Res Commun 1997; 230: 462-5
62. ++ channel current and intracellular Ca++ in the SH-SY5Y human neuroblastoma cell line. Br J Pharmacol 1996; 118: 205-7
63. 2+ channel inhibition and its desensitization in NG108-15 cells. Eur J Pharmacol 1998; 351: 247-52
64. Knoflach F, Reinscheid RK, Civelli O, et al. Modulation of voltage-gated calcium channels by orphanin FQ in freshly dissociated hippocampal neurons. J Neurosci 1996; 16: 6657-64
65. Pu L, Bao GB, Ma L, et al. Acute desensitization of nociceptin/orphanin FQ inhibition of voltage-gated calcium channels in freshly dissociated hippocampal neurons. Eur J Neurosci 1999; 11: 3610-6
66. 2+ channel currents of acutely dissociated rat periaqueductal grey neurons. J Physiol (London) 1998; 509: 47-58
67. 2+ channel current in rat sensory neurons by a G protein-independent mechanism. J Neurosci 1997; 17: 8721-8
68. Vaughan CW, Christie MJ. Increase by the ORL1 receptor (opioid receptor-like 1) ligand, nociceptin, of inwardly rectifying potassium conductance in dorsal raphe nucleus neurons. Br J Pharmacol 1996; 117: 1609-11
69. Connor M, Vaughan CW, Chieng B. et al. Nociceptin receptor coupling to a potassium conductance in rat locus coeruleus neurons in vitro. Br J Pharmacol 1996; 119: 1614-8
70. Vaughan CW, Ingram SL, Christie MJ. Actions of the ORL1 receptor ligand nociceptin on membrane properties of rat periaqueductal gray neurons in vitro. J Neurosci 1997; 17: 996-1003
71. + currents in hippocampal CA1 neurons by both ORL-1 and opiate receptor mechanisms. J Neurophysiol 1999; 82: 1776-85
72. Amano T, Matsubayashi H, Tamura Y, et al. Orphanin FQ-induced outward current in rat hippocampus. Brain Res 2000; 853: 269-74
73. + conductance by orphanin FQ/nociceptin in vasopressin-containing neurons. Neuroendocrinology 1999; 69: 385-96
74. + evoked glutamate release from rat cerebral cortex. Br J Pharmacol 1996; 119: 1081-3
75. 3H]-5-HT release from rat cerebral cortex slices. Br J Pharmacol 1999; 128: 119-23
76. Itoh K, Konya H, Takai E, et al. Modification of acetylcholine release by nociceptin in conscious rat striatum. Brain Res 1999; 845: 242-5
77. Neal MJ, Cunningham JR, Paterson SJ, et al. Inhibition by nociceptin of the light-evoked release of ACh from retinal cholinergic neurons. Br J Pharmacol 1997; 120: 1399-400
78. Patel HJ, Giembycz MA, Spicuzza L, et al. Naloxone-insensitive inhibition of acetylcholine release from parasympathetic nerves innervating guinea pig trachea by the novel opioid, nociceptin. Br J Pharmacol 1997; 120: 735-6
79. Murphy NP, Ly HT, Maidment NT. Intracerebroventricular orphanin FQ/nociceptin suppresses dopamine release in the nucleus accumbens of anaesthetized rats. Neuroscience 1996; 75: 1-4
80. Gintzler AR, Adapa ID, Toll L, et al. Modulation of enkephalin release by nociceptin (orphanin FQ). Eur J Pharmacol 1997; 325: 29-34
81. Schlicker E, Werthwein S, Kathmann M, et al. Nociceptin inhibits noradrenaline release in the mouse brain cortex via presynaptic ORL1 receptors. Naunyn Schmiedebergs Arch Pharmacol 1998; 358: 418-22
82. Bucher B. ORL1 receptor-mediated inhibition by nociceptin of noradrenaline release from perivascular sympathetic nerve endings of the rat tail artery. Naunyn Schmiedebergs Arch Pharmacol 1998; 358: 682-5
83. Nemeth J, Helyes Z, Oroszi G, et al. Inhibition of nociceptin on sensory neuropeptide release and mast-cell plasma extravasation in rats. Eur J Pharmacol 1998; 347: 101-4
84. Bryant W, Janik J, Baumann M, et al. Orphanin FQ stimulates prolactin and growth hormone release in male and female rats. Brain Res 1998; 807: 228-33
85. Faber ES, Chambers JP, Evans RH, et al. Depression of glutamatergic transmission by nociceptin in the neonatal rat hemisected spinal cord preparation in vitro. Br J Pharmacol 1996; 119: 189-90
86. Liebel JT, Swandulla D, Zeilhofer HU. Modulation of excitatory synaptic transmission by nociceptin in superficial dorsal horn neurons of the neonatal rat spinal cord. Br J Pharmacol 1997; 121: 425-32
87. Shu YS, Zhao ZQ, Li MY, et al. Orphanin FQ/nociceptin modulates glutamate-and kainic acid-induced currents in acutely isolated rat spinal dorsal horn neurons. Neuropeptides 1998; 32: 567-71
88. Giuliani S, Maggi CA. Inhibition of tachykinin release from peripheral nerve endings of sensory nerves by nociceptin, a novel opioid peptide. Br J Pharmacol 1996; 118: 1567-9
89. Fischer A, Forssmann WG, Undem BJ. Nociceptin-induced inhibition of tachykinergic neurotransmission in guinea pig bronchus. J Pharmacol Exp Ther 1998; 285: 902-7
90. Kyuhou S, Gemba H. Injection of orphanin FQ/nociceptin into the periaqueductal gray suppresses the forebrain-elicited vocalization in the guinea pig. Neurosci Lett 1999; 260: 113-6
91. Stanfa LC, Chapman V, Kerr N, et al. Inhibitory action of nociceptin on spinal dorsal horn neurones of the rat, in vivo. Br J Pharmacol 1996; 118: 1875-7
92. Wang XM, Zhang KM, Mokha SS. Nociceptin (orphanin FQ), an endogenous ligand for the QRL1 (opioid-receptor-like 1) receptor, modulates responses of trigeminal neurons evoked by excitatory amino acids and somatosensory stimuli. J Neurophysiol 1996; 76: 3568-72
93. Heinricher MM, McGaraughty S, Grandy DK. Circuitry underlying anti-opioid actions of orphanin FQ in the rostral ventromedial medulla. J Neurophysiol 1997; 78: 3351-8
94. Pan ZZ, Hirakawa N, Fields HL. A cellular mechanism for the bidirectional painmodulating actions of orphanin FQ/nociceptin. Neuron 2000; 26: 515-22
95. Chu X, Xu N, Li P, et al. Profound inhibition of cardiomotor neurons in the rat rostral ventrolateral medulla by nociceptin/orphanin FQ. Neuroreport 1998; 9: 1081-4
96. + conductance. Neuroendocrinology 1998; 67: 73-82
97. Doi N, Dutia MB, Russell JA. Inhibition of rat oxytocin and vasopressin supraoptic nucleus neurons by nociceptin in vitro. Neuroscience 1998; 84: 913-21
98. Meis S, Pape HC. Postsynaptic mechanisms underlying responsiveness of amygdaloid neurons to nociceptin/orphanin FQ. J Neurosci 1998; 18: 8133-44
99. Hara N, Minami T, Okuda-Ashitaka E, et al. Characterization of nociceptin hyperalgesia and allodynia in conscious mice. Br J Pharmacol 1997; 121: 401-8
100. Kavaliers M, Perrot-Sinal TS. Pronociceptive effects of the neuropeptide, nociceptin, in the land snail, cepaea nemoralis. Peptides 1996; 17: 763-8
101. Kavaliers M, Choleris E, Saucier DM. The NMDA receptor antagonist, NPC 12626, reduces the pronociceptive effects of orphanin FQ and kappa opiate antinociception in the land snail, cepaea nemoralis. Peptides 1997; 18: 943-7
102. Tian JH, Xu W, Zhang W, et al. Involvement of endogenous orphanin FQ in electroacupuncture-induced analgesia. Neuroreport 1997; 8: 497-500
103. Tian JH, Xu W, Fang Y, et al. Bidirectional modulatory effect of orphanin FQ on morphine-induced analgesia: antagonism in brain and potentiation in spinal cord of the rat. Br J Pharmacol 1997; 120: 676-80
104. Grisel JE, Mogil JS. Effects of supraspinal orphanin FQ/nociceptin. Peptides 2000; 21: 1037-45
105. Vanderah TW, Raffa RB, Lashbrook J, et al. Orphanin-FQ/nociceptin: lack of antinociceptive hyperalgesic or allodynic effects in acute thermal or mechanical tests following intracerebroventricular or intrathecal administration to mice or rats. Eur J Pain 1998; 2: 267-80
106. Zhu CB, Cao XD, Xu SF, et al. Orphanin FQ potentiates formalin-induced pain behavior and antagonizes morphine analgesia in rats. Neurosci Lett 1997; 235: 37-40
107. Wang JL, Zhu CB, Cao XD, et al. Distinct effect of intracerebroventricular and intrathecal injections of nociceptin/orphanin FQ in the rat formalin test. Regul Pept 1999; 79: 159-63
108. Inoue M, Kobayashi M, Kozaki S, et al. Nociceptin/orphanin FQ-induced nociceptive responses through substance P release from peripheral nerve endings in mice. Proc Natl Acad Sci USA 1998; 95: 10949-53
109. Carpenter KJ, Vithlani M, Dickenson A. Unaltered peripheral excitatory actions of nociceptin contrast with enhanced spinal inhibitory effects after carrageenan inflammation: an electrophysiological study in the rat. Pain 2000; 85: 433-41
110. Mork H, Hommel K, Uddman R, et al. Does nociceptin play a role in pain disorders in man? Peptides 2002; 23: 1581
111. Xu XJ, Hao JX, Wiesenfeld-Hallin Z. Nociceptin or antinociceptin: potent spinal antinociceptive effect of orphanin FQ/nociceptin in the rat. Neuroreport 1996; 7: 2092-4
112. Hao JX, Wiesenfeld-Hallin Z, Xu XJ. Lack of cross-tolerance between the antinociceptive effect of intrathecal orphanin FQ and morphine in the rat. Neurosci Lett 1997; 223: 49-52
113. Taylor F, Dickenson A. Nociceptin/orphanin FQ: a new opioid, a new analgesic. Neuroreport 1998; 9: R65-70
114. Moran TD, Abdulla FA, Smith PA. Cellular neurophysiological actions of nociceptin/orphanin FQ. Peptides 2000; 21: 969-76
115. Erb K, Liebel JT, Tegeder I, et al. Spinally delivered nociceptin/orphanin FQ reduces flinching behaviour in the rat formalin test. Neuroreport 1997; 8: 1967-70
116. Yamamoto T, Nozaki-Taguchi N, Kimura S. Analgesic effect of intrathecally administered nociceptin, an opioid receptor-like 1 receptor agonist, in the rat formalin test. Neuroscience 1997; 81: 249-54
117. Yamamoto T, Nozaki-Taguchi N, Kimura S. Effects of intrathecally administered nociceptin, an opioid receptor-like 1 (ORL1) receptor agonist, on the thermal hyperalgesia induced by carageenan injection into the rat paw. Brain Res 1997; 754: 329-32
118. Yamamoto T, Nozaki-Taguchi N, Kimura S. Effects of intrathecally administered nociceptin, an opioid receptor-like 1 (ORL1) receptor agonist, on the thermal hyperalgesia induced by unilateral constriction injury to the sciatic nerve in the rat. Neurosci Lett 1997; 224: 107-10
119. Hao JX, Xu IS, Wiesenfeld-Hallin Z, et al. Anti-hyperalgesic and anti-allodynic effects of intrathecal nociceptin/orphanin FQ in rats after spinal cord injury, peripheral nerve injury, and inflammation. Pain 1998; 76: 385-93
120. Xu IS, Grass S, Wiesenfeld-Hallin Z, et al. Effects of intrathecal orphanin FQ on a flexor reflex in the rat after inflammation or peripheral nerve section. Eur J Pharmacol 1999; 370: 17-22
121. Abdulla FA, Smith PA. Axotomy reduces the effect of analgesic opioids yet increases the effect of nociceptin on dorsal root ganglion neurons. J Neurosci 1998; 18: 9685-94
122. Yamamoto T, Sakashita Y. The role of the spinal opioid receptor like 1 receptor, the NK-1 receptor, and cyclooxygenase-2 in maintaining postoperative pain in the rat. Anesth Analg 1999; 89: 1203-8
123. Helyes Z, Nemeth J, Pinter E, et al. Inhibition by nociceptin of neurogenic inflammation and the release of SP and CGRP from sensory nerve terminals. Br J Pharmacol 1997; 121: 613-5
124. Habler H, Timmermann L, Stegman J, et al. Effects of nociceptin and nocistatin on antidromic vasodilatation in hairless skin of the rat hindlimb in vivo. Br J Pharmacol 1999; 127: 1719-27
125. Dong XW, Williams PA, Jia YP, et al. Activation of spinal ORL-1 receptors prevents acute cutaneous neurogenic inflammation: role of nociceptin-induced suppression of primary afferent depolarization. Pain 2002; 96: 309-18
126. Kimura T, Kitaichi K, Hiramatsu K, et al. Intradermal application of nociceptin increases vascular permeability in rats: the possible involvement of histamine release from mast cells. Eur J Pharmacol 2000; 407: 327-32
127. Grond S, Gabriel A, Pietruck C, et al. Bi-directional modulation of 5-hydroxytryptamine-induced plasma extravasation in the rat knee joint by nociceptin. Neuroscience 2001; 103: 1085-92
128. 4. J Immunol 2001; 166: 3650-4
129. 2 exert anti-opioid effects in the Freund's adjuvant-induced arthritic rat model of chronic pain. Br J Pharmacol 1999; 128: 1252-8
130. Andoh T, Itoh M, Kuraishi Y. Nociceptin gene expression in rat dorsal root ganglia induced by peripheral inflammation. Neuroreport 1997; 8: 2793-6
131. Itoh M, Takasaki I, Andoh T, et al. Induction by carrageenan inflammation of prepronociceptin mRNA in VR1-immunoreactive neurons in rat dorsal root ganglia. Neurosci Res 2001; 40: 227-33
132. Jia Y, Linden DR, Serie JR, et al. Nociceptin/orphanin FQ binding increases in superficial laminae of the rat spinal cord during persistent peripheral inflammation. Neurosci Lett 1998; 250: 21-4
133. Anderberg UM, Liu Z, Berglund L, et al. Plasma levels on nociceptin in female fibromyalgia syndrome patients. Z Rheumatol 1998; 57: 77-80
134. Brooks H, Elton CD, Smart D, et al. Identification of nociceptin in human cerebrospinal fluid: comparison of levels in pain and non-pain states. Pain 1998; 78: 71-3
135. Rosen A, Lundeberg T, Bytner B, et al. Central changes in nociceptin, dynorphin B and Met-enkephalin-Arg-Phe in different models of nociception. Brain Res 2000; 857: 212-8
136. Ko MH, Kim YH, Woo RS, et al. Quantitative analysis of nociceptin in blood of patients with acute and chronic pain. Neuroreport 2002; 13: 1631-3
137. Nishi M, Houtani T, Noda Y, et al. Unrestrained nociceptive response and disregulation of hearing ability in mice lacking the nociceptin/orphanin FQ receptor. EMBO J 1997; 16: 1858-64
138. Manabe T, Noda Y, Mamiya T, et al. Facilitation of long-term potentiation and memory in mice lacking nociceptin receptors. Nature 1998; 394: 577-81
139. Mamiya T, Noda Y, Ren X, et al. Morphine tolerance and dependence in the nociceptin receptor knockout mice. J Neural Transm 2001; 108: 1349-61
140. Ueda H, Inoue M, Takeshima H, et al. Enhanced spinal nociceptin receptor expression develops morphine tolerance and dependence. J Neurosci 2000; 20: 7640-7
141. Koster A, Montkowski A, Schulz S, et al. Targeted disruption of the orphanin FQ/nociceptin gene increases susceptibility and impairs stress adaptation in mice. Proc Natl Acad Sci USA 1999; 96: 10444-9
142. Kest B, Hopkins E, Palmese CA, et al. Morphine tolerance and dependence in nociceptin/orphanin FQ transgenic knock-out mice. Neuroscience 2001; 104: 217-22
143. Dooley CT, Houghten RA. Orphanin FQ: receptor binding and analog structure activity relationships in rat brain. Life Sci 1996; 59: PL23-9
144. Calo' G, Bigoni R, Rizzi A, et al. Nociceptin/orphanin FQ receptor ligands. Peptides 2000; 21: 935-47
145. Calo' G, Rizzi A, Marzola G, et al. Pharmacological characterization of the nociceptin receptor mediating hyperalgesia in the mouse tail withdrawal assay. Br J Pharmacol 1998; 125: 373-8
146. Okada K, Sujaku T, Chuman Y, et al. Highly potent nociceptin analog containing the Arg-Lys triple repeat. Biochem Biophys Res Commun 2000; 278: 493-8
147. Rizzi D, Rizzi A, Bigoni R, et al. Arg(14), Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. J Pharmacol Exp Ther 2002; 300: 57-63
148. Guerrini R, Calo' G, Rizzi A, et al. A new selective antagonist of the nociceptin receptor. Br J Pharmacol 1998; 123: 163-5
149. 2]noc-(1-13)-amide is an agonist of the nociceptin (ORL1) receptor. Eur J Pharmacol 1998; 349: R5-6
150. 2, a proposed antagonist of the nociceptin receptor, is a potent and stable agonist in the rat spinal cord. Neurosci Lett 1998; 249: 127-30
151. 2 acts as an agonist of the orphanin FQ/nociceptin receptor in vivo. Eur J Pharmacol 1998; 357: R1-3
152. Guerrini R, Calo G, Bigoni R, et al. Further studies on nociceptin-related peptides: discovery of a new chemical template with antagonist activity on the nociceptin receptor. J Med Chem 2000; 43: 2805-13
153. 2 on nociceptin receptor mediated inhibition of cAMP formation in Chinese hamster ovary cells stably expressing the recombinant human nociceptin receptor. Neurosci Lett 2000; 278: 109-12
154. 2, a new selective nociceptin receptor antagonist. Br J Pharmacol 2000; 129: 1183-93
155. 2 selectively reduces the spinal inhibitory effect of nociceptin. Life Sci 2002; 70: 1151-7
156. Rizzi A, Bigoni R, Marzola G, et al. The nociceptin/orphanin FQ receptor antagonist, [Nphe1]NC(1-13)NH2, potentiates morphine analgesia. Neuroreport 2000; 11: 2369-72
157. 2 in mice. Neurosci Lett 2001; 316: 25-8
158. 2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor. Br J Pharmacol 2002; 136: 303-11
159. Dooley CT, Spaeth CG, Berzetei-Gurske IP, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther 1997; 283: 735-41
160. Lapalu S, Moisand C, Mazarguil H, et al. Comparison of the structure-activity relationships of nociceptin and dynorphin A using chimeric peptides. FEBS Lett 1997; 417: 333-6
161. Topham CM, Moulddous L, Poda G, et al. Molecular modelling of the ORL1 receptor and its complex with nociceptin. Protein Eng 1998; 11: 1163-79
162. Mollereau C, Mouledous L, Lapalu S, et al. Distinct mechanisms for activation of the opioid receptor-like 1 and kappa-opioid receptors by nociceptin and dynorphin A. Mol Pharmacol 1999; 55: 324-31
163. Rizzi A, Rizzi D, Marzola G, et al. Pharmacological characterization of the novel nociceptin/orphanin FQ receptor ligand, ZP120: in vitro and in vivo studies in mice. Br J Pharmacol 2002; 137: 369-74
164. Ronzoni S, Peretto I, Giardina GAM. Lead generation and lead optimisation approaches in the discovery of selective, non-peptide ORL1 receptor agonists and antagonists. Exp Opin Ther Patents 2001; 11: 525-46
165. Butour J-L, Moisand C, Mazarguil H, et al. Recognition and activation of the opioid receptor-like ORL1 receptor by nociceptin, nociceptin analogs and opioids. Eur J Pharmacol 1997; 321: 97-103
166. Yeadon M, Kitchen I. Comparative binding of m- and d-selective ligands in whole brain and pons/medulla homogenates from rat: affinity profiles of fentanyl derivatives. Neuropharmacology 1988; 27: 345-8
167. Kawamoto H, Ozaki S, Itoh Y, et al. 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-2Hbenzimidazol-2-one (J-113397). J Med Chem 1999; 42: 5061-3
168. Ozaki S, Kawamoto H, Itoh Y, et al. A potent and highly selective nonpeptidyl nociceptin/orphanin FQ receptor (ORL1) antagonist, J-113397. Eur J Pharmacol 2000; 387: R17-8
169. Vaughan CW, Connor M, Jennings EA, et al. Actions of nociceptin/orphanin FQ and other prepronociceptin products on rat rostral ventromedial medulla neurons in vitro. J Physiol 2001; 534: 849-59
170. Ozaki S, Okuda S, Miyaji M, et al. Pharmacological characterization of J-113397, a potent ORL1 receptor antagonist. 31st International Narcotics Research Conference; 2000 Jul 7; Seattle
171. Yamamoto T, Sakashita Y, Nozaki-Taguchi N. Antagonism of ORL1 receptor produces an algesic effect in the rat formalin test. Neuroreport 2001; 12: 1323-7
172. Shinkai H, Ito T, Iida T, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem 2000; 43: 4667-77
173. Yamada H, Nakamoto H, Suzuki Y, et al. Pharmacological profiles of a novel opioid receptor-like 1 (ORL1) receptor antagonist, JTC-801. Br J Pharmacol 2002; 135: 323-32
174. Muratani T, Minami T, Enomoto U, et al. Characterization of nociceptin/orphanin FQ-induced pain responses by the novel receptor antagonist N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide monohydrochloride. J Pharmacol Exp Ther 2002; 303: 424-30
175. Jenck F, Wichmann J, Dautzenberg FM, et al. A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat. Proc Natl Acad Sci USA 2000; 97: 4938-43
176. Ciccocioppo R, Biondini M, Antonelli L, et al. Reversal of stress- and CRF-induced anorexia in rats by the synthetic nociceptin/orphanin FQ receptor agonist, Ro 64-6198. Psychopharmacology (Berl) 2002; 161: 113-9
177. Dautzenberg FM, Wichmann J, Higelin J, et al. 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. J Pharmacol Exp Ther 2001; 298: 812-9
178. Le Pen G, Wichmann J, Moreau JL, et al. The orphanin receptor agonist
179. 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. Br J Pharrnacol 2000; 131: 903-8
180. Mogil JS, Pasternak GW. The molecular and behavioral pharmacology of the orphanin FQ/nociceptin peptide and receptor family. Pharmacol Rev 2001; 53: 381-415
181. Chen Z, Inoue M, Hopkins E, et al. Nociceptin/oFQ gene knockout reveals an antinociceptive role for nociceptin/oFQ in the mouse. Soc Neurosci Abstr 1999; 25: 1472
182. Yamamoto T, Nozaki-Taguchi N, Sakashita Y, et al. Nociceptin/orphanin FQ: role in nociceptive information processing. Prog Neurobiol 1999; 57: 527-35