Advanced search
Publication Cover
Expert Opinion on Therapeutic Patents Volume 15, 2005 - Issue 4
Submit an article Journal homepage
125
Views
51
CrossRef citations to date
0
Altmetric
Review

Recent advances towards the discovery of ORL-1 receptor agonists and antagonists

Gilles C Bignan Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000, Route 202, PO Box 300, Raritan, NJ 08869, USA. [email protected]
,
Peter J Connolly Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000, Route 202, PO Box 300, Raritan, NJ 08869, USA. [email protected]
&
Steven A Middleton Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000, Route 202, PO Box 300, Raritan, NJ 08869, USA. [email protected]
Pages 357-388 | Published online: 22 Apr 2005

Bibliography

  • COX BM, CHAVKIN C, CHRISTIE MJ et al.: Opioid receptors. In: The IUPHAR Compendium of Receptor Characterization and Classification. Girdlestone D (Ed.), IUPHAR Media Ltd, London (2000):321–333.
  • MEUNIER JC, MOLLEREAU C, TOLL L et al.: Isolation and structure of the endogenous agonist of opioid receptor-like ORL-1 receptor. Nature (1995) 377(6549):532–535.
  • REINSCHEID RK, NOTHACKER HP, BOURSON A et al.: Orphanin FQ: A neuropeptide that activates an opioid like G-protein-coupled receptor. Science (1995) 270(5237):792–794.
  • MOLLEREAU C, PARMENTIER M, MAILLEUX P et al.: ORL-1, a novel member of the opioid receptor family � cloning, functional expression and localization. FEBS Lett. (1994) 341(1):33–38.
  • HRUBY VJ, GEHRIG CA: Recent developments in the design of receptor specific opioid peptides. Med. Res. Rev. (1989) 9(3):343–401.
  • PATERSON SJ, KOSTERLITZ HW, VAVREK RJ et al.: Effects of D-amino acid substitution in dynorphin A (1-9) on binding at the mu-, delta- and kappa-sites. Neuropeptides (1984) 5 ( 1-3): 177–180.
  • SHIMOHIGASHI Y: Design principles: enkephalins with predictable mu/delta receptor specificity. Natl Inst. Drug Abuse Res. Monogr. Ser. (1986) 69:65–100
  • REINSCHEID RK, ARDATI A, MONSMA FJ JR et al.: Structure�activity relationship studies on the novel neuropeptide orphanin FQ j Biol. Chem. (1996) 271(24):14163–14168.
  • •Nociceptin peptide SAR study.
  • BUTOUR J-L, MOISAND C, MAZARGUIL H et al.: Recognition and activation of the opioid receptor-like ORL-1 receptor by nociceptin, nociceptin analogs and opioids. Eur. J. Pharmacol (1997) 321(1):97–103.
  • GUERRINI R, CALO G, RIZZI A et ell.: Address and message sequences for the nociceptin receptor: a structure�activity study of nociceptin-(1–13)-peptide amide. J. Med. Chem. (1997) 40(12):1789–1793.
  • REINSCHEID RK, HIGELIN J, HENNINGSEN RA et al.: Structures that delineate orphanin FQ and dynorphin A pharmacological selectivities. Biol. Chem. (1998) 273(3):1490–1495.
  • SHIMOHOGASHI Y, HATANO R, FUJITA T et al.: Sensitivity of opioid receptor-like receptor ORL-1 for chemical modification on nociceptin, a naturally occurring nociceptive peptide. J. Biol. Chem. (1996) 271(30:23642–23645.
  • CORBETT AD, PATERSON SJ, McKNIGHT AT et al.: Dynorphin1_8 and dynorphin1_9 are ligands for the K-subtype of opiate receptor. Nature (1982) 299(5878):79–81.
  • SEKI T, MINAMI M, KIMURA C et al: Bremazocine recognizes the difference in four amino acid residues to discriminate between a nociceptin/orphanin FQ receptor and opioid receptors. Jpn. j Pharmacol (1998) 77(4):301–306.
  • LAPALU S, MOISAND C, BUTOUR J-L et al.: Different domains of the ORL-1 and K-opioid receptors are involved in recognition of nociceptin and dynorphin A. FEBS Lett. (1998) 427(2):296–300.
  • MENG F, UDE Y, HOVERSTEN MT et al.: Creating a functional opioid alkaloid binding site in the orphanin FQ receptor through site-directed mutagenesis. MoL Pharmacol (1998) 53(4):772–777.
  • MENG F, TAYLOR LP, HOVERSTEN MT et al.: Moving from the orphanin FQ receptor to an opioid receptor using four point mutations. J. Biol. Chem. (1996) 271(50):32016–32020.
  • PAN YX, XU J, RYAN-MORO J et al: Dissociation of affinity and efficacy in KOR-3 chimeras. FEBS Lett. (1996) 395(2-3):207–210.
  • MOLLEREAU C, MOISAND C, BUTOUR J-L et al.: Replacement of G1n280 by His in TM6 of the human ORL-1 receptor increases affinity but reduces intrinsic activity of opioids. FEBS Lett. (1990 395(1):17–21.
  • CONNOR M, VAUGHAN, CW, CHIENG B et al.: Nociceptin receptor coupling to a potassium conductance in rat locus ceruleus neurons in vitro. Br. J. Pharmacol (1996) 119(8):1614–1618.
  • VAUGHAN C, CHRISTIE MJ: Increase by the ORL-1 receptor (opioid receptor-like-1) ligand, nociceptin, of inwardly rectifying K conductance in dorsal raphe nucleus neurons. Br. J. Pharmacol (1996) 117(8):1609–1611.
  • MATTHES H, SEWARD EP, KIEFFER B et al: Functional selectivity of orphanin FQ for its receptor coexpressed with potassium channel subunits in Xenopus laevis oocytes. MoL Pharmacol (1996) 50(3):447–450.
  • VAUGHAN C, INGRAM SL, CHRISTIE MJ et al: Actions of the ORL-1 receptor ligand nociceptin on membrane properties of rat periaqueductal gray neurons in vitro. J. Neurosci. (1997):17(3):996–1003.
  • KOBAYASHI T, IKEDA K, TOGASHI S et al.: Effects of ligands on the nociceptin/ orphanin FQ receptor coexpressed with the G-protein-activated IQ channel in Xenopus oocytes. Br. J. Pharmacol (1997) 120(0:986–987.
  • IKEDA K, KOBAYASHI K, KOBAYASHI T et al.: Functional coupling of the nociceptin/orphanin FQ receptor with the G-protein-activated K (GIRK) channel. Mol Brain Res. (1997) 45(1):117–126.
  • CONNOR M, YEO A, HENDERAON G et al.: Special report. The effect of nociceptin on Ca2* channel current and intracellular Ca2* in the SH-SY5Y human neuroblastoma cell line. Br. J. Pharmacol (1996) 118(2):205–207.
  • KNOFLACH F, REINSCHEID RK, CIVELLI 0 et al.: Modulation of voltage-gated calcium channels by orphanin FQ in freshly dissociated hippocampal neurons. J. Neurosci. (1997) 16(20:6657–6664.
  • CONNOR M, CHRISTIE MJ: Modulation of Ca2* channel currents of acutely dissociated rat periaqueductal gray neurons. J. PhysioL (1998) 509(1):47–58.
  • FUKUDA K, SHODA T, MORIKAWA H et al.: Activation of mitogen-activated protein kinase by the nociceptin receptor expressed in Chinese hamster ovary cells. FEBS Lett. (1997) 412(2):290–294.
  • HAWES BE, FRIED S, YAO X et al.: Nociceptin (ORL-1) and ii-opioid receptors mediate mitogen-activated protein kinase activation in CHO cells through a 0-coupled signaling pathway: evidence for distinct mechanisms of agonist-mediated desensitization. J. Neurochemistry (1998) 71(3):1024–1033.
  • LOU L-G, ZHANG Z, MA L et ell.: Nociceptin/orphanin FQ activates mitogen-activated protein kinase in Chinese hamster ovary cells expressing opioid receptor-like receptor. J. Neurochem. (1998) 70(3):1316–1322.
  • NICOL B, LAMBERT DG, ROWBOTHAM DJ et al: Nociceptin induced inhibition of IQ- evoked glutamate release from rat cerebrocortical slices. Br. J. PharmacoL (1996) 119(6):1081–1083.
  • 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(3):425–432.
  • LAI CC, WU SY, DUN SL et al: Nociceptin-like immunoreactivity in the rat dorsal horn and inhibition of substantia gelatinosa neurons. Neuroscience (1997) 81(4):887–891.
  • 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(5):735–736.
  • 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(8):1399–1400.
  • GIULIANI S, MAGGI CA: Inhibition of tachykinin release from peripheral endings of sensory nerves by nociceptin, a novel opioid peptide. Br. J. Pharmacol (1996) 118(7):1567–1569.
  • FISCHER A. FORSSMANN WG, UNDEM BJ: Nociceptin-induced inhibition of tachykinergic neurotransmission in guinea pig bronchus./ Pharmacol Exp. Ther. (1998) 285(2):902–907.
  • SCHLICKER E, WERTHWEIN S, KATHMANN M et al.: Nociceptin inhibits noradrenaline release in the mouse brain cortex via presynaptic ORL-1 Receptors. Naunyn-Schmied. Arch. Pharmacol (1998) 358(4):418–422.
  • DARLAND T, HEINRICHER MM, GRANDY DK: Orphanin FQ/nociceptin: a role in pain and analgesia, but so much more. Trends Neurosci. (1998) 21(5):215–221.
  • HOUTANI T, NISHI M, TAKESHIMA H et al.: Structure and regional distribution of nociceptin/orphanin FQ precursor. Biochem. Biophys. Res. Comm. (1996) 219(3):714–719.
  • LACHOWICZ JE, SHEN Y, MONSMA FJ JR et al.: Molecular cloning of a novel G-protein-coupled receptor related to the opiate family. J. Neurochem. (1995) 64(1):34–40.
  • MEIS S, PAPE HC: Postsynaptic mechanisms underlying responsiveness of amygdaloid neurons to nociceptin/orphanin FQ. J. Neurosci. (1998) 18(20):8133–8144.
  • FLORIN S, MEUNIER JC, COSTENTIN J et al.: Autoradiographic localization of PFIlnociceptin binding sites in the rat brain. Brain Res. (1997) 880(1,2):11–16.
  • NEAL CR JR, MANSOUR A, REINSCHEID R et al.: Opioid receptor-like (ORL-1) receptor distribution in the rat central nervous system: comparison of ORL-1 receptor mRNA expression with 125I-(14Tyr)-orphanin FQ binding. J. Comp. NeuroL (1999) 412(4):563–605. 383 Expert Opin. Ther. Patents (2005) 15(4)
  • LETCHWORTH SR, MATHIS JP, ROSSI GC et al.: Autoradiographic localization of 1251[-cyr14]orphanin FQ/ Nociceptin and 1251[-cyr10]Orphanin FQ/ Nociceptin(1-11) binding sites in rat brain. J. Comp. NeuroL (2000) 423(2):319–329.
  • PELUSO J, LAFORGE KS, MATTHES HW et al.: Distribution of nociceptin/ orphanin FQreceptor transcript in human central nervous system and immune cells. J. NeuroimmunoL (1998) 81(1-2):184–192.
  • BRIDGE KE, WAIN WRIGHT A. REILLY K et al.: Autoradiographic localization of125I[-cyr14] nociceptin/ orphanin FQ Binding sites in macaque primate CNS. Neuroscience (2003) 118(2):513–523.
  • 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(8):1369–1372.
  • SCHULZ S, SCHREFF M, NUE D et aL: Nociceptin/orphanin FO and opioid peptides show overlapping distribution but not co-localization in pain-modulatory brain regions. Neuroreport (1996) 7(18):3021–3025.
  • ZEILHOFER HU, CALO G: Nociceptin/orphanin FQ and its receptor-potential targets for pain therapy? J. PharmacoL Exp. Ther. (2003) 306(2):423–429.
  • ••Perspective article discussing ORL-1 as apotential target for new analgesic drugs.
  • MEUNIER J-C: Utilizing functional genomics to identify new pain treatments: the example of nociceptin. Am. J. Pharmacogenomics (2003) 3(2):117–130.
  • NISHI M, HOUTANI T, NODA Y et ed.: Unrestrained nociceptive response and disregulation of hearing ability in mice lacking the nociceptin/orphanin FQ receptor. EMBO J. (1997) 16(8):1858–1864.
  • ROSSI GC, LEVENTHAL L, PASTERNAK GW et al.: Naloxone sensitive orphanin FQ-induced analgesia in mice. Eur. j PharmacoL (1996) 311(2/3):R7–R8.
  • ROSSI GC, PERLMUTTER M, LEVENTHAL Let al.: Orphanin FQ/ nociceptin analgesia in the rat. Brain Res. (1998) 792(2):327–330.
  • MOGIL JS, GRISEL JE, REINSCHEID RK et al.: Orphanin FQ is a functional anti-opioid peptide. Neuroscience (1996) 75(2):333–337.
  • SUAUDEAU C, FLORIN S, MEUNIER J-C et al.: Nociceptin-induced apparent hyperalgesia in mice as a result of the prevention of opioid autoanalgesic mechanisms triggered by the stress of an intracerebroventricular injection. Fundam. Clin. PharmacoL (1998) 12(4):420–425.
  • XU X-J, HAO J-X, -WIESENFELD-HALLIN Z: Nociceptin or antinociceptin: potent spinal antinociceptive effect of orphanin FQ/nociceptin in the rat. Neuroreport (1996) 7(13):2092–2094.
  • KING MA, ROSSI GC, CHANG AH et al.: Spinal analgesic activity of orphanin FQ/nociceptin and its fragments. Neurosci. Lett. (1997) 223(2):113–116.
  • TIAN JH, XU W, FANG Y et ell.: Bidirectional modulatory effect of orphanin FQ on morphine-induced analgesia: antagonism in brain and potentiation in spinal cord of the rat. Brit. J. PharmacoL (1997) 120(4):676–680.
  • JHAMANDAS KH, SUTAK M, HENDERSON G et al.: Antinociceptive and morphine modulatory actions of spinal orphanin FQ. Can. J. PhysioL PharmacoL (1998) 76(3):314–324.
  • HAO J-X, 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(3):385–393.
  • YAMAMOTO T, NOZAKI-TAGUCHI N, KIMURA S: Effects of intrathecally administered nociceptin, an opioid receptor-like-1 (ORL-1) receptor agonist, on the thermal hyperalgesia induced by unilateral constriction injury to the sciatic nerve in the rat. Neurosci. Lett. (1997) 224(2):107–H O.
  • YAMAMOTO T, NOZAKI-TAGUCHI N: Effects of intrathecally administered nociceptin, an opioid receptor-like-1 receptor agonist, and N-methyl-D-aspartate receptor antagonists on the thermal hyperalgesia induced by partial sciatic nerve injury in the rat. Anesthesiology (1997) 87(5):1145–1152.
  • YAMAMOTO T, NOZAKI-TAGUCHI N, KIMURA S: Effects of intrathecally administered nociceptin, an opioid receptor-like-1 (ORL-1) receptor agonist, on the thermal hyperalgesia induced by carageenan injection into the rat paw. Brain Res. (1997) 754(1,2):329–332.
  • 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(1):249–254.
  • ERB K, LIEBEL JT, TEGEDER I et al.: Spinally delivered nociceptin/orphanin FQ reduces flinching behavior in the rat formalin test. Neuroreport (1997) 8(8):1967–1970.
  • DAWSON-BASOA M, GINTZLER AR: Nociceptin (orphanin FQ) abolishes gestational and ovarian sex steroid-induced antinociception and induces hyperalgesia. Brain Res. (1997) 750(1,2):48–52.
  • OKUDA-ASHITAKA E, TACHIBANA S, HOUTANI T et al.: Identification and characterization of an endogenous ligand for opioid receptor homolog ROR-C: its involvement in allodynic response to innocuous stimulus. MoL Brain Res. (1996) 43(1,2):96–104.
  • XU X, GRASS S, HAO J et aL: Nociceptin/ orphanin FQ in spinal nociceptive mechanisms under normal and pathological conditions. Peptides (2000) 21(7):1031–1036.
  • PAN ZZ, HIRAKAWA N, FIELDS HL: A cellular mechanism for the bidirectional pain-modulating actions of orphanin FQ/ nociceptin. Neuron (2000) 26(2):515–522.
  • JENCK F, WICHMANN J, DAUTZENBERG FM et al.: A synthetic agonist at the orphanin FQ/nociceptin receptor ORL-1: anxiolytic profile in the rat. Proc. Natl. Acad. Sci. USA (2000) 97(9):4938–4943.
  • •Detailed study of Roche's Ro 64–6198 in models of anxiety and locomotor activity.
  • MOGIL JS, GRISEL JE, ZHANGS G et al.: Functional antagonism of mu-, delta-and kappa-opioid antinociception by orphanin FQ. Neurosci. Lett. (1996) 214(2-3):131–134.
  • GRISEL JE, MOGIL JS, BELKNAP JK et al.: Orphanin FQ acts as a supraspinal, but not a spinal, anti-opioid peptide. Neuroreport (1996) 7(13):2125–2129.
  • TIAN J-H, XU W, ZHANG Wet al.: Involvement of endogenous orphanin FQ in electroacupuncture-induced analgesia. Neuroreport (1997) 8(2):497–500.
  • UEDA H, YAMAGUCHI T, TOKUYAMA S et al.: partial loss of tolerance liability to morphine analgesia in mice lacking the nociceptin receptor gene. Neurosci. Lett. (1997) 237(2,3):136–138.384
  • KOTLINSKA J, SUDER P, LEGOWSKA A et al.: Orphanin FQ/ nociceptin inhibits morphine withdrawal. Life Sci. (2000) 66(8):PL119–123.
  • WALKER JR, SPINA M, TERENIUS L et al.: Nociceptin fails to affect heroin self-administration in the rat. Neuroreport (1998) 9(10):2243–2247.
  • DEVINE DP, REINSCHEID RK, MONSMA FJ JR et al.: The novel neuropeptide orphanin FQ fails to produce conditioned place preference or aversion. Brain Res. (1996) 727(1,2):225–229.
  • JENCK F, MOREAU J-L, MARTIN JR et al.: Orphanin FQ acts as an anxiolytic to attentuate behavioral responses to stress. Proc. NatL Acad. Sci. USA (1997) 94(26):14854–14858.
  • GRIEBEL G, PERRAULT G, SANGER DJ: Orphanin FQ, a novel neuropeptide with anti-stress-like activity. Brain Res. (1999) 836(1-2):221–224.
  • 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(18):10444–10449.
  • OLSZEWSKI PK, LEVINE AS: Minireview: characterization of influence of central nociceptin/orphanin FQ on consummatory behavior. Endocrinology (2004) 145(6):2627–2632.
  • POMONIS JD, BILLINGTON CJ, LEVINE AS: Orphanin FQ, agonist of orphan opioid receptor ORL-1, stimulates feeding in rats. Neuroreport (1996) 8(1):369–371.
  • LEVENTHAL L, MATHIS JP, ROSSI GC et al.: Orphan opioid receptor antisense probes block orphanin FQ-induced hyperphagia. Eur. J. PharmacoL (1998) 349(1):R1–R3.
  • CICCOCIOPPO R, MARTIN-FARDON R, WEISS F, MASSI M: Nociceptin/orphanin FQ inhibits stress- and CRF-induced anorexia in rats. Neuroreport (2001) 12(6):1145–1149.
  • 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 ORLI receptor in vitro and lack of tolerance in vivo. PharmacoL Exp. Ther. (2001) 298(2):812–819.
  • KAPUSTA, DR, SEZEN SF, CHANG J-K et al.: Diuretic and antinatriuretic responses produced by the endogenous opioid-like peptide, nociceptin (orphanin FQ). Life Sci. (1997) 60(1):PL15–PL21.
  • CHAMPION HC, CZAPLA MA, KADOWITZ PJ: Nociceptin, an endogenous ligand for the ORL-1 receptor, decreases cardiac output and total peripheral resistance in the rat. Peptides (1997) 18(5):729–732.
  • NOSSAMAN, BD, CHAMPION HC, KAYE AD et al.: Nociceptin has vasodilator activity in the pulmonary vascular bed of the rat. J. Cardiovas. PharmacoL Ther. (1998) 3(3):253–258.
  • WEI Y, HUANG Q, ZHU Yet al.: Potent hypotensive effects of orphanin FQ in conscious stroke-prone spontaneously hypertensive rats. Chin. Med. Sci. J. (1998) 13(2):67–70.
  • KAPUSTA DR, CHANG J-K, KENIGS VA: Central administration of WhelY(CF12-NH)G1y2lnociceptin(1-13)-WhelY(CF12-NH)G1y2lnociceptin(1-13)-NH2 and orphanin FQ/nociceptin (OFQ/ N) produce similar cardiovascular and renal responses in conscious rats. J. PharmacoL Exp. Ther. (1999) 289(1):173–180.
  • GIULIANI S, LECCI A, TRAMONTANA M et al.: The inhibitory effect of nociceptin on the micturition reflex in anesthetized rats. Brit. J. PharmacoL (1998) 124(7):1566–1572.
  • LECCI A, GIULIANI S, MEINI S et al.: Nociceptin and the micturition reflex. Peptides (2000) 21(7):1007–1021.
  • OSINSKI MA, BROWN DR et al.: Orphanin FQ/nociceptin: a novel neuromodulator of gastrointestinal function? Peptides (2000) 21(7):999–1005.
  • TANIGUCHI H, YOMOTA E, NOGI K et al.: The effect of nociceptin, an endogenous ligand for the ORL-1 receptor, on rat colonic contraction and transit. Eur. J. PharmacoL (1998) 353(2-3):265–271.
  • CICCOCIOPPO R, ECONOMIDOU D, FEDELI A et al.: The nociceptin/orphanin FQ/NOP receptor system as a target for treatment of alcohol abuse: a review of recent work in alcohol-preferring rats. PhysioL Behav. (2003) 79(1):121–128.
  • CICCOCIOPPOR, PANOCKA I, POLIDORI C et al.: Effect of nociceptin on alcohol intake in alcohol-preferring rats. PsychopharmacoL (1999) 141(2):220–224.
  • MCLEOD RI,, PARRA LE, MUTTER JC et al.: Nociceptin inhibits cough in the guinea-pig by activation of ORL(1) receptors. Brit. J. PharmacoL (2001) 132(0:1175–8.
  • CORBOZ MR, FERNANDEZ X, EGAN RW et al.: Inhibitory activity of nociceptin/orphanin FQ on capsaicin-induced bronchoconstriction in the guinea-pig. Life Sci. (2001) 69(10):1203–1211.
  • RIZZI k CALO G, TREVISANI M et al.: Nociceptin receptor activation inhibits tachykinergic nonadrenergic-noncholinergic contraction of guinea pig isolated bronchus. Life, Sci. (1999) 64(13):PL157–PL163.
  • CORBOZ MR, RIVELLI MA, EGAN RW et al.: Nociceptin inhibits capsaicin-induced bronchoconstriction in isolated guinea pig lung. Eur. j PharmacoL (2000) 402(1/2):171–179.
  • ROUGET C, CUI YY, D'AGOSTINO B et al.: Nociceptin inhibits airway microvascular leakage induced by HC1 intra-oesophageal instillation. Brit. J. PharmacoL (2004) 141(6):1077–1083.
  • JIA Y, WANG X, APONTE SI et al.: Nociceptin/orphanin FQ inhibits capsaicin-induced guinea-pig airway contraction through an inward-rectifier potassium channel. Brit. J. PharmacoL (2002) 135(3):764–770.
  • MANABE T, NODA Y, MAMIYA T et ed.: Facilitation of long-term potentiation and memory in mice lacking nociceptin receptors. Nature (1998) 394(6693):577–581.
  • MAMIYA T, NODA Y, NISHI M et al.: Enhancement of spatial attention in nociceptin/orphanin FQ receptor-knockout Mice. Brain Res. (1998) 783(2):236–240.
  • SANDIN J, GEORGIEVA J, SCHOTT PA et al.: Nociceptin/orphanin FQ microinjected into hippocampus impairs spatial learning in rats. Eur. J. Neurosci. (1997) 9(1):194–197.
  • YU T-P, FEIN J, PT-JAN T et al.: Orphanin FQ inhibits synaptic transmission and long-term potentiation in rat hippocampus. Hippocampus (1997) 7(1):88–94.
  • YU T-P, XIEOrphanin FQ/ nociceptin inhibits synaptic transmission and long-term potentiation in rat dentate gyrus through postsynaptic mechanisms. NeurophysioL (1998) 80(3):1277–1284.
  • HIRAMATSU M, INOUE K: Improvement by low doses of nociceptin on scopolamine-induced impairment of learning and/or memory. Eur. j PharmacoL (2000) 395(2):149–156.
  • MARTI M, MELA F, VERONESI C et Blockade of nociceptin/orphanin FQreceptor signaling in rat substantia nigra pars reticulata stimulates nigrostriatal dopaminergic transmission and motor behavior. J. Neurosci. (2004) 24(30):6659–6666.
  • MARTI M, MELA F, GUERRINI R et al.: Blockade of nociceptin/orphanin FQ transmission in rat substantia nigra reverses haloperidol-induced akinesia and normalizes nigral glutamate release. J. Neurochem. (2004) 91(6):1501–1504.
  • LAZZERI M, CALO G, SPINELLI M et al.: Urodynamic effects of intravesical nociceptin/orphanin FQ in patients with overactive bladder - a randomised, placebo-controlled, double-blind study. European Urology Supplements (2003) 2(1):72.
  • KAPUSTA DR, DAYAN, LA, KENIGS VA et al.: Nociceptin/orphanin FQ modulates the cardiovascular, but not renal, responses to stress in spontaneously hypertensive rats. an. Exp. PharmacoL PhysioL (2002) 29(3):254–259.
  • LECUDENNEC C, NAUDIN B, DOREGO J-C et al.: Nociceptin/orphanin FQ and related peptides reduce the increase in plasma corticosterone elicited in mice by an intracerebroventricular injection. Life Sci. (2002) 72(2):163–171.
  • JONASSEN TE, HADRUP N, BROEND Let al.: The aquaretic effect of the nociceptin analogue ZP120C is associated with marked downregulation of aquaporin 2. Oral presentation at American Heart Association Scientific Sessions 2002, Chicago, USA, November 17–20, 2002. Circulation (2002) 106(19)(Suppl.II):p11-135; abstract 680.
  • HADRUP N, PETERSEN JS, PRAETORIUS J et al.: Opioid receptor-like-1 stimulation in the collecting duct induces aquaresis through vasopressin-independent aquaporin-2 downregulation. Am. J. PhysioL (2004) 287(1, Pt.2): F160–F168.
  • KAPUSTA DR, KENIGS VA, VINGE MM, et aL: ZP120C, is a peripherally acting nociceptin analogue with water diuretic and potassium sparing properties. FASEBJ. (2002) 16(5, Pt. 2): A841. Poster no. 640.23.
  • RIZZI A, RIZZI D, MARZOLA G et Pharmacological characterization of the novel nociceptin/orphanin FQ receptor ligand ZP-120: in vitro and in vivo studies in mice. Br. J. PharmacoL (2002) 137(3):369–374.
  • •Report describing the pharmacology of Zealand Pharma's peptidic agonist, currently in Phase II trials.
  • MCDONALD J, CALO G, GUERRINI R et al.: UFP-101, a high affinity antagonist for the nociceptin/orphanin FQ receptor: radioligand and GTP-y-355 binding studies. Naunyn-Schmied. Arch. PharmacoL (2003) 367(2):183–187.
  • GAVIOLI EC, VAUGHAN CW, MARZOLA G et al.: Antidepressant-like effects of the nociceptin/orphanin FQ receptor antagonist UFP-101: new evidence from rats and mice. Naunyn Schmied. Arch. PharmacoL (2004) 369(6):547–553.
  • HUANG P, KEHNER GB, COWAN A et al.: Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist. j PharmacoL Exp. Ther. (2001) 297(2):688–695.
  • WNENDT S, KRUGER T, JANOCHA E et al.: Agonistic effect of buprenorphine in a nociceptin/OFQ receptor-triggered reporter gene assay. MoL PharmacoL (1999) 56(2):334–338.
  • LUTFY K, COWAN k Buprenorphine: a unique drug with complex pharmacology Curr. Neuropharm. (2004) 2(4):395–402.
  • MONTOYA ID, GORELICK DA, PRESTON KL et al.: Randomized trial of buprenorphine for treatment of concurrent opiate and cocaine dependence. Clin. PharmacoL Ther. (2004) 75(1):34–48.
  • SEKI T, AWAMURA S, KIMURA C et al.: Pharmacological properties of TRK-820 on cloned mu-, delta- and kappa-opioid receptors and nociceptin receptor. Eur. PharmacoL (1999) 376(1-2):159–167.
  • MIZOGUCHI H, HUNG K-C, LEITERMANN R et al.: Blockade of u-opioid receptor-mediated G-protein activation and antinociception by TRK-820 in mice. Eur. j PharmacoL (2003) 461(1):35–39.
  • PICK CG, PETER Y, SCHREIBER S et al.: Pharmacological characterization of buprenorphine, a mixed agonist-antagonist with 1(3 analgesia. Brain Res. (1997) 744(1):41–46.
  • GISTRAK MA, PAUL D, HAHN EF et al.: Pharmacological actions of a novel mixed opiate agonist/antagonist: naloxone benzoylhydrazone. J. PharmacoL Exp. Ther. (1989) 251(2):469–76.
  • IDDB3 reference: HOHLWEG R, PETTERSSON I: Trans-3-(phenoxymethyl)-4-phenylpiperidines - new selective nociceptin antagonists found by HTS. Int. Symp. Pharm. Chem. 2001 3rd:149–150.
  • RONZONI S, PERETTO I, GIARDINA GAM.: Lead generation and lead optimization approaches in the discovery of selective, non-peptide ORL-1 receptor agonists and antagonists. Exp. Opin. Ther. Patents (2001) 11(4):525–546.
  • ••Comprehensive, pre-2001 overview of thereceptor, with discussion of early peptidic and non-peptidic ligands.
  • ZAVERI N: Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL-1: research tools and potential therapeutic agents. Lift Sci. (2003) 73(6):663–678.
  • ••Review with a nice summary of peptideligand SAR, plus a section describing non-peptidic molecules.
  • BARLOCCO D, TOMA L, CIGNARELLA G: Non peptidic ligands at the opioid receptor like-1 (ORL-1). Mini Rev. Med. Chem. (2001) 1:363–375.
  • Drug Data Report (2001) 23(3):317.
  • THOMSEN C, HOHLWEG R: 8-Naphthalen-1-ylmethy1-4-oxo-1-phenyl-1,3,8-triaza-spiro [4.5] dec-3-y1)-acetic acid methyl ester (NNC 63–0532) is a novel potent nociceptin receptor agonist. Br. J. PharmacoL (2000) 131(5):903–908.
  • •Paper describing Novo Nordisk's 1,3,8-triazaspirodecanone agonist.
  • KAWAMOTO H, OZAKI S, ITOH Y et ed.: Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 14(3R,4R)-1-cyclooctylmethy1-3-hydroxymethy1-4-piperidy1]-3-ethyl-1,3-dihydro-2H-benzirniclazol-2-one (J-113397). J. Med. Chem. (1999) 42(25):5061–5063.
  • OZAKI S, KAWAMOTO H, ITOH Y et al.: In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL-1 receptor antagonist. Eur. J. PharmacoL (2000) 402 (1 /2):45–53.
  • •Pharmacology of Banyu-Merck's potent and selective ORL-1 agonist.
  • Drug Data Report (2002) 24(5):403.
  • MARTI M, STOCCHI S, PAGANINI F et al.: Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex. Br. PharmacoL (2003) 138(1):91–98.
  • YAMADA H, NAKAMOTO H, SUZUKI Yet al: Pharmacological profiles of a novel opioid receptor-like-1 (ORL-1) receptor antagonist, JTC-801. Br. J. PharmacoL (2002) 135(2):323–332.
  • •Profile of the former development candidate from Japan Tobacco.
  • MURATINI 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-y1)-2-(4-ethylphenoxymethypbenzamide monohydrochloride. j Pharmacol Exp. Ther. (2002) 303(1):424–430.
  • SHINKAI H, ITO T, IIDA T et al.: 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J. Med. Chem. (2000) 43(24):4667–4677.
  • Drug Data Report (2003) 25 (11): 1001.

Websites

  • http://integrity.prous.com/serylet/xmlxs1/ pk_prod_list.xml_prod_list_card_pr?p_id 253988 Prous Science Integrity
  • http://integrity.prous.com/sery1et/xm1xs1/ pk_prod_list.xml_prod_list_card_pr?p_id 325243 Prous Science Integrity
  • http://integrity.prous.com/serylet/xmbisl/ pk_prod_list.xml_prod_list_card_pr?p_id 336424 Prous Science Integrity
  • http://integrity.prous.com/sery1et/xm1xs1/ pk_prod_list.xml_prod_list_card_pr?p_id 217944 Prous Science Integrity
  • http://integrity.prous.com/serylet/xmbisl/ pk_prod_list.xml_prod_list_card_pr?p_id 297035 Prous Science Integrity

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.