The therapeutic potential of nociceptin/orphanin FQ receptor agonists as analgesics without abuse liability.

PubWeight™: 0.94‹?›

🔗 View Article (PMC 3582300)

Published in ACS Chem Neurosci on November 06, 2012

Authors

Ann P Lin1, Mei-Chuan Ko

Author Affiliations

1: Department of Psychology, School of Arts and Sciences, University of Pittsburgh , Pittsburgh, PA 15260, USA.

Associated clinical trials:

Nociceptin Concentration in Synovial Fluid and Plasma | NCT02528916

Articles citing this

Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. J Med Chem (2016) 1.10

Functional plasticity of the N/OFQ-NOP receptor system determines analgesic properties of NOP receptor agonists. Br J Pharmacol (2014) 0.97

Small-molecule nociceptin receptor agonist ameliorates mast cell activation and pain in sickle mice. Haematologica (2015) 0.93

Differential effects of opioid-related ligands and NSAIDs in nonhuman primate models of acute and inflammatory pain. Psychopharmacology (Berl) (2013) 0.87

Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain. J Pharmacol Exp Ther (2013) 0.86

Supraspinal actions of nociceptin/orphanin FQ, morphine and substance P in regulating pain and itch in non-human primates. Br J Pharmacol (2015) 0.86

Central N/OFQ-NOP Receptor System in Pain Modulation. Adv Pharmacol (2015) 0.82

The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor. Structure (2015) 0.81

Novel mixed NOP/MOP agonist BU08070 alleviates pain and inhibits gastrointestinal motility in mouse models mimicking diarrhea-predominant irritable bowel syndrome symptoms. Eur J Pharmacol (2014) 0.81

A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates. Proc Natl Acad Sci U S A (2016) 0.80

Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain. J Med Chem (2016) 0.79

Spinal antinociceptive effects of the novel NOP receptor agonist PWT2-nociceptin/orphanin FQ in mice and monkeys. Br J Pharmacol (2015) 0.78

Distinct functions of opioid-related peptides and gastrin-releasing peptide in regulating itch and pain in the spinal cord of primates. Sci Rep (2015) 0.78

Effects of the NOP agonist SCH221510 on producing and attenuating reinforcing effects as measured by drug self-administration in rats. Eur J Pharmacol (2014) 0.77

Neuraxial opioid-induced itch and its pharmacological antagonism. Handb Exp Pharmacol (2015) 0.75

Pharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist. Pharmacol Res Perspect (2016) 0.75

Altered expression of glial markers, chemokines, and opioid receptors in the spinal cord of type 2 diabetic monkeys. Biochim Biophys Acta (2016) 0.75

Articles cited by this

Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor. Nature (1995) 6.72

Orphanin FQ: a neuropeptide that activates an opioidlike G protein-coupled receptor. Science (1995) 5.74

ORL1, a novel member of the opioid receptor family. Cloning, functional expression and localization. FEBS Lett (1994) 3.78

The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov (2007) 3.39

International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev (2005) 3.33

Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature (2012) 2.96

Intrathecal and epidural administration of opioids. Anesthesiology (1984) 2.91

Anatomy of CNS opioid receptors. Trends Neurosci (1988) 2.82

Curbing the opioid epidemic in the United States: the risk evaluation and mitigation strategy (REMS). JAMA (2012) 2.50

Opioid-induced constipation: challenges and therapeutic opportunities. Am J Gastroenterol (2011) 2.17

Regional distribution of opiate receptor binding in monkey and human brain. Nature (1973) 2.02

Dose-response pharmacology of intrathecal morphine in human volunteers. Anesthesiology (1993) 2.01

Pharmacology of nociceptin and its receptor: a novel therapeutic target. Br J Pharmacol (2000) 1.97

Risk factors for drug dependence among out-patients on opioid therapy in a large US health-care system. Addiction (2010) 1.95

75 years of opioid research: the exciting but vain quest for the Holy Grail. Br J Pharmacol (2006) 1.91

Comparison of responses of warm and nociceptive C-fiber afferents in monkey with human judgments of thermal pain. J Neurophysiol (1978) 1.90

The molecular and behavioral pharmacology of the orphanin FQ/nociceptin peptide and receptor family. Pharmacol Rev (2001) 1.86

The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential. Nat Rev Drug Discov (2008) 1.85

The development of a comprehensive risk-management program for prescription opioid analgesics: researched abuse, diversion and addiction-related surveillance (RADARS). Pain Med (2007) 1.70

Buprenorphine-induced antinociception is mediated by mu-opioid receptors and compromised by concomitant activation of opioid receptor-like receptors. J Neurosci (2003) 1.59

A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat. Proc Natl Acad Sci U S A (2000) 1.57

In vivo characterization of 6beta-naltrexol, an opioid ligand with less inverse agonist activity compared with naltrexone and naloxone in opioid-dependent mice. J Pharmacol Exp Ther (2005) 1.54

Current knowledge of buprenorphine and its unique pharmacological profile. Pain Pract (2010) 1.53

The orphan opioid receptor and its endogenous ligand--nociceptin/orphanin FQ. Trends Pharmacol Sci (1997) 1.44

Problems and concerns of patients receiving chronic opioid therapy for chronic non-cancer pain. Pain (2010) 1.42

Methylnaltrexone: treatment for opioid-induced constipation. Am J Hosp Palliat Care (2010) 1.41

Increase by the ORL1 receptor (opioid receptor-like1) ligand, nociceptin, of inwardly rectifying K conductance in dorsal raphe nucleus neurones. Br J Pharmacol (1996) 1.40

Agonist-induced regulation and trafficking of kappa opioid receptors. Life Sci (2004) 1.36

Prescription opioid abuse in chronic pain: a review of opioid abuse predictors and strategies to curb opioid abuse. Pain Physician (2012) 1.35

The role of central mu opioid receptors in opioid-induced itch in primates. J Pharmacol Exp Ther (2004) 1.33

The effect of nociceptin on Ca2+ channel current and intracellular Ca2+ in the SH-SY5Y human neuroblastoma cell line. Br J Pharmacol (1996) 1.31

Behavioral effects of the delta-selective opioid agonist SNC80 and related compounds in rhesus monkeys. J Pharmacol Exp Ther (1998) 1.31

Neuraxial opioid-induced pruritus: a review. J Clin Anesth (2003) 1.27

Comparing the subjective, psychomotor and physiological effects of intravenous buprenorphine and morphine in healthy volunteers. J Pharmacol Exp Ther (1997) 1.26

Dose-response relationship of intrathecal morphine for postcesarean analgesia. Anesthesiology (1999) 1.26

Kappa opioids in rhesus monkeys. I. Diuresis, sedation, analgesia and discriminative stimulus effects. J Pharmacol Exp Ther (1987) 1.25

Acquisition, expression, and reinstatement of ethanol-induced conditioned place preference in mice: effects of opioid receptor-like 1 receptor agonists and naloxone. J Pharmacol Exp Ther (2003) 1.25

The direct and indirect costs of opioid-induced constipation. J Pain Symptom Manage (2010) 1.23

Economic costs of nonmedical use of prescription opioids. Clin J Pain (2011) 1.22

An experimental itch model in monkeys: characterization of intrathecal morphine-induced scratching and antinociception. Anesthesiology (2000) 1.21

Nociceptin or antinociceptin: potent spinal antinociceptive effect of orphanin FQ/nociceptin in the rat. Neuroreport (1996) 1.19

The value of nonhuman primates in drug abuse research. Exp Clin Psychopharmacol (2007) 1.19

Behavioral effects of a synthetic agonist selective for nociceptin/orphanin FQ peptide receptors in monkeys. Neuropsychopharmacology (2009) 1.18

Behavioral effects of the systemically active delta opioid agonist BW373U86 in rhesus monkeys. J Pharmacol Exp Ther (1994) 1.17

Antinociceptive effects of nociceptin/orphanin FQ administered intrathecally in monkeys. J Pain (2009) 1.14

Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist. Eur J Pharmacol (2004) 1.12

Effects of intravenous ketamine, alfentanil, or placebo on pain, pinprick hyperalgesia, and allodynia produced by intradermal capsaicin in human subjects. Pain (1995) 1.12

Intracisternal nor-binaltorphimine distinguishes central and peripheral kappa-opioid antinociception in rhesus monkeys. J Pharmacol Exp Ther (1999) 1.08

Effects of intrathecally administered nociceptin/orphanin FQ in monkeys: behavioral and mass spectrometric studies. J Pharmacol Exp Ther (2006) 1.07

Roles of μ-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates. J Pharmacol Exp Ther (2012) 1.07

Activation of kappa-opioid receptors inhibits pruritus evoked by subcutaneous or intrathecal administration of morphine in monkeys. J Pharmacol Exp Ther (2003) 1.05

Long-lasting antinociceptive spinal effects in primates of the novel nociceptin/orphanin FQ receptor agonist UFP-112. Pain (2009) 1.05

Pathophysiology and management of opioid-induced pruritus. Drugs (2007) 1.05

Norbinaltorphimine, a selective kappa-opioid receptor antagonist, induces an itch-associated response in mice. Eur J Pharmacol (2001) 1.05

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) 1.05

Characterization of scratching responses in rats following centrally administered morphine or bombesin. Behav Pharmacol (2003) 1.05

Nociceptin/orphanin FQ receptor activation attenuates antinociception induced by mixed nociceptin/orphanin FQ/mu-opioid receptor agonists. J Pharmacol Exp Ther (2009) 1.04

Inhibition by nociceptin of neurogenic inflammation and the release of SP and CGRP from sensory nerve terminals. Br J Pharmacol (1997) 1.03

Naloxone benzoylhydrazone (NalBzoH) analgesia. J Pharmacol Exp Ther (1990) 1.03

Antiallodynic effects of loperamide and fentanyl against topical capsaicin-induced allodynia in unanesthetized primates. J Pharmacol Exp Ther (2004) 1.02

A novel delta opioid agonist, BW373U86, in squirrel monkeys responding under a schedule of shock titration. J Pharmacol Exp Ther (1993) 1.01

The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510). J Pharmacol Exp Ther (2008) 1.01

Inhibition of tachykinin release from peripheral endings of sensory nerves by nociceptin, a novel opioid peptide. Br J Pharmacol (1996) 1.00

The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mouse models of acute pain and cocaine-induced reward. J Pharmacol Exp Ther (2010) 1.00

Analgesic effect of intrathecally administered nociceptin, an opioid receptor-like1 receptor agonist, in the rat formalin test. Neuroscience (1997) 0.99

Effects of nociceptin/orphanin FQ receptor (NOP) agonist, Ro64-6198, on reactivity to acute pain in mice: comparison to morphine. Eur J Pharmacol (2007) 0.97

Alfentanil, but not amitriptyline, reduces pain, hyperalgesia, and allodynia from intradermal injection of capsaicin in humans. Anesthesiology (1997) 0.94

Brain and whole-body imaging of nociceptin/orphanin FQ peptide receptor in humans using the PET ligand 11C-NOP-1A. J Nucl Med (2012) 0.94

Effects of butorphanol on morphine-induced itch and analgesia in primates. Anesthesiology (2007) 0.94

Studies of micro-, kappa-, and delta-opioid receptor density and G protein activation in the cortex and thalamus of monkeys. J Pharmacol Exp Ther (2003) 0.94

Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates. J Pharmacol Exp Ther (2008) 0.94

In vitro and in vivo studies on UFP-112, a novel potent and long lasting agonist selective for the nociceptin/orphanin FQ receptor. Peptides (2007) 0.93

Spinally delivered nociceptin/orphanin FQ reduces flinching behaviour in the rat formalin test. Neuroreport (1997) 0.92

Opioids, ventilation and acute pain management. Anaesth Intensive Care (2011) 0.92

Species comparison and pharmacological characterization of human, monkey, rat, and mouse TRPA1 channels. J Pharmacol Exp Ther (2012) 0.92

Differential in vivo potencies of naltrexone and 6beta-naltrexol in the monkey. J Pharmacol Exp Ther (2005) 0.92

δ-Opioid mechanisms for ADL5747 and ADL5859 effects in mice: analgesia, locomotion, and receptor internalization. J Pharmacol Exp Ther (2012) 0.91

Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. J Med Chem (2011) 0.91

Intrathecal opioids for combined spinal-epidural analgesia during labour. CNS Drugs (2003) 0.91

Brain and whole-body imaging in rhesus monkeys of 11C-NOP-1A, a promising PET radioligand for nociceptin/orphanin FQ peptide receptors. J Nucl Med (2011) 0.90

Effects of E-2078, a stable dynorphin A(1-8) analog, on sedation and serum prolactin levels in rhesus monkeys. Psychopharmacology (Berl) (1999) 0.90

Nociceptin-induced scratching, biting and licking in mice: involvement of spinal NK1 receptors. Br J Pharmacol (1999) 0.90

Reverse physiology: discovery of the novel neuropeptide, orphanin FQ/nociceptin. Crit Rev Neurobiol (1998) 0.89

The nociceptin/orphanin FQ receptor (NOP) as a target for drug abuse medications. Curr Top Med Chem (2011) 0.89

The effects of nociceptin/orphanin FQ receptor agonist Ro 64-6198 and diazepam on antinociception and remifentanil self-administration in rhesus monkeys. Psychopharmacology (Berl) (2010) 0.89

Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. Biochem Pharmacol (2009) 0.89

[Dmt1]N/OFQ(1-13)-NH2: a potent nociceptin/orphanin FQ and opioid receptor universal agonist. Br J Pharmacol (2013) 0.88

Antinociceptive actions of BW373U86 in the mouse. J Pharmacol Exp Ther (1993) 0.86

Recently patented and promising ORL-1 ligands: where have we been and where are we going? Expert Opin Ther Pat (2010) 0.85

The orphanin receptor agonist RO 64-6198 does not induce place conditioning in rats. Neuroreport (2002) 0.84

Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids. Bioorg Med Chem (2007) 0.84

Naloxone benzylhydrazone is a µ-selective opioid antagonist without kappa agonist effects in rhesus monkeys. Behav Pharmacol (1992) 0.82

Homology modeling and molecular dynamics simulations of the active state of the nociceptin receptor reveal new insights into agonist binding and activation. Proteins (2012) 0.82

The detection and perceived intensity of noxious thermal stimuli in monkey and in human. J Neurophysiol (1989) 0.81

UFP-112 a potent and long-lasting agonist selective for the Nociceptin/Orphanin FQ receptor. CNS Neurosci Ther (2010) 0.81

Opioids in preclinical and clinical trials. Top Curr Chem (2011) 0.80

The primate as a model for the human temperature-sensing system: 1. Adapting temperature and intensity of thermal stimuli. Somatosens Res (1985) 0.77

Buprenorphine self-administration by the baboon: comparison with other opioids. NIDA Res Monogr (1983) 0.77

Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther (2007) 0.76

Articles by these authors

Most efficient cocaine hydrolase designed by virtual screening of transition states. J Am Chem Soc (2008) 2.33

Thermostable variants of cocaine esterase for long-time protection against cocaine toxicity. Mol Pharmacol (2008) 1.60

Design, preparation, and characterization of high-activity mutants of human butyrylcholinesterase specific for detoxification of cocaine. Mol Pharmacol (2010) 1.48

Cocaine esterase prevents cocaine-induced toxicity and the ongoing intravenous self-administration of cocaine in rats. J Pharmacol Exp Ther (2009) 1.19

Structural analysis of thermostabilizing mutations of cocaine esterase. Protein Eng Des Sel (2010) 1.10

Central kappa-opioid receptor-mediated antidepressant-like effects of nor-Binaltorphimine: behavioral and BDNF mRNA expression studies. Eur J Pharmacol (2007) 1.09

Roles of μ-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates. J Pharmacol Exp Ther (2012) 1.07

Long-lasting effects of a PEGylated mutant cocaine esterase (CocE) on the reinforcing and discriminative stimulus effects of cocaine in rats. Neuropsychopharmacology (2011) 1.06

Long-lasting antinociceptive spinal effects in primates of the novel nociceptin/orphanin FQ receptor agonist UFP-112. Pain (2009) 1.05

The role of central gastrin-releasing peptide and neuromedin B receptors in the modulation of scratching behavior in rats. J Pharmacol Exp Ther (2011) 1.00

Amelioration of the cardiovascular effects of cocaine in rhesus monkeys by a long-acting mutant form of cocaine esterase. Neuropsychopharmacology (2011) 0.98

Effects of butorphanol on morphine-induced itch and analgesia in primates. Anesthesiology (2007) 0.94

Subunit stabilization and polyethylene glycolation of cocaine esterase improves in vivo residence time. Mol Pharmacol (2011) 0.89

The effects of nociceptin/orphanin FQ receptor agonist Ro 64-6198 and diazepam on antinociception and remifentanil self-administration in rhesus monkeys. Psychopharmacology (Berl) (2010) 0.89

Effects of mu, kappa, and delta opioid receptor agonists on the function of hypothalamic-pituitary-adrenal axis in monkeys. Psychoneuroendocrinology (2008) 0.89

Physiological function of gastrin-releasing peptide and neuromedin B receptors in regulating itch scratching behavior in the spinal cord of mice. PLoS One (2013) 0.88

PEGylation of bacterial cocaine esterase for protection against protease digestion and immunogenicity. J Control Release (2009) 0.88

Effects of a long-acting mutant bacterial cocaine esterase on acute cocaine toxicity in rats. Drug Alcohol Depend (2011) 0.87

Differential effects of opioid-related ligands and NSAIDs in nonhuman primate models of acute and inflammatory pain. Psychopharmacology (Berl) (2013) 0.87

Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain. J Pharmacol Exp Ther (2013) 0.86

The spinal antinociceptive effects of endomorphins in rats: behavioral and G protein functional studies. Anesth Analg (2008) 0.84

Electrospray sample deposition for matrix-assisted laser desorption/ionization (MALDI) and atmospheric pressure MALDI mass spectrometry with attomole detection limits. Rapid Commun Mass Spectrom (2004) 0.84

Repeated administration of a mutant cocaine esterase: effects on plasma cocaine levels, cocaine-induced cardiovascular activity, and immune responses in rhesus monkeys. J Pharmacol Exp Ther (2012) 0.83

The fate of bacterial cocaine esterase (CocE): an in vivo study of CocE-mediated cocaine hydrolysis, CocE pharmacokinetics, and CocE elimination. J Pharmacol Exp Ther (2011) 0.82

Pharmacokinetic evidence for the long-lasting effect of nor-binaltorphimine, a potent kappa opioid receptor antagonist, in mice. Neurosci Lett (2013) 0.80

Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther (2007) 0.76