Preclinical Studies on Nalfurafine (TRK-820), a Clinically Used KOR Agonist.

No abstract is available for this paper.

• Publication year

  2021

• Venue

  Handbook of Experimental Pharmacology

• Publication date

  2021-04-09

• Fields of study

  Medicine

• Identifiers
  DOI 10.1007/164_2021_443PMID 33834276PMCID PMC9249371
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• The kappa-opioid receptor agonist, nalfurafine, blocks acquisition of oxycodone self-administration and oxycodone’s conditioned rewarding effects in male rats

  2020cited by this paper
• Drug Addiction: Hyperkatifeia/Negative Reinforcement as a Framework for Medications Development

  2020cited by this paper
• Quantification of observable behaviors induced by typical and atypical kappa-opioid receptor agonists in male rhesus monkeys

  2020cited by this paper
• Modulation of cocaine-related behaviors by low doses of the potent KOR agonist nalfurafine in male C57BL6 mice

  2020cited by this paper
• mTORC1 pathway is involved in the kappa opioid receptor activation-induced increase in excessive alcohol drinking in mice.

  2020cited by this paper
• Nalfurafine modulates the reinforcing effects of oxycodone in male and female adolescent C57BL/6J mice.

  2020cited by this paper
• Comparison of Pharmacological Properties between the Kappa Opioid Receptor Agonist Nalfurafine and 42B, Its 3-Dehydroxy Analogue: Disconnect between in Vitro Agonist Bias and in Vivo Pharmacological Effects.

  2020cited by this paper
• Kappa opioid agonists reduce oxycodone self-administration in male rhesus monkeys

  2020cited by this paper
• Kappa opioid receptors in the bed nucleus of the stria terminalis regulate binge-like alcohol consumption in male and female mice.

  2020cited by this paper
• Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

  2020cited by this paper
• Kappa opioid receptor and dynorphin signaling in the central amygdala regulates alcohol intake

  2019cited by this paper
• Signaling properties of structurally diverse kappa opioid receptor ligands: towards in vitro models of in vivo responses.

  2019cited by this paper
• Clinically utilized kappa-opioid receptor agonist nalfurafine combined with low-dose naltrexone prevents alcohol relapse-like drinking in male and female mice.

  2019cited by this paper
• Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine

  2019cited by this paper
• Combination of Clinically Utilized Kappa-Opioid Receptor Agonist Nalfurafine With Low-Dose Naltrexone Reduces Excessive Alcohol Drinking in Male and Female Mice.

  2019cited by this paper
• In vivo brain GPCR signaling elucidated by phosphoproteomics

  2018cited by this paper
• Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor.

  2018cited by this paper
• Post-marketing surveillance study of the safety and efficacy of nalfurafine hydrochloride (Remitch® capsules 2.5 μg) in 3,762 hemodialysis patients with intractable pruritus

  2018cited by this paper
• Kappa Opioid Receptor Distribution and Function in Primary Afferents.

  2018cited by this paper
• Phosphoproteomic approach for agonist-specific signaling in mouse brains: mTOR pathway is involved in κ opioid aversion

  2018cited by this paper
• Dissociable effects of the kappa opioid receptor agonist nalfurafine on pain/itch-stimulated and pain/itch-depressed behaviors in male rats

  2017cited by this paper
• Role of the Dynorphin/Kappa Opioid Receptor System in the Motivational Effects of Ethanol.

  2017cited by this paper
• Effects of nalfurafine on the reinforcing, thermal antinociceptive, and respiratory-depressant effects of oxycodone: modeling an abuse-deterrent opioid analgesic in rats

  2017cited by this paper
• Nalfurafine is a G-protein biased agonist having significantly greater bias at the human than rodent form of the kappa opioid receptor.

  2017cited by this paper
• Topical nalfurafine exhibits anti-inflammatory and anti-pruritic effects in a murine model of AD.

  2016cited by this paper
• The G Protein–Biased κ-Opioid Receptor Agonist RB-64 Is Analgesic with a Unique Spectrum of Activities In Vivo

  2015cited by this paper
• Supersensitive Kappa Opioid Receptors Promotes Ethanol Withdrawal-Related Behaviors and Reduce Dopamine Signaling in the Nucleus Accumbens

  2015cited by this paper
• Pharmacology and anti‐addiction effects of the novel κ opioid receptor agonist Mesyl Sal B, a potent and long‐acting analogue of salvinorin A

  2015cited by this paper
• Effects of Intrathecal &kgr;-Opioid Receptor Agonist on Morphine-Induced Itch and Antinociception in Mice

  2015cited by this paper
• Nalfurafine suppresses pruritogen- and touch-evoked scratching behavior in models of acute and chronic itch in mice.

  2015cited by this paper
• The one-two punch of alcoholism: role of central amygdala dynorphins/kappa-opioid receptors.

  2014cited by this paper
• Essential structure of the κ opioid receptor agonist nalfurafine for binding to the κ receptor.

  2014cited by this paper
• Assessment of the kappa opioid agonist, salvinorin A, as a punisher of drug self-administration in monkeys

  2014cited by this paper
• Dynorphin Acts as a Neuromodulator to Inhibit Itch in the Dorsal Horn of the Spinal Cord

  2014cited by this paper
• Different alcohol exposures induce selective alterations on the expression of dynorphin and nociceptin systems related genes in rat brain

  2013cited by this paper
• Effects of voluntary alcohol drinking on corticotropin-releasing factor and preprodynorphin mRNA levels in the central amygdala of Sardinian alcohol-preferring rats.

  2013cited by this paper
• Efficacy and Safety of a Novel ĸ-Agonist for Managing Intractable Pruritus in Dialysis Patients

  2012cited by this paper
• Effects of corticotropin-releasing hormone receptor antagonists on the ethanol-induced increase of dynorphin A1-8 release in the rat central amygdala.

  2011cited by this paper
• Effect of a novel kappa-receptor agonist, nalfurafine hydrochloride, on severe itch in 337 haemodialysis patients: a Phase III, randomized, double-blind, placebo-controlled study.

  2010cited by this paper
• Effect of kappa-opioid receptor agonists U69593, U50488H, spiradoline and salvinorin A on cocaine-induced drug-seeking in rats.

  2009cited by this paper
• Comparison of the diuretic effects of chemically diverse kappa opioid agonists in rats: nalfurafine, U50,488H, and salvinorin A

  2009cited by this paper
• Nalfurafine prevents 5'-guanidinonaltrindole- and compound 48/80-induced spinal c-fos expression and attenuates 5'-guanidinonaltrindole-elicited scratching behavior in mice.

  2009cited by this paper
• Effects of Atypical κ-Opioid Receptor Agonists on Intrathecal Morphine-Induced Itch and Analgesia in Primates

  2009cited by this paper
• Nalfurafine hydrochloride: a new drug for the treatment of uremic pruritus in hemodialysis patients.

  2009cited by this paper
• Micro/kappa opioid interactions in rhesus monkeys: implications for analgesia and abuse liability.

  2008cited by this paper
• [Effect of TRK-820, a selective kappa opioid receptor agonist, on scratching behavior in an animal model of atopic dermatitis].

  2008cited by this paper
• Stress-Induced p38 Mitogen-Activated Protein Kinase Activation Mediates κ-Opioid-Dependent Dysphoria

  2007cited by this paper
• Stress-induced p38 mitogen-activated protein kinase activation mediates kappa-opioid-dependent dysphoria.

  2007cited by this paper
• Nalfurafine, a kappa opioid receptor agonist, inhibits scratching behavior secondary to cholestasis induced by chronic ethynylestradiol injections in rats.

  2006cited by this paper
• A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist.

  2006cited by this paper
• Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.

  2005cited by this paper
• Spontaneous scratching behavior in MRL/lpr mice, a possible model for pruritus in autoimmune diseases, and antipruritic activity of a novel kappa-opioid receptor agonist nalfurafine hydrochloride.

  2005cited by this paper
• Comparison of Pharmacological Activities of Three Distinct κ Ligands (Salvinorin A, TRK-820 and 3FLB) on κ Opioid Receptors in Vitro and Their Antipruritic and Antinociceptive Activities in Vivo

  2005cited by this paper
• Nalmefene Induced Elevation in Serum Prolactin in Normal Human Volunteers: Partial Kappa Opioid Agonist Activity?

  2005cited by this paper
• Suppression of Acute Herpetic Pain-Related Responses by the κ-Opioid Receptor Agonist (-)-17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-3-trans-3-(3-furyl) Acrylamido] Morphinan Hydrochloride (TRK-820) in Mice

  2004cited by this paper
• Inhibitory effects of TRK-820 on systemic skin scratching induced by morphine in rhesus monkeys.

  2004cited by this paper
• Kappa opioid agonists suppress chloroquine-induced scratching in mice.

  2004cited by this paper
• Possible pharmacotherapy of the opioid kappa receptor agonist for drug dependence.

  2004cited by this paper
• Possible Pharmacotherapy of the Opioid κ Receptor Agonist for Drug Dependence

  2004cited by this paper
• Motivational properties of kappa and mu opioid receptor agonists studied with place and taste preference conditioning

  2004cited by this paper
• Suppression of acute herpetic pain-related responses by the kappa-opioid receptor agonist (-)-17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-beta-[n-methyl-3-trans-3-(3-furyl) acrylamido] morphinan hydrochloride (TRK-820) in mice.

  2004cited by this paper
• Involvement of central μ-opioid system in the scratching behavior in mice, and the suppression of it by the activation of κ-opioid system

  2003cited by this paper
• Involvement of central mu-opioid system in the scratching behavior in mice, and the suppression of it by the activation of kappa-opioid system.

  2003cited by this paper
• Effects of a newly synthesized κ-opioid receptor agonist, TRK-820, on the discriminative stimulus and rewarding effects of cocaine in rats

  2002cited by this paper
• Effects of bremazocine on self-administration of smoked cocaine base and orally delivered ethanol, phencyclidine, saccharin, and food in rhesus monkeys: a behavioral economic analysis.

  2002cited by this paper
• Antipruritic activity of the kappa-opioid receptor agonist, TRK-820.

  2002cited by this paper
• Antipruritic activity of the κ-opioid receptor agonist, TRK-820

  2002cited by this paper
• Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans

  2001cited by this paper
• The selective κ-opioid receptor agonist U50,488H attenuates voluntary ethanol intake in the rat

  2001cited by this paper
• The novel kappa-opioid receptor agonist TRK-820 suppresses the rewarding and locomotor-enhancing effects of morphine in mice.

  2001cited by this paper
• TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys.

  2001cited by this paper
• The selective kappa-opioid receptor agonist U50,488H attenuates voluntary ethanol intake in the rat.

  2001cited by this paper
• The novel kappa-opioid receptor agonist TRK-820 has no affect on the development of antinociceptive tolerance to morphine in mice.

  2000cited by this paper
• Characterization of the antinociceptive effects of TRK-820 in the rat.

  2000cited by this paper
• A novel kappa-opioid receptor agonist, TRK-820, blocks the development of physical dependence on morphine in mice.

  2000cited by this paper
• Potent antinociceptive effects of TRK-820, a novel κ-opioid receptor agonist

  1999cited by this paper
• Pharmacological properties of TRK-820 on cloned mu-, delta- and kappa-opioid receptors and nociceptin receptor.

  1999cited by this paper
• Pharmacological properties of TRK-820 on cloned μ-, δ- and κ-opioid receptors and nociceptin receptor

  1999cited by this paper
• Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.

  1999cited by this paper
• Discovery of a structurally novel opioid kappa-agonist derived from 4,5-epoxymorphinan.

  1998cited by this paper
• Effects of kappa opioid agonists on cocaine- and food-maintained responding by rhesus monkeys.

  1998cited by this paper
• Analgesic efficacy of enadoline versus placebo or morphine in postsurgical pain.

  1996cited by this paper
• In-vivo studies on kappa opioid receptors

  1986cited by this paper
• Differential effects of mu and kappa opioid systems on motivational processes.

  1986cited by this paper
• Psychotomimesis mediated by kappa opiate receptors

  1986cited by this paper
• U-50,488: a selective and structurally novel non-Mu (kappa) opioid agonist.

  1983cited by this paper
• Locomotor activity and antinociception after putative mu, kappa and sigma opioid receptor agonists in the rat: influence of dopaminergic agonists and antagonists.

  1981cited by this paper

• κ-opioid receptor: from analgesic target to neuroimmune hub

  2026cites this paper
• Biased Kappa-opioid Agonist Strategies in Pain Management: Approaches to Clinical Benefits with Reduced Adverse Effects

  2026influential citation
• SLL-023ACP, a KOR/MOR dual agonist, produces potent antinociception with fewer side effects.

  2026cites this paper
• Structure-activity relationship of N-cyclopropylmethyl-7α-(m-methylaminophenyl)-6,14-endoethano-northebaine derivatives as G-protein-biased KOR-selective agonists.

  2026cites this paper
• Triazole 187 is a biased KOR agonist that suppresses itch without sedation and induces anxiolytic-like behaviors in mice

  2025cites this paper
• Determinants of drug effects in preclinical assays of pain-related behavioral depression: Considerations for analgesic drug development.

  2025cites this paper
• Opioid receptors in GtoPdb v.2025.3

  2025cites this paper
• Structure-Activity Relationship of N-Cyclopropylmethyl-7α-[para-(arylcarboxamido)phenyl]-6,14-endoethano-tetrahydronorthebaines as Potent and Selective Kappa Opioid Receptor Agonists.

  2025cites this paper
• KOR agonists for the treatment and/or prevention of opioid use disorder and cocaine use disorder.

  2025cites this paper
• Diagnosis and Management of Keppen-Lubinsky Syndrome in a Lebanese Infant: A Case Report

  2025cites this paper
• Kappa opioids inhibit spinal output neurons to suppress itch

  2024cites this paper
• NCP, a Dual Kappa and mu Opioid Receptor Agonist, Is a Potent Analgesic Against Inflammatory Pain without Reinforcing or Aversive Properties

  2024cites this paper
• Systematic Structure–Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments

  2024cites this paper
• Emerging GPCR targets for AUD: Insights from preclinical studies.

  2024cites this paper
• Effects of Selective and Mixed-Action Kappa and Delta Opioid Receptor Agonists on Pain-Related Behavioral Depression in Mice

  2024cites this paper
• Preclinical evaluation of abuse potential of the peripherally-restricted kappa opioid receptor agonist HSK21542.

  2024cites this paper
• Contingent administration of typical and biased kappa opioid agonists reduces cocaine and oxycodone choice in a drug vs. food choice procedure in male rhesus monkeys

  2023cites this paper
• Identification of a convergent spinal neuron population that encodes itch

  2023cites this paper
• Quantification of observable behaviors following oral administration of oxycodone and nalfurafine in male rhesus monkeys.

  2023cites this paper
• Agonist-Promoted Phosphorylation and Internalization of the Kappa Opioid Receptor in Mouse Brains: Lack of Connection With Conditioned Place Aversion

  2022cites this paper
• The G-protein biased kappa opioid agonists, triazole 1.1 and nalfurafine, produce non-uniform behavioral effects in male rhesus monkeys.

  2022cites this paper
• Nalfurafine Hydrochloride, a κ-Opioid Receptor Agonist, Induces Melanophagy via PKA Inhibition in B16F1 Cells

  2022cites this paper
• Signaling underlying kappa opioid receptor-mediated behaviors in rodents

  2022cites this paper
• Peptide Kappa Opioid Receptor Ligands and Their Potential for Drug Development.

  2021cites this paper