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Preclinical Studies on Nalfurafine (TRK-820), a Clinically Used KOR Agonist
Nalfurafine has been used clinically in Japan for treatment of itch in kidney dialysis patients and in patients with chronic liver diseases. A...
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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
RationaleCombinations of mu and kappa-opioid receptor (KOR) agonists have been proposed as analgesic formulations with reduced abuse potential. The...
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Modulation of cocaine-related behaviors by low doses of the potent KOR agonist nalfurafine in male C57BL6 mice
RationaleAgonists of the kappa opioid receptor (KOR) have been shown to block the rewarding effects of drugs of abuse, but with negative side...
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Clinical Profiles of Nalfurafine Hydrochloride for the Treatment of Pruritus Patients
Nalfurafine hydrochloride is a selective kappa-opioid agonist that has antipruritic effects. Here we describe the clinical trials for treatment of...
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The kappa-opioid receptor agonist, triazole 1.1, reduces oxycodone self-administration and enhances oxycodone-induced thermal antinociception in male rats
RationaleTriazole 1.1 is a novel kappa-opioid receptor (KOR) agonist reported to produce antinociception without KOR-typical adverse effects. When...
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Effects of kappa opioid receptor agonists on fentanyl vs. food choice in male and female rats: contingent vs. non-contingent administration
RationaleStrategies are needed to decrease the abuse liability of mu opioid receptor (MOR) agonists. One strategy under consideration is to combine...
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Quantification of observable behaviors induced by typical and atypical kappa-opioid receptor agonists in male rhesus monkeys
RationaleKappa-opioid receptor (KOR) agonists are antinociceptive but have side effects that limit their therapeutic utility. New KOR agonists have...
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Kappa opioid agonists reduce oxycodone self-administration in male rhesus monkeys
RationaleCombinations of mu and kappa opioid receptor (KOR) agonists have been proposed as potential analgesic formulations with reduced abuse...
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Antipruritic Effects of Kappa Opioid Receptor Agonists: Evidence from Rodents to Humans
Centrally administered bombesin induces scratching and grooming in rats. These behaviors were blocked by early benzomorphan kappa opioid receptor...
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Novel selective κ agonists SLL-039 and SLL-1206 produce potent antinociception with fewer sedation and aversion
SLL-039 ( N -cyclopropylmethyl-7α−4′-( N ’-benzoyl) amino-phenyl-6,14-endoethano-tetrahydronorthebaine) and SLL-1206 ( N -cyclopropylmethyl-7α−3′-( p -methoxy...
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Unlocking opioid neuropeptide dynamics with genetically encoded biosensors
Neuropeptides are ubiquitous in the nervous system. Research into neuropeptides has been limited by a lack of experimental tools that allow for the...
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Antinociceptive Effects of Kappa-Opioid Receptor Agonists
Preclinical models that assess “pain” in rodents typically measure increases in behaviors produced by a “pain stimulus.” A large literature exists...
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Unique Pharmacology, Brain Dysfunction, and Therapeutic Advancements for Fentanyl Misuse and Abuse
Fentanyl is a fully synthetic opioid with analgesic and anesthetic properties. It has become a primary driver of the deadliest opioid crisis in the...
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Dissociable effects of the kappa opioid receptor agonist nalfurafine on pain/itch-stimulated and pain/itch-depressed behaviors in male rats
RationaleNalfurafine is a G protein signaling-biased kappa opioid receptor (KOR) agonist approved in Japan for second-line treatment of uremic...
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Kappa Opioid Receptor Ligands and Pharmacology: Diphenethylamines, a Class of Structurally Distinct, Selective Kappa Opioid Ligands
The kappa opioid receptor (KOR), a G protein-coupled receptor, and its endogenous ligands, the dynorphins, are prominent members of the opioid...
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Evolution and challenges of opioids in pain management: Understanding mechanisms and exploring strategies for safer analgesics
Opioids traced back to ancient civilizations, have evolved in their usage for acute and chronic pain treatment. Their interaction with the endogenous...
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Peptide Kappa Opioid Receptor Ligands and Their Potential for Drug Development
Ligands for kappa opioid receptors (KOR) have potential uses as non-addictive analgesics and for the treatment of pruritus, mood disorders, and...
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Effects of nalfurafine on the reinforcing, thermal antinociceptive, and respiratory-depressant effects of oxycodone: modeling an abuse-deterrent opioid analgesic in rats
RationaleStrategies to reduce the misuse of mu opioid agonists are critically needed. Previous work has shown that kappa opioid agonists can diminish...
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Kappa Opioid Agonist-Induced Diuresis: Characteristics, Mechanisms, and Beyond
Activation of the kappa opioid receptor (KOR) induces antinociception, anti-pruritic activity, diuresis, sedation, and dysphoria. KOR agonist-induced...
