Results 181 to 190 of about 25,455 (216)
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Specific kappa opioid receptor agonists.
Farmaco (Societa chimica italiana : 1989), 2000The results of studies on the design of a heterocyclic scaffold for the dynorphin A pharmacophore and on structure-affinity relationships in the MPCB/CCB series are described. The representative ligands provide insights to binding modes of benzomorphan derivatives to the kappa opioid receptor.
RONSISVALLE, Giuseppe +5 more
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TENA, a selective kappa opioid receptor antagonist
Life Sciences, 1985A number of opioid antagonists (TENA, naloxone, Mr 2266, WIN 44441) were evaluated for their selectivity in antagonizing the effect of mu, kappa, and delta agonists in the guinea pig ileum (GPI) and mouse vas deferens (MVD) preparations. Among these four antagonists, TENA was the most potent and the only ligand which was selective for kappa receptors ...
P S, Portoghese, A E, Takemori
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Journal of Medicinal Chemistry, 1994
2-(3,4-Dichlorophenyl)-N-methyl-N-[1-(3- or 4-substituted phenyl)-2-(1-pyrrolidinyl)ethyl]-acetamides 3-6 were synthesized as kappa-selective affinity labels and evaluated for opioid activity. In smooth muscle preparations, the non-electrophilic parent compound (+)-S-2 and the affinity labels 3-6 behaved as kappa agonists in that they were potently ...
A C, Chang +4 more
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2-(3,4-Dichlorophenyl)-N-methyl-N-[1-(3- or 4-substituted phenyl)-2-(1-pyrrolidinyl)ethyl]-acetamides 3-6 were synthesized as kappa-selective affinity labels and evaluated for opioid activity. In smooth muscle preparations, the non-electrophilic parent compound (+)-S-2 and the affinity labels 3-6 behaved as kappa agonists in that they were potently ...
A C, Chang +4 more
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Kappa Opioid Receptor Endocytosis by Dynorphin Peptides
DNA and Cell Biology, 2000Internalization and downregulation are important steps in the modulation of receptor function. Recent work with the beta2 adrenergic and opioid receptors have implicated these processes in receptor-mediated activation of mitogen-activated protein kinase (MAPK).
B A, Jordan, S, Cvejic, L A, Devi
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Kappa opioid receptor patented
Trends in Pharmacological Sciences, 2001The sequence of the cloned mammalian kappa opioid receptor, a receptor that might play a key role in the development of non-addictive analgesic agents, has been patented by the US-based Adolor Corporation. The exclusive worldwide licence gives Adolor sole access to develop further pharmaceuticals tools aimed at this receptor, as well as related opioid ...
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The FASEB Journal, 2022
Kappa opioid receptor (KOR) agonists produce a variety of beneficial effects such as nonaddictive analgesia and diuresis, but their translation into the clinic has been hindered by central adverse effects (dysphoria). In clinical studies, difelikefalin, a KOR agonist recently FDA approved for treatment of pruritus in hemodialysis patients, was shown to
Jacob Meariman +3 more
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Kappa opioid receptor (KOR) agonists produce a variety of beneficial effects such as nonaddictive analgesia and diuresis, but their translation into the clinic has been hindered by central adverse effects (dysphoria). In clinical studies, difelikefalin, a KOR agonist recently FDA approved for treatment of pruritus in hemodialysis patients, was shown to
Jacob Meariman +3 more
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Expert Opinion on Therapeutic Patents, 2004
For years the design of κ-opioid receptor (KOR) agonists focussed on generating yet more potent and selective ligands that could access the CNS. As it became apparent that this approach was not going to provide analgesics without significant side effects, effort was directed towards the design of peripherally-acting ligands.
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For years the design of κ-opioid receptor (KOR) agonists focussed on generating yet more potent and selective ligands that could access the CNS. As it became apparent that this approach was not going to provide analgesics without significant side effects, effort was directed towards the design of peripherally-acting ligands.
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Kappa Opioid Receptor Function
2010This chapter describes recent developments in the analysis of kappa opioid receptor (KOR) function at a molecular, cellular and systems level within the central and peripheral nervous system. A combination of neuroanatomical, electrophysiological and behavioral techniques have been used to probe the functional consequences of KOR activation in the ...
Julia C. Lemos, Charles Chavkin
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Antinociceptive Effects of Kappa-Opioid Receptor Agonists
2021Preclinical models that assess "pain" in rodents typically measure increases in behaviors produced by a "pain stimulus." A large literature exists showing that kappa opioid receptor (KOR) agonists can decrease these "pain-stimulated behaviors" following many different pain stimuli.
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New kappa opioid receptor from zebrafish Danio rerio
Neuroscience Letters, 2006A cDNA that encodes a kappa opioid receptor like from zebrafish (ZFOR3) has been cloned and characterized. The encoded protein is 377 residues long and presents 70% identity with the mammalian kappa receptors, although less homology is found in the amino- and carboxyl-terminus as well as in the extracellular loops.
Franscisco Alvar, Alvarez +5 more
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