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A review of the kappa opioid receptor system in opioid use [PDF]
The kappa opioid receptor (KOR) system is implicated in dysphoria and as an "anti-reward system" during withdrawal from opioids. However, no clear consensus has been made in the field, as mixed findings have been reported regarding the relationship between the KOR system and opioid use.
Salih Cayir +7 more
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Antagonists of the kappa opioid receptor
Bioorganic & Medicinal Chemistry Letters, 2014The research community has increasingly focused on the development of OPRK antagonists as pharmacotherapies for the treatment of depression, anxiety, addictive disorders and other psychiatric conditions produced or exacerbated by stress. Short-acting OPRK antagonists have been recently developed as a potential improvement over long-acting prototypic ...
Mariangela, Urbano +3 more
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Specific kappa opioid receptor agonists.
Farmaco (Societa chimica italiana : 1989), 2001The 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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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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The kappa-opioid receptor: Evidence for the different subtypes
Life Sciences, 1993Classification of drugs acting on the kappa-opioid receptors seems to be difficult, since some of these ligands are also sigma agonists and/or display non-opioid actions as well. Furthermore, certain benzomorphans having kappa-agonistic character, are shown to be mu-antagonists too.
M, Wollemann, S, Benyhe, J, Simon
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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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PARTICIPATION OF CENTRAL KAPPA-OPIOID RECEPTOR IN ARRHYTHMOGENESIS
Life Sciences, 1997The effect of kappa receptors agonists and antagonists was studied in the model of epinephrine induced arrhythmias. Kappa receptor agonists U-50,488 and [D-Ala2]-Dynorphin A (1-13) administered I.C.V. potentiate the arrhythmogenic effect of epinephrine.
Y B, Lishmanov +3 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 beta 2 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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Involvement of dynorphin and the kappa opioid receptor in feeding
Peptides, 1983Dynorphin-(1-17) produces a highly specific increase in food ingestion. Similar enhancement of food ingestion is found with dynorphin fragments (1-10), (1-11), (1-13) and (3-13) but not with (1-8) and (1-9). Dynorphin B (rimorphin) also enhances food intake.
J E, Morley, A S, Levine
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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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