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Antagonists of the kappa opioid receptor

Bioorganic & Medicinal Chemistry Letters, 2014
The 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
openaire   +2 more sources

Specific kappa opioid receptor agonists.

Farmaco (Societa chimica italiana : 1989), 2001
The 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

2010
This 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, 1993
Classification 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, 1985
A 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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A review of the kappa opioid receptor system in opioid use

Neuroscience & Biobehavioral Reviews
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
openaire   +2 more sources

PARTICIPATION OF CENTRAL KAPPA-OPIOID RECEPTOR IN ARRHYTHMOGENESIS

Life Sciences, 1997
The 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
openaire   +2 more sources

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