Results 211 to 220 of about 71,106 (270)

Kappa Opioid Receptor Antagonists as Potential Therapeutics for Stress-Related Disorders.

Annual Review of Pharmacology and Toxicology, 2020
Exposure to stressful stimuli activates kappa opioid receptor (KOR) signaling, a process known to produce aversion and dysphoria in humans and other species. This endogenous opioid system is dysregulated in stress-related disorders, specifically in major
Moriah L. Jacobson, C. Browne, I. Lucki
semanticscholar   +1 more source

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

Signaling properties of structurally diverse kappa opioid receptor ligands: towards in vitro models of in vivo responses.

ACS Chemical Neuroscience, 2019
Biased ligands preferentially activate certain signaling pathways downstream of their target receptor, leading to differential physiological or behavioral responses downstream.
Amelia D. Dunn   +4 more
semanticscholar   +1 more source

Specific kappa opioid receptor agonists.

Farmaco (Societa chimica italiana : 1989), 2000
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
openaire   +3 more sources

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
openaire   +2 more sources

Involvement of dynorphin and the kappa opioid receptor in feeding

Peptides, 1983
Dynorphin-(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
openaire   +2 more sources

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
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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