Results 191 to 200 of about 25,455 (216)

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, L N, Maslov, D S, Ugdyzhekova, G N, Smagin   +3 more
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Arylacetamides as peripherally restricted kappa opioid receptor agonists

Bioorganic & Medicinal Chemistry Letters, 2000
Analogues of the kappa (kappa) opioid receptor agonist, ICI 199441, were prepared. Ki values for these analogues at the cloned human kappa opioid receptor ranged from 0.058 to 25 nM. Trifluoromethylaryl derivatives were potent analgesics when administered subcutaneously in the rat and were more peripherally restricted than the parent compound, ICI ...
V, Kumar, M A, Marella, L, Cortes-Burgos, A C, Chang, J A, Cassel, J D, Daubert, R N, DeHaven, D L, DeHaven-Hudkins, S L, Gottshall, E, Mansson, A L, Maycock   +10 more
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Kappa-opioid receptor modulation of nicotine-induced behaviour

Neuropharmacology, 2000
The ability of kappa-opioid receptor ligands to modulate dependence-related behavioural effects of drugs like morphine and cocaine is well documented. The present study examined the effects of kappa-opioid agonists on nicotine-induced locomotor stimulation in rats chronically pre-exposed to nicotine (0.4 mg/kg/day). U50,488 [0.5-3 mg/kg subcutaneously (
Hahn, B, Stolerman, I P, Shoaib, M
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Novel opioid peptides as kappa opioid receptor antagonists

2006
Our laboratory is interested in identifying potent and selective peptide antagonists for opioid receptors and in exploring the structure-activity relationships for antagonist activity at these receptors. We have designed potential antagonists for receptors using the “message-address” concept [1] by combining small peptides with opioid antagonist ...
Jane V. Aldrich, Qiang Wan, Murray F. Thomas   +2 more
openaire   +1 more source

Kappa Opioid Receptor Ligands and Pharmacology: Diphenethylamines, a Class of Structurally Distinct, Selective Kappa Opioid Ligands

2021
The kappa opioid receptor (KOR), a G protein-coupled receptor, and its endogenous ligands, the dynorphins, are prominent members of the opioid neuromodulatory system. The endogenous kappa opioid system is expressed in the central and peripheral nervous systems, and has a key role in modulating pain in central and peripheral neuronal circuits and a wide
Mariana, Spetea, Helmut, Schmidhammer
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Morphine Upregulates Kappa-opioid Receptors of Human Lymphocytes

2006
Opioids such as morphine are potent analgesic and addictive compounds. Chronic morphine use also induces immunomodulatory and immunosuppressive effects, as especially evident in HIV-infected patients. Morphine acts on the immune cells primarily through its binding to mu-opioid receptors on the plasma membrane.
S, Suzuki, T K, Chuang, L F, Chuang, R H, Doi, R Y, Chuang   +4 more
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Molecular recognition at kappa opioid receptors

Pure and Applied Chemistry, 2001
Abstract Structure­activity relationships are rarely straightforward, and often are more complicated than they appear. For this reason, the use of site-directed mutagenesis as a complementary tool to analyze structure­activity relationships has been invaluable.
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Nicotine withdrawal and κ-opioid receptors

Psychopharmacology, 2009
The synthesis and release of dynorphin are increased in the caudate/putamen (CPU) and nucleus accumbens (NAc) of nicotine-withdrawn mice, suggesting a role in the nicotine abstinence syndrome.This study aims to investigate the consequences of enhanced dynorphinergic activity on kappa-opioid receptor (KOPr) expression, coupling, and function in CPU and ...
Michael J, McCarthy, Hailing, Zhang, Norton H, Neff, Maria, Hadjiconstantinou   +3 more
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Buprenorphine has potent kappa opioid receptor antagonist activity

Neuropharmacology, 1987
Buprenorphine was studied for its effects on urinary output to determine if it was an agonist, partial agonist, or antagonist at the kappa receptor. Buprenorphine was a potent antagonist of bremazocine-induced urination and had no kappa agonist activity.
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In-vivo studies on kappa opioid receptors

Trends in Pharmacological Sciences, 1986
Abstract The actions of opioids are mediated by multiple types of opioid receptor. As a result, ‘obtaining the right balance' is the catchphrase most frequently heard these days in analgesic research laboratories throughout the pharmaceutical industry.
Cowan, Alan, Gmerek, Debra E.
openaire   +2 more sources