Results 231 to 240 of about 83,214 (263)
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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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Novel opioid peptides as kappa opioid receptor antagonists
2006Our 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 +2 more
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Delta and kappa opioid receptors in eyestalk ganglia of a crustacean
Brain Research, 1997Crustacean eyestalk ganglia are part of the protocerebrum and have been demonstrated to produce numerous neurohormones. 3H(2-D-Pen, 5-D-Pen)-enkephalin, 3H-(-)-ethylketocyclazocine and 3H(D-Ala2-NMePhe-Glyol5)-enkephalin were used as ligands for opioid receptors on neuronal membrane preparations of eyestalk ganglia under consideration of their ...
J, Hanke +3 more
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Potent and Selective Indolomorphinan Antagonists of the Kappa-Opioid Receptor
Journal of Medicinal Chemistry, 2000The indole moiety in the delta-opioid antagonist, naltrindole (2, NTI), was employed as a scaffold to hold an "address" for interaction with the kappa-opioid receptor. The attachment of the address to the 5'-position of the indole moiety was based on superposition of NTI upon the kappa antagonist, norbinaltorphimine (1, norBNI).
W C, Stevens +5 more
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The contribution of serotonin 1A receptors to kappa opioid immunosuppression
Neuroscience and Behavioral Physiology, 2009Activation of kappa opioid receptors (kappa-OR) with the selective agonist rimorphin (0.1 mg/kg) produced marked suppression of the immune response in CBA mice. This effect was not seen on administration of rimorphin on the background of a reduction in the activity of the serotoninergic (5-HTergic) system resulting from stimulation of presynaptic (8-OH-
M A, Cheido, G V, Idova
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Molecular recognition at kappa opioid receptors
Pure and Applied Chemistry, 2001Abstract 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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Kappa opioid receptors as modulators of novelty processing
Neuropsychopharmacology, 2023Kathryn Braden, Daniel C. Castro
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Kappa-opioid receptors and analgesia.
Trends in pharmacological sciences, 1990Over the past decade, opioids have attracted great attention. One important reason for this is the need for novel, strong analgesics free of the abuse potential and side-effects of narcotics such as morphine. Because morphine acts at mu-opioid receptors, efforts have been made to characterize analgesia mediated by non-mu sites, in particular kappa ...
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Agonist-induced regulation and trafficking of $kappa; opioid receptors
Life Sciences, 2004Chronic or repeated administration of kappa opioid agonists leads to tolerance to the subsequent drug administration. The mechanisms underlying tolerance are complex and changes at the receptor level contribute in part to the development of tolerance.
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Studies on Ligands of the Kappa Opioid Receptor
2016This thesis is comprised of three parts. In the first part, we investigated zyklophin, a novel selective short-acting kappa opioid receptor (KOPR) antagonist, and its effects on scratching behaviors in Swiss-Webster mice. We investigated whether zyklophin was able to induce scratching in a dose-dependent fashion, and whether this scratching behavior ...
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