Results 181 to 190 of about 1,463,708 (228)
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Expert Opinion on Therapeutic Patents, 2004
For years the design of κ-opioid receptor (KOR) agonists focussed on generating yet more potent and selective ligands that could access the CNS. As it became apparent that this approach was not going to provide analgesics without significant side effects, effort was directed towards the design of peripherally-acting ligands.
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For years the design of κ-opioid receptor (KOR) agonists focussed on generating yet more potent and selective ligands that could access the CNS. As it became apparent that this approach was not going to provide analgesics without significant side effects, effort was directed towards the design of peripherally-acting ligands.
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The Journal of Pharmacology and Experimental Therapeutics, 1997
Receptor binding studies and electrophysiological studies demonstrated the existence of at least two kappa opioid receptors, which have been designated kappa-1 and kappa-2. Several agonists and antagonists are selective for the kappa-1 receptor whereas no known ligands are selective for the kappa-2 receptor. In this study, the kappa opioid GR89,696 was
R M, Caudle, A J, Mannes, M J, Iadarola
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Receptor binding studies and electrophysiological studies demonstrated the existence of at least two kappa opioid receptors, which have been designated kappa-1 and kappa-2. Several agonists and antagonists are selective for the kappa-1 receptor whereas no known ligands are selective for the kappa-2 receptor. In this study, the kappa opioid GR89,696 was
R M, Caudle, A J, Mannes, M J, Iadarola
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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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Antinociceptive Effects of Kappa-Opioid Receptor Agonists
2021Preclinical models that assess "pain" in rodents typically measure increases in behaviors produced by a "pain stimulus." A large literature exists showing that kappa opioid receptor (KOR) agonists can decrease these "pain-stimulated behaviors" following many different pain stimuli.
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In-vivo studies on kappa opioid receptors
Trends in Pharmacological Sciences, 1986Abstract 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.
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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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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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Kappa opioid receptors as modulators of novelty processing
Neuropsychopharmacology, 2023Kathryn Braden, Daniel C. Castro
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Kappa Opioid Receptor Antagonists as Potential Therapeutics for Stress-Related Disorders
Annual Review of Pharmacology and Toxicology, 2020Caroline A Browne, Irwin Lucki
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