Results 221 to 230 of about 71,106 (270)
Some of the next articles are maybe not open access.
Kappa Opioid Receptor Endocytosis by Dynorphin Peptides
DNA and Cell Biology, 2000Internalization and downregulation are important steps in the modulation of receptor function. Recent work with the beta2 adrenergic and opioid receptors have implicated these processes in receptor-mediated activation of mitogen-activated protein kinase (MAPK).
B A, Jordan, S, Cvejic, L A, Devi
openaire +2 more sources
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
openaire +2 more sources
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
openaire +2 more sources
Kappa opioid receptor patented
Trends in Pharmacological Sciences, 2001The sequence of the cloned mammalian kappa opioid receptor, a receptor that might play a key role in the development of non-addictive analgesic agents, has been patented by the US-based Adolor Corporation. The exclusive worldwide licence gives Adolor sole access to develop further pharmaceuticals tools aimed at this receptor, as well as related opioid ...
openaire +1 more source
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.
openaire +1 more source
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.
openaire +1 more source
Kappa Opioid Receptor Function
2010This 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
openaire +1 more source
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.
openaire +2 more sources
The role of kappa opioid receptors in immune system – An overview
European Journal of Pharmacology, 2022Opioids are one of the most effective anti-nociceptive agents used in patients with cancer pain or after serious surgery in most countries. The endogenous opioid system participates in pain perception, but recently its role in inflammation was determined.
Adrian Szczepaniak +3 more
openaire +2 more sources
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.
openaire +2 more sources
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
openaire +2 more sources
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
openaire +2 more sources
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
openaire +1 more source