Results 41 to 50 of about 2,577,172 (407)
British Journal of Pharmacology, 2018 PZM21 is a novel μ‐opioid receptor ligand that has been reported to induce minimal arrestin recruitment and be devoid of the respiratory depressant effects characteristic of classical μ receptor ligands such as morphine.
R. Hill +8 more
semanticscholar +1 more source
Pharmacology Research & Perspectives, 2022 Morphine is frequently applied in cancer patients for pain management. However, its effects on cancer are not well understood but observed to be specific to certain cancer types. We previously revealed the stimulatory properties of morphine in esophageal
Zhengwen Yu +3 more
doaj +1 more source
Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence [PDF]
, 2010 Internalisation of the mu opioid receptor from the surface of cells is generally achieved by receptor occupancy with agonist ligands of high efficacy. However, in many situations the potent analgesic morphine fails to promote internalisation effectively ...
Lopez-Gimenez, J.F., Milligan, G.
core +2 more sources
Structural insights into μ-opioid receptor activation
Nature, 2015 Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X-ray crystal structure of the murine μOR bound to the morphinan ...
Weijiao Huang +17 more
semanticscholar +1 more source
Molecules, 2020 Achieving effective pain management is one of the major challenges associated with modern day medicine. Opioids, such as morphine, have been the reference treatment for moderate to severe acute pain not excluding chronic pain modalities.
Abdelfattah Faouzi +2 more
doaj +1 more source
Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]
, 2013 Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Birkás, Erika +12 more
core +3 more sources
Science Signaling, 2018 High-efficacy opioids enhance receptor desensitization due to rapid and sustained GRK2/β-arrestin interactions. Controlling opioid receptor desensitization Chronic opioid use leads to tolerance and the need for increasing doses to achieve pain relief ...
E. Miess +13 more
semanticscholar +1 more source
Receptors for morphine and opioids
General Pharmacology: The Vascular System, 1976 Two points concerning enzymatic systems acting on disposal of morphine are discussed, namely the multiplicity of glucuronyltransferase and the effect of nalorphine on N-demethylation of morphine. Evidences of the presence of at least two different glucuronyltransferases in microsomes of rat liver, kidney and intestine are presented. These evidences are
Sánchez, Emílio +2 more
openaire +4 more sources
Butorphanol: Effects of a Prototypical Agonist-Antagonist Analgesic on κ-Opioid Receptors
Journal of Pharmacological Sciences, 2005 The opioid analgesic, butorphanol (17-cyclobutylmethyl-3,14-dihydroxymorphinan) tartrate is a prototypical agonist-antagonist opioid analgesic agent whose potential for abuse has been the cause of litigation in the United States.
Stephen Commiskey +3 more
doaj +1 more source
An opioid-like system regulating feeding behavior in C. elegans [PDF]
, 2015 Neuropeptides are essential for the regulation of appetite. Here we show that neuropeptides could regulate feeding in mutants that lack neurotransmission from the motor neurons that stimulate feeding muscles. We identified nlp-24 by an RNAi screen of 115
Artyukhin, Alexander B. +3 more
core +3 more sources