Pain and Therapy, 2020 Buprenorphine is a Schedule III opioid analgesic with unique pharmacodynamic and pharmacokinetic properties that may be preferable to those of Schedule II full μ-opioid receptor agonists.
Jeffrey Gudin, Jeffrey Fudin
doaj +1 more source
Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors
BMC Neuroscience, 2002 Background The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors.
Clark J +3 more
doaj +1 more source
The Use of Computational Approaches in the Discovery and Mechanism Study of Opioid Analgesics
Frontiers in Chemistry, 2020 Opioid receptors that belong to class A G protein-coupled receptors (GPCRs) are vital in pain control. In the past few years, published high-resolution crystal structures of opioid receptor laid a solid basis for both experimental and computational ...
Bangyi Zhao, Wei Li, Lijie Sun, Wei Fu
doaj +1 more source
Chronic morphine treatment attenuates cell growth of human BT474 breast cancer cells by rearrangement of the ErbB signalling network. [PDF]
, 2013 There is increasing evidence that opioid analgesics may interfere with tumour growth. It is currently thought that these effects are mediated by transactivation of receptor tyrosine kinase (RTK)-controlled ERK1/2 and Akt signalling.
Weingaertner, Inka Regine +5 more
core +1 more source
GTPγS-Autoradiography for Studies of Opioid Receptor Functionality
, 2020 The opioid receptors have been an interesting target for the drug industry for decades. These receptors were pharmacologically characterized in the 1970s and several drugs and peptides have emerged over the years.
Alfhild Grönbladh +3 more
core +1 more source
Pharmacological Profiles of Oligomerized μ-Opioid Receptors
Cells, 2013 Opioids are widely prescribed pain relievers with multiple side effects and potential complications. They produce analgesia via G-protein-protein coupled receptors: μ-, δ-, κ-opioid and opioid receptor-like 1 receptors.
Ing-Kang Ho, Cynthia Wei-Sheng Lee
doaj +1 more source
BmK-YA, an enkephalin-like peptide in scorpion venom. [PDF]
PLoS ONE, 2012 By screening extracts of venom from the Asian scorpion Buthus martensii Karsch (BmK) for their abilities to activate opioid receptors, we have identified BmK-YA, an amidated peptide containing an enkephalin-like sequence. BmK-YA is encoded by a precursor
Yan Zhang +5 more
doaj +1 more source
Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.
PLoS ONE, 2014 Inflammation enhances the peripheral analgesic efficacy of opioid drugs, but the mechanisms involved in this phenomenon have not been fully elucidated. Crotalphine (CRP), a peptide that was first isolated from South American rattlesnake C.d.
Vanessa Olzon Zambelli +6 more
doaj +1 more source
The opioid receptor: emergence through millennia of pharmaceutical sciences
Frontiers in Pain Research, 2023 Throughout history humanity has searched for an optimal approach to the use of opioids that maximizes analgesia while minimizing side effects. This review reflects upon the conceptualization of the opioid receptor and the critical role that the ...
Carolyn A. Fairbanks +4 more
doaj +1 more source
Molecular and cellular mechanisms of the age-dependency of opioid analgesia and tolerance
Molecular Pain, 2012 The age-dependency of opioid analgesia and tolerance has been noticed in both clinical observation and laboratory studies. Evidence shows that many molecular and cellular events that play essential roles in opioid analgesia and tolerance are actually age-
Zhao Jing +4 more
doaj +1 more source