On the G-protein-coupled receptor heteromers and their allosteric receptor-receptor interactions in the central nervous system: focus on their role in pain modulation [PDF]
, 2013 The modulatory role of allosteric receptor-receptor interactions in the pain pathways of the Central Nervous System and the peripheral nociceptors has become of increasing interest.
Agnati, Luigi F +6 more
core +3 more sources
High-affinity naloxone binding to filamin a prevents mu opioid receptor-Gs coupling underlying opioid tolerance and dependence. [PDF]
PLoS ONE, 2008 Ultra-low-dose opioid antagonists enhance opioid analgesia and reduce analgesic tolerance and dependence by preventing a G protein coupling switch (Gi/o to Gs) by the mu opioid receptor (MOR), although the binding site of such ultra-low-dose opioid ...
Hoau-Yan Wang +2 more
doaj +1 more source
BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates [PDF]
, 2019 © 2019 British Journal of Anaesthesia. Published by Elsevier Ltd. All rights reserved.Background: The marked increase in mis-use of prescription opioids has greatly affected our society. One potential solution is to develop improved analgesics which have
Cami-Kobeci, Gerta +9 more
core +5 more sources
Challenges and new opportunities for detecting endogenous opioid peptides in reward
Addiction Neuroscience, 2022 The endogenous opioid peptide system, comprised of enkephalins, endorphins, dynorphins, and nociceptin, is a highly complex neurobiological system. Opioid peptides are derived from four precursor molecules and undergo several processing events yielding ...
Sineadh M. Conway +2 more
doaj +1 more source
Toxins, 2018 The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer.
Ana C. N. Freitas +11 more
doaj +1 more source
An Engineered Endomorphin-2 Gene for Morphine Withdrawal Syndrome. [PDF]
PLoS ONE, 2016 An optimal therapeutics to manage opioid withdrawal syndrome is desired for opioid addiction treatment. Down-regulation of endogenous endomorphin-2 (EM2) level in the central nervous system after continuous morphine exposure was observed, which suggested
Fei-Xiang Wu +6 more
doaj +1 more source
Frontiers in Pharmacology, 2023 Kappa opioid receptors have exceptional potential as an analgesic target, seemingly devoid of many problematic Mu receptor side-effects. Kappa-selective, small molecule pharmaceutical agents have been developed, but centrally mediated side-effects limit ...
Rink-Jan Lohman +4 more
doaj +1 more source
Opioid peptide-derived analgesics [PDF]
The AAPS Journal, 2005 Two recent developments of opioid peptide-based analgesics are reviewed. The first part of the review discusses the dermorphin-derived, cationic-aromatic tetrapeptide H-Dmt-D-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA, where Dmt indicates 2',6'-dimethyltyrosine), which showed subnanomolar mu receptor binding affinity, extraordinary mu receptor selectivity, and ...
openaire +2 more sources
Synthesis, biological evaluation, and SAR studies of 14β-phenylacetyl substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones derivatives : Ligands with mixed NOP and opioid receptor profile [PDF]
, 2018 © 2018 Kumar, Polgar, Cami-Kobeci, Thomas, Khroyan, Toll and Husbands.A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and ...
Cami-Kobeci +47 more
core +4 more sources
Morphine activates neuroinflammation in a manner parallel to endotoxin [PDF]
, 2012 Opioids create a neuroinflammatory response within the CNS, compromising opioid-induced analgesia and contributing to various unwanted actions. How this occurs is unknown but has been assumed to be via classic opioid receptors.
A. A. Somogyi +42 more
core +2 more sources