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Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists
Yusuke Karasawa+12 more
doaj +1 more source
An opioid-like system regulating feeding behavior in C. elegans [PDF]
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
Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.
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
BmK-YA, an enkephalin-like peptide in scorpion venom. [PDF]
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
Machine-learning Repurposing of DrugBank Compounds for Opioid Use Disorder [PDF]
Opioid use disorder (OUD) is a chronic and relapsing condition that involves the continued and compulsive use of opioids despite harmful consequences. The development of medications with improved efficacy and safety profiles for OUD treatment is urgently needed.
arxiv
Estradiol and Mu opioid-mediated reward: The role of estrogen receptors in opioid use
Opioid use and opioid use disorder are characterized by sex and gender differences, and some of these differences may be mediated by differences in the hormonal milieu within and across individuals.
Sarah B. Ethridge, Mark A. Smith
doaj
Molecular and cellular mechanisms of the age-dependency of opioid analgesia and tolerance
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
BackgroundOpioid receptors are expressed not only by neural cells in the central nervous system, but also by many solid tumor cancer cells. Whether perioperative opioids given for analgesia after tumor resection surgery might inadvertently activate tumor
Amparo Belltall+16 more
doaj +1 more source
Multi-objective Molecular Optimization for Opioid Use Disorder Treatment Using Generative Network Complex [PDF]
Opioid Use Disorder (OUD) has emerged as a significant global public health issue, with complex multifaceted conditions. Due to the lack of effective treatment options for various conditions, there is a pressing need for the discovery of new medications. In this study, we propose a deep generative model that combines a stochastic differential equation (
arxiv
The effects of pioglitazone, a PPARγ receptor agonist, on the abuse liability of oxycodone among nondependent opioid users [PDF]
Aims: Activation of PPARγ by pioglitazone (PIO) has shown some efficacy in attenuating addictive-like responses in laboratory animals. The ability of PIO to alter the effects of opioids in humans has not been characterized in a controlled laboratory ...
Alonzo+74 more
core +1 more source