Flavonoids have been recognized as the active ingredients of many medicinal plant extracts due to interactions with proteins via phenolic groups and low toxicity. Here, we report the investigation of the flavonoid core as a potential new scaffold for the development of opioid receptor ligands. Biological results suggest that stereochemistry of the C2 and C3 positions is important for antagonist activity and selectivity. Our results also suggest that the actions of Hypericum perforatum may be mediated in part by opioid receptors.
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http://dx.doi.org/10.1021/np070194x | DOI Listing |
Front Pharmacol
December 2024
Jiangsu Province Key Laboratory of Anesthesiology, Xuzhou Medical University, Xuzhou, Jiangsu, China.
Introduction: The paraventricular thalamic nucleus (PVT) is recognized for its critical role in pain regulation, yet the precise molecular mechanisms involved remain poorly understood. Here, we demonstrated an essential role of the microglial adenosine A receptor (AR) in the PVT in regulating pain sensation and non-opioid analgesia.
Method And Results: Specifically, AR was predominantly expressed in ionized calcium binding adapter molecule 1 (Iba1)-positive microglia cells within the PVT, with expression levels remaining unchanged in mice experiencing persistent inflammatory pain induced by complete Freund's adjuvant (CFA).
Front Med (Lausanne)
December 2024
Metabolic Disease Research Center, Qazvin University of Medical Sciences, Qazvin, Qazvin, Iran.
Introduction: This study systematically examines the effects of chronic oral methadone use on the glomerular filtration rate (GFR) in patients participating in methadone maintenance therapy (MMT) in Qazvin City, Iran. Methadone, a synthetic -opioid receptor agonist, is predominantly utilized for the management of opioid dependence and pain relief; however, there is growing concern regarding its potential nephrotoxic effects.
Methods: An observational cross-sectional study was executed involving 150 participants who had been on methadone syrup for a minimum duration of 2 years.
Trials
January 2025
Department of Addiction Medicine, Haukeland University Hospital, Bergen, Norway.
Background: There is a lack of knowledge on effective treatment methods for comorbid benzodiazepine dependence in populations undergoing opioid agonist treatment (OAT). Tapering and discontinuation of benzodiazepines has long been considered the standard treatment, even though there is limited evidence for this practice. There is also limited research on benzodiazepine agonist treatment; however, peer and clinical experiences indicate that such approaches may be beneficial for a subgroup of the patients with long-lasting benzodiazepine dependence not responding to other treatment approaches.
View Article and Find Full Text PDFBr J Anaesth
December 2024
Department of Anesthesiology, Daping Hospital, Third Military Medical University (Army Medical University), Chongqing, China. Electronic address:
Background: Recent studies have implicated a role for perioperative medications in determining patient outcomes after surgery for malignant tumours, including relapse and metastasis.
Methods: A combined approach spanned molecular, cellular, and organismal levels, including bioinformatics, immunohistochemical staining of clinical and animal samples, RNA sequencing of glioblastoma multiforme (GBM) cells with Ingenuity Pathway Analysis, lentiviral-mediated gene expression modulation, in vitro cell experiments, and in vivo orthotopic tumour transplantation.
Results: We observed a significant correlation between increased kappa opioid receptor (KOP receptor) expression and better prognosis in patients with glioma.
Nat Commun
December 2024
Department of Biochemistry, Duke University School of Medicine, Durham, NC, 27710, USA.
The current opioid crisis urgently calls for developing non-addictive pain medications. Progress has been slow, highlighting the need to uncover targets with unique mechanisms of action. Extracellular adenosine alleviates pain by activating the adenosine A1 receptor (A1R).
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