Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.

J Nat Prod

Division of Medicinal & Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA.

Published: August 2007

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.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2265593PMC
http://dx.doi.org/10.1021/np070194xDOI Listing

Publication Analysis

Top Keywords

opioid receptor
8
receptor ligands
8
flavonoids opioid
4
ligands identification
4
identification preliminary
4
preliminary structure-activity
4
structure-activity relationships
4
relationships flavonoids
4
flavonoids recognized
4
recognized active
4

Similar Publications

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).

View Article and Find Full Text PDF

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.

View Article and Find Full Text PDF

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 PDF

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.

View Article and Find Full Text PDF

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).

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!