ArticleScientific reports2016
Ignavine: a novel allosteric modulator of the μ opioid receptor.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 33 citations in OpenAlex.
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- Novel 1-(1-Arylimiazolin-2-Yl)-3-Arylalkilurea Derivatives with Modulatory Activity on Opioid MOP Receptors.Molecules (Basel, Switzerland) · 2024Article
- Shenfu Injection Mediated NLRP3/Caspase 1 Through (R)-Norcoclaurinee Alleviates Sepsis-Induced Cognitive Dysfunction.Journal of inflammation research · 2024Article
- Modulation of the MOP Receptor (μ Opioid Receptor) by Imidazo[1,2-Molecules (Basel, Switzerland) · 2022Article
- Antinociceptive effect and mechanism of supercritical carbon dioxide extract of Aloysia gratissima leaves in mice.Biomedical journal · 2021Article
- Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling.Journal of natural products · 2021Article
- Oxycodone in the Opioid Epidemic: High 'Liking', 'Wanting', and Abuse Liability.Cellular and molecular neurobiology · 2021Review
- How Aconiti Radix Cocta can Treat Gouty Arthritis Based on Systematic Pharmacology and UPLC-QTOF-MS/MS.Frontiers in pharmacology · 2021Article
- In Vivo Pharmacokinetic Analysis Utilizing Non-Targeted and Targeted Mass Spectrometry and In Vitro Assay against Transient Receptor Potential Channels of Maobushisaishinto and Its Constituent Asiasari Radix.Molecules (Basel, Switzerland) · 2020Article
- Determining Pharmacological Mechanisms of Chinese Incompatible Herbs Fuzi and Banxia in Chronic Obstructive Pulmonary Disease: A Systems Pharmacology-Based Study.Evidence-based complementary and alternative medicine : eCAM · 2020Article
- Insights from molecular dynamics simulations to exploit new trends for the development of improved opioid drugs.Neuroscience letters · 2019Review
- Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.Journal of medicinal chemistry · 2019Review
- Allostery at opioid receptors: modulation with small molecule ligands.British journal of pharmacology · 2018Review
- Recent Advances in the Realm of Allosteric Modulators for Opioid Receptors for Future Therapeutics.ACS chemical neuroscience · 2017Review
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Processed Aconiti tuber (PAT) is used to treat pain associated with various disorders. Although it has been demonstrated that the κ opioid receptor (KOR) signaling pathway is a mediator of the analgesic effect of PAT, active components affecting opioid signaling have not yet been identified. In this study, we explored candidate components of PAT by pharmacokinetic analysis and identified ignavine, which is a different structure from aconitine alkaloids. A receptor binding assay of opioid receptors showed that ignavine specifically binds the μ opioid receptor (MOR), not the KOR. Receptor internalization assay in MOR-expressing cell lines revealed that ignavine augmented the responses produced by D-Ala(2)-N-Me-Phe(4)-Gly-ol(5)-enkephalin (DAMGO), a representative MOR agonist, at a low concentration and inhibited it at a higher concentration. Ignavine also exerted positive modulatory activity for DAMGO, endomorphin-1 and morphine in cAMP assay. Additionally, ignavine alone showed an analgesic effect in vivo. In silico simulation analysis suggested that ignavine would induce a unique structural change distinguished from those induced by a representative MOR agonist and antagonist. These data collectively suggest the possibility that ignavine could be a novel allosteric modulator of the MOR. The present results may open the way for the development of a novel pain management strategy.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.