ArticleEuropean journal of medicinal chemistry2019
Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.
Article in European journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 35 citations in OpenAlex.
- Low-intensity focused ultrasound-activated piezoelectric gel bandage for diabetic wound repair and neuropathic pain relief.Nature communications · 2026Article
- Unlocking the Potential of Deep Eutectic Solvents for C-H Activation and Cross-Coupling Reactions: A Review.Molecules (Basel, Switzerland) · 2023Review
- Piperidine Derivatives: Recent Advances in Synthesis and Pharmacological Applications.International journal of molecular sciences · 2023Review
- Bibliometric Analysis of Global Research on Transient Receptor Potential Vanilloid 1 in the Field of Pain.Journal of pain research · 2023Article
- A bibliometrics analysis and visualization study of TRPV1 channel.Frontiers in pharmacology · 2023Review
- Neurophysiological mechanisms of cancer-induced bone pain.Journal of advanced research · 2022Review
- Antioxidative and Analgesic Effects of Naringin through Selective Inhibition of Transient Receptor Potential Vanilloid Member 1.Antioxidants (Basel, Switzerland) · 2021Article
- Virus-CKB: an integrated bioinformatics platform and analysis resource for COVID-19 research.Briefings in bioinformatics · 2021Article
- QSAR Model for Predicting the Cannabinoid Receptor 1 Binding Affinity and Dependence Potential of Synthetic Cannabinoids.Molecules (Basel, Switzerland) · 2020Article
- The Circadian Hormone Melatonin Inhibits Morphine-Induced Tolerance and Inflammation via the Activation of Antioxidative Enzymes.Antioxidants (Basel, Switzerland) · 2020Article
- Lipid Nanoparticle Inclusion Prevents Capsaicin-Induced TRPV1 Defunctionalization.Pharmaceutics · 2020Article
- Two Vanilloid Ligand Bindings Per Channel Are Required to Transduce Capsaicin-Activating Stimuli.Frontiers in molecular neuroscience · 2019Article
Corrections and comments
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Authors and funding
14 authors at 4 institutions in 3 countries.
Funding
Abstract
In order to discover a novel type of analgesic, we investigated dual activity ligands with TRPV1 antagonism and mu-opioid receptor affinity with the goal of eliciting synergistic analgesia while avoiding the side effects associated with single targeting. Based on a combination approach, a series of 4-benzyl-4-(dimethylamino)piperidinyl analogues were designed, synthesized and evaluated for their receptor activities. Among them, compound 49 exhibited the most promising dual-acting activity toward TRPV1 and the mu-opioid receptor in vitro. In vivo,49 displayed potent, dose-dependent antinociceptive activity in both the 1st and 2nd phases in the formalin assay. Consistent with its postulated mechanism, we confirmed that in vivo, as in vitro, compound 49 both antagonized TRPV1 and functioned as a mu-opioid agonist. This result indicates that dual-acting TRPV1 antagonist/mu-opioid ligands can be made and represent a new and promising class of analgesic.
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Registered trials
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.