ArticleBioorganic & medicinal chemistry2008
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
Article in Bioorganic & medicinal chemistry, 2008. 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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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed, 30 citations in OpenAlex.
- Anticancer Activity of Region B Capsaicin Analogs.Journal of medicinal chemistry · 2023Review
- Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia.Nature communications · 2023Article
- Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor.Molecules (Basel, Switzerland) · 2022Article
- De Novo Design of Peptidic Positive Allosteric Modulators Targeting TRPV1 with Analgesic Effects.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2021Article
- Relative Study of Luminescent Properties with Judd-Ofelt Characterization in Trivalent Europium Complexes Comprising ethyl-(4-fluorobenzoyl) Acetate.Journal of fluorescence · 2017Article
- Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels.PloS one · 2017Article
- Molecular Surgery Concept from Bench to Bedside: A Focus on TRPV1+ Pain-Sensing Neurons.Frontiers in physiology · 2017Review
- A chemoselective route to β-enamino esters and thioesters.Organic letters · 2014Article
- Positive allosteric modulation of TRPV1 as a novel analgesic mechanism.Molecular pain · 2012Article
- Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH.The Journal of pharmacology and experimental therapeutics · 2012Article
- The vanilloid agonist resiniferatoxin for interventional-based pain control.Current topics in medicinal chemistry · 2011Review
- Resiniferatoxin for Pain Treatment: An Interventional Approach to Personalized Pain Medicine.The open pain journalArticle
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
Vanilloid agonists such as capsaicin activate ion flux through the TRPV1 channel, a heat- and ligand-gated cation channel that transduces painful chemical or thermal stimuli applied to peripheral nerve endings in skin or deep tissues. We have probed the SAR of a variety of 1,4-dihydropyridine (DHP) derivatives as novel 'enhancers' of TRPV1 activity by examining changes in capsaicin-induced elevations in (45)Ca(2+)-uptake in either cells ectopically expressing TRPV1 or in cultured dorsal root ganglion (DRG) neurons. The enhancers increased the maximal capsaicin effect on (45)Ca(2+)-uptake by typically 2- to 3-fold without producing an action when used alone. The DHP enhancers contained 6-aryl substitution and small alkyl groups at the 1 and 4 positions, and a 3-phenylalkylthioester was tolerated. Levels of free intracellular Ca(2+), as measured by calcium imaging, were also increased in DRG neurons when exposed to the combination of capsaicin and the most efficacious enhancer 23 compared to capsaicin alone. Thus, DHPs can modulate TRPV1 channels in a positive fashion.
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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.