ArticleBritish journal of pharmacology2014
Effect of chirality and lipophilicity in the functional activity of evodiamine and its analogues at TRPV1 channels.
Article in British journal of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 23 citations in OpenAlex.
- Activation of human and mouse transient receptor potential vanilloid 1 by enantiomeric evodiamine and rutaecarpine.Journal of natural medicines · 2026Article
- The Novel TRPV1 Agonist ST-6631 Improves Swallowing Function in Rat Models of Stroke-Related Dysphagia and Demonstrates Pharmaceutical Advantage Over Capsaicin, by Exhibiting Minimal Pungent and Irritant Properties.Pharmacology research & perspectives · 2026Article
- Indole-2-Carboxamide as an Effective Scaffold for the Design of New TRPV1 Agonists.Molecules (Basel, Switzerland) · 2025Article
- Evodiamine: A Extremely Potential Drug Development Candidate of Alkaloids fromInternational journal of nanomedicine · 2024Review
- Evodiamine-inspired dual inhibitors of histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2) with potent antitumor activity.Acta pharmaceutica Sinica. B · 2020Article
- Antiproliferative Effects of Alkaloid Evodiamine and Its Derivatives.International journal of molecular sciences · 2018Review
- Anticancer Activity of Natural and Synthetic Capsaicin Analogs.The Journal of pharmacology and experimental therapeutics · 2018Review
- The pharmacology of TRP channels.British journal of pharmacology · 2014Article
Corrections and comments
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Authors and funding
7 authors at 6 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeEvodiamine, a racemic quinazolinocarboline alkaloid isolated from the traditional Chinese medicine Evodiae fructus, has been reported to act as an agonist of the transient receptor potential vanilloid type-1 (TRPV1) cation channel both in vitro and in vivo. Evodiamine is structurally different from all known TRPV1 activators, and has significant clinical potential as a thermogenic agent. Nevertheless, the molecular bases for its actions are still poorly understood. EXPERIMENTAL APPROACH: To investigate the structure-activity relationships of evodiamine, the natural racemate was resolved, and a series of 23 synthetic analogues was prepared, using as the end point the intracellular Ca(2+) elevation in HEK-293 cells stably overexpressing either the human or the rat recombinant TRPV1. KEY
resultsS-(+) evodiamine was more efficacious and potent than R-(-) evodiamine, and a new potent lead (Evo30) was identified, more potent than the reference TRPV1 agonist, capsaicin. In general, potency and efficacy correlated with the lipophilicity of the analogues. Like other TRPV1 agonists, several synthetic analogues could efficiently desensitize TRPV1 to activation by capsaicin. CONCLUSIONS AND IMPLICATIONS: Evodiamine qualifies as structurally unique lead structure to develop new potent TRPV1 agonists/desensitizers.
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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.