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Novel TRPV1 Modulators with Reduced Pungency Induce Analgesic Effects in Mice

ACS Omega. 2022-01; 
Anny Treat, Vianie Henri, Junke Liu, Joyce Shen, Mauricio Gil-Silva, Alejandro Morales, Avaneesh Rade, Kevin Joseph Tidgewell, Benedict Kolber, Young Shen
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Plasmid DNA Preparation … The plasmid DNA carrying the human TRPV1 coding sequence (GenScript Biotech Corp, Piscataway, NJ) was introduced into Escherichia coli DH5α-competent cells (Invitrogen) to … Get A Quote

摘要

Capsaicin, the compound in hot chili peppers responsible for their pungency and an agonist of the transient receptor potential cation channel, subfamily V, member 1 (TRPV1), has long been known to promote the desensitization of nociceptors at high concentrations. This has led to the utilization and implementation of topical capsaicin cream as an analgesic to treat acute and chronic pain. Critically, the application of capsaicin cream is limited due to capsaicin's high pungency, which is experienced prior to analgesia. To combat this issue, novel capsaicin analogues were developed to provide analgesia with reduced pungency. Analogues reported in this paper add to and show some differences from previous structure... More

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