AI Article Synopsis
- The study identified that the tetrahydroisoquinoline (TIQ) structure is key to activating TRPV1 receptors.
- Six TIQ-fatty acid compounds were created and tested for their ability to mobilize calcium in specific cells.
- Three of these compounds demonstrated partial activation of TRPV1, showing moderate effectiveness compared to capsaicin.
Article Abstract
The SAR of capsazepine revealed that tetrahydroisoquinoline (TIQ) moiety is a core pharmacophore of TRPV1 activity. This implied that conjugates of endogenous TIQs with fatty acids would be active at TRPV1 receptors. Six such compounds were synthesized and tested for calcium mobilization at recombinant TRPV1 receptors overexpressed in HEK293 cells. Three compounds showed partial TRPV1 agonism with EC(50) values in the low micromolar range and maximal efficacies between 25% and 55% of capsaicin.
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| http://dx.doi.org/10.1016/j.bmc.2007.06.032 | DOI Listing |
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