Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population.

@article{Tth2004DesignOA,
  title={Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population.},
  author={Attila L. T{\'o}th and Peter M. Blumberg and Zili Chen and Alan P. Kozikowski},
  journal={Molecular pharmacology},
  year={2004},
  volume={65 2},
  pages={282-91}
}
We describe the synthesis and characterization of N-(4-chlorobenzyl) -N'-(4-hydroxy-3-iodo-5-methoxybenzyl)thiourea (IBTU), a novel antagonist of the vanilloid receptor 1 (TRPV1 or VR1). IBTU competitively inhibited 45Ca2+ uptake into CHO cells heterologously expressing rat TRPV1, whether induced by capsaicin or resiniferatoxin (Ki = 99 +/- 23 and 93 +/- 34 nM, respectively). IBTU was thus somewhat more potent (5-fold) than capsazepine. In contrast to its antagonism of vanilloid-induced calcium… CONTINUE READING

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