Journal of Medicinal Chemistry
Journal of Medicinal Chemistry
5 years ago

Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1)

Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1)
Peter M. Blumberg, Jeewoo Lee, Amelework D. Habtemichael, Shivaji A. Thorat, Larry V. Pearce, Brienna K. A. Herold, Aeran Jung, Jihyae Ann
Transient receptor potential vanilloid 1 (TRPV1) has emerged as a promising therapeutic target. While radiolabeled resiniferatoxin (RTX) has provided a powerful tool for characterization of vanilloid binding to TRPV1, TRPV1 shows 20-fold weaker binding to the human TRPV1 than to the rodent TRPV1. We now describe a tritium radiolabeled synthetic vanilloid antagonist, 1-((2-(4-(methyl-[3H])piperidin-1-yl-4-[3H])-6-(trifluoromethyl)pyridin-3-yl)methyl)-3-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)urea ([3H]MPOU), that embodies improved absolute affinity for human TRPV1 and improved synthetic accessibility.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00859

DOI: 10.1021/acs.jmedchem.7b00859

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