Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.

@article{Honore2009RepeatedDO,
  title={Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.},
  author={Prisca Honore and Prasant Chandran and Gricelda Hernandez and Donna M. Gauvin and Joseph P. Mikusa and Chengmin M Zhong and Shailen K. Joshi and Joseph R. Ghilardi and Molly A Sevcik and Ryan M. Fryer and Jason A. Segreti and Patricia N Banfor and Kennan Marsh and Torben R. Neelands and Erol K Bayburt and Jerome F Daanen and Arthur R Gomtsyan and C Lee and Michael Kort and Regina M. Reilly and Carol S. Surowy and Philip R. Kym and Patrick W Mantyh and James P. Sullivan and Michael F. Jarvis and Connie R. Faltynek},
  journal={Pain},
  year={2009},
  volume={142 1-2},
  pages={27-35}
}
Transient receptor potential vanilloid type 1 (TRPV1) is a ligand-gated ion channel that functions as an integrator of multiple pain stimuli including heat, acid, capsaicin and a variety of putative endogenous lipid ligands. TRPV1 antagonists have been shown to decrease inflammatory pain in animal models and to produce limited hyperthermia at analgesic doses. Here, we report that ABT-102, which is a potent and selective TRPV1 antagonist, is effective in blocking nociception in rodent models of… CONTINUE READING

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