Methods for screening for inhibitors of TRPV2 activation

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Reexamination Certificate

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Reexamination Certificate

active

07915012

ABSTRACT:
The present invention relates to a method for activation of TRPV2 (transient receptor potential vanilloid 2) using probenecid, more precisely a method for selecting a candidate for TRPV2 blocker using probenecid. Probenecid of the present invention works on TRPV2 specifically so that it facilitates the isolation of sensory neurons expressing TRPV2. Therefore, probenecid of the invention can be effectively used for the studies on TRPV2 mechanisms and the development of a TRPV2 based anodyne.

REFERENCES:
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patent: 2010/0137260 (2010-06-01), Hwang et al.
patent: 20072597 (2007-10-01), None
patent: 2007053526 (2007-10-01), None
Behrendt H. et al. Characterization of the Mouse Cold Menthol Receptor TRPM8 . . . British J of Pharmacology 141(4)737-745, Feb. 2, 2004.
Lee S. et al. Sensitization of Vanilloid Receptor Involves an Increase in the Phosphorylated Form of the Channel. Archives of Pharmacal Research 28(4)405-412, 2005.
Hu H. et al. 2-Aminoethoxydiphenyl Borate is a Common Activator of TRPV1, TRPV2 and TRPV3. J of Biological Chemistry 279(34)35741-8, Aug. 20, 2004.
Bang S. et al. “Transient receptor potential V2 expressed in sensory neurons is activated by probenecid”; (Aug. 24, 2007)Neurosci.Lett. 425(2):120-125.
Prosecution history for related application U.S. Appl. No. 12/109,256, 62 pp.
Andrade et al. (Apr. 25, 2006) “Contractile mechanisms coupled to TRPA1 receptor activation in rat urinary bladder” Biochem Pharmacol. 72(1):104-114.
Bandell et al. (Mar. 2004) “Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin” Neuron. 41(6):849-857.
Bang et al. (Oct. 23, 2007) “Transient receptor potential A1 mediates acetaldehyde-evoked pain sensation” Eur. J. Neurosci. 26(9):2516-23.
Trevisani et al. (Aug. 7, 2007) “4-Hydroxynonenal, an endogenous aldehyde, causes pain and neurogenic inflamation through activation of the irritant receptor TRPA1” Proc. Natl. Acad. Sci. U.S.A. 104(33):13519-13524.

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