The transient receptor potential, subfamily C (TRPC) channels are ubiquitously expressed among cell types and mediate signals in response to phospholipase C (PLC)-coupled receptors[1]. Among the TRPs, the 6 members of the human TRPC subfamily are unique in that they are not only responsible for agonist-activated nonselective cation currents, but they also participate in the so-called slow sustained mode of Ca2+ signaling, which requires sustained elevations of intracellular Ca2+ ([Ca2+]i)[2]. For all organisms, detection and adaptation to cold temperature is crucial to survival. Cold sensing in the innocuous range of cold (>10-15 °C) in the mammalian peripheral nervous system is thought to rely primarily on transient receptor potential (TRP) ion channels, most notably the menthol receptor, TRPM8. The TRP cation channel, subfamily C member 5 (TRPC5), is found to be highly sensitive to cold in the temperature range 37–25 °C, and is thus hypothesized to play a role in sensing cold[3]. Additionally, the channel may have an important role in the pathogenesis of hypertension[4].

[1] J. Soboloff et al. TRPC channels: integrators of multiple cellular signals. Handb Exp Pharmacol. 2007;(179):575-91.
[2] L. Birnbaumer. The TRPC class of ion channels: a critical review of their roles in slow, sustained increases in intracellular Ca(2+) concentrations. Annu Rev Pharmacol Toxicol. 2009;49:395-426.
[3] K. Zimmermann et al. Transient receptor potential cation channel, subfamily C, member 5 (TRPC5) is a cold-transducer in the peripheral nervous system. Proc Natl Acad Sci U S A. 2011 Nov 1;108(44):18114-9.
[4] K.T. Cheng et al. Contribution and regulation of TRPC channels in store-operated Ca2+ entry. Curr Top Membr. 2013;71:149-79.

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3036 BI 749327 Potent, selective and orally bioavailable TRPC6 inhibitor  Recently added €160.00
2458 Clemizole Inhibitor of the transient receptor potential channel TRPC5 €75.00

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