Abstract: TRPC ion channels are non-selective channels widely expressed in human tissues. These channels are involved in numerous physiological functions and are putative targets for the development of novel medicines. There is a need to gain a better understanding of TRPC ion channels in cells and beyond. The present invention provides a pharmacological tool compound that allows to study TRPC ion channels due to its discriminating inhibition of TRPC subfamilies. In the present invention, norgestimate is shown to selectively inhibit TRPC3, TRPC6 and TRPC7.

Abstract: TRPC ion channels are non-selective channels widely expressed in human tissues. These channels are involved in numerous physiological functions and are putative targets for the development of novel medicines. There is a need to gain a better understanding of TRPC ion channels in cells and beyond. The present invention provides a pharmacological tool compound that allows to study TRPC ion channels due to its discriminating inhibition of TRPC subfamilies. In the present invention, norgestimate is shown to selectively inhibit TRPC3, TRPC6 and TRPC7.

Abstract: The present invention relates to an isolated complex comprising a first protein comprising or consisting of a classical transient receptor potential channel (TRPC) or a functionally active variant thereof and a second protein comprising or consisting of the first spectrin (Spec 1) domain of SEC14 and spectrin domains 1 (SESTD1), a test system comprising the first protein and the second protein as well as means for detecting interaction of the first and the second protein, a method for screening for a TRPC modulator using the system and the use of the test system for the identification of a TRPC modulator.