Use of norgestimate as a selective inhibitor of trpc3, trpc6...

A - Human Necessities – 61 – K

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A61K 31/57 (2006.01) A61P 9/00 (2006.01) A61P 13/12 (2006.01) A61P 29/00 (2006.01) G01N 33/15 (2006.01)

Patent

CA 2702510

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.

L'invention concerne des canaux ioniques TRPC qui sont non sélectifs largement exprimés dans des tissus humains. Ces canaux sont impliqués dans de nombreuses fonctions physiologiques et sont des cibles putatives pour l'élaboration de nouveaux médicaments. Il y a lieu de mieux comprendre les canaux ioniques TRPC dans des cellules et au délà. L'invention concerne en outre un composé pharmacologique qui permet d'étudier les canaux ioniques TRPC du fait de son inhibition discriminative des sous-familles TRPC. En l'occurrence, norgestimate inhibe de manière sélective TRPC3, TRPC6 et TRPC7.

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