Na channels, disease, and related assays and compositions

Details Na channels, disease, and related assays and compositions Na channels, disease, and related assays and compositions

C - Chemistry, Metallurgy

07

D

C07D 233/76 (2006.01) A61K 31/165 (2006.01) A61K 31/404 (2006.01) A61K 31/4164 (2006.01) C07C 51/09 (2006.01) C07C 59/58 (2006.01) C07C 213/02 (2006.01) C07D 209/14 (2006.01) C12Q 1/68 (2006.01) G01N 33/574 (2006.01) G01N 33/58 (2006.01) G01N 33/68 (2006.01) C07C 217/46 (2006.01)

Patent

CA 2734322

Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.

L'invention concerne des molécules et leur synthèse, destinées à être utilisées pour bloquer des canaux ioniques à bornes comme des canaux sodiques sensibles à la tension (VGSC) et des canaux de sodium à tension de prostate (PVSC). Ces inhibiteurs ont une efficacité de blocage supérieure, par exemple lors du déplacement du ligand radioactif [3H]-batrachotoxine-B ([3H]-BTX-B) qui se lie au site 2 d'un VGSC. Les molécules de l'invention comprennent un fragment qui augmente la fiabilité de liaison de molécules pour le site de liaison de protéine dans des cellules du cancer de la prostate (PC), et qui est également fluorescent. Dans un mode de réalisation, les molécules de l'invention sont un système d'inhibition qui peut être utilisé pour cibler des VGSC surabondants ou hyperactifs sélectivement dans la douleur, l'épilepsie ou le cancer de la prostate, en inhibant la prolifération de PC. Le fragment fluorescent facilite également un criblage, un suivi et des études pharmacodynamiques du médicament dans un échantillon biologique, in vitro et in vivo.

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