Biological Activity
Selective inositol triphosphate receptor type 1 (ITPR1) potentiator for wild-type as well as two ITPR1 SCA29 mutantsR269W or T267M.
ARN11391 is a selective inositol triphosphate receptor type 1 (ITPR1)but not ITPR2 or ITPR3potentiator (open channel probability (Po) = 0.2 with 20 μM ARN11391 and <0.01 without by on-nucleus nuclear patch-clamp using TPR1-YFP-expressing HEK293 cells) th at potenitates IP3- (by photolysis of caged IP3) and UPT-induced calcium increase in HEK293 transfectants expressing wild-type as well as ITPR1 SCA29 mutantsR269W or T267M (5 μM UTP with or without 10 μM ARN11391).
