Figure 5.
SB-706375 is a competitive antagonist of hU-II-induced [Ca2+]i-mobilization (FLIPR) in HEK293 cells stably expressing the (a) mouse, (b) rat, (c) monkey or (d) human UT receptor. Concentration–response curves to hU-II (10 pM–3.3 μM for mouse and monkey UT receptors, 30 pM–10 μM for rat and human UT receptors) were rightward-shifted in a parallel manner by SB-706375 (0.1–30 μM) without any significant suppression of the maximal response to hU-II consistent with competitive antagonism (n=3).