Figure 2.

SB-706375 inhibits [¹²⁵I]hU-II binding to HEK293 membranes stably transfected with mammalian recombinant UT receptors. Membranes isolated from HEK293 cells transfected with the mouse, rat, cat, monkey or human UT receptor were incubated with SB-706375 (0.1 nM–1 μM) and [¹²⁵I]hU-II (0.3 nM) for 60 min at 25°C. Nonlinear regression analysis revealed high-affinity non-cooperative interactions with a single class of binding sites (each point represents the mean of duplicate determinations and is representative of three to six independent experiments; K_is are shown in Table 1).