these different GIRK channels would have been desired, but its low potency (around 5 μM) limited further studies. Furthermore, the authors observed off-target activity on ATP-gated Kir6.1/SUR2a and Kir6.1/SUR2b channels [45]. Nonetheless, the discovery of VU0529331 represents the first step in the development of GIRK1-lacking channels activators, such as homomeric GIRK2 or GIRK2/GIRK3, and could provide new insights into the role of these channels in addiction. Future SAR studies and chemical optimization of VU0529331 should be performed to achieve these goals.
