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Background  3-guanidinopropionic acid derivatives reduce body weight in obese, diabetic mice. We have assessed whether one of these analogues, the aminoguanidine carboxylate BVT.12777, opens K ATP  channels in rat insulinoma cells, by the same mechanism as leptin.    Results  BVT.12777 hyperpolarized CRI-G1 rat insulinoma cells by activation of K ATP  channels. In contrast, BVT.12777 did not activate heterologously expressed pancreatic β-cell K ATP  subunits directly. Although BVT.12777 stimulated phosphorylation of MAPK and STAT3, there was no effect on enzymes downstream of PI3K. Activation of K ATP  in CRI-G1 cells by BVT.12777 was not dependent on MAPK or PI3K activity. Confocal imaging showed that BVT.12777 induced a re-organization of cellular actin. Furthermore, the activation of K ATP  by BVT.12777 in CRI-G1 cells was demonstrated to be dependent on actin cytoskeletal dynamics, similar to that observed for leptin.    Conclusions  This study shows that BVT.12777, like leptin, activates K ATP  channels in insulinoma cells. Unlike leptin, BVT.12777 activates K ATP  channels in a PI3K-independent manner, but, like leptin, channel activation is dependent on actin cytoskeleton remodelling. Thus, BVT.12777 appears to act as a leptin mimetic, at least with respect to K ATP  channel activation, and may bypass up-stream signalling components of the leptin pathway.

The aminoguanidine carboxylate BVT.12777 activates ATP-sensitive K+ channels in the rat insulinoma cell line, CRI-G1.