Sulfonylurea MOA

This forum made possible through the generous support of SDN members, donors, and sponsors. Thank you.

DPT2DO

Full Member
15+ Year Member
Joined
Sep 22, 2008
Messages
69
Reaction score
1
I'm hoping that someone could clear this up. The Goodman pharm textbook notes in a diagram that sulfonylureas inhibit inward K+ currents into beta-cells, decreasing intracellular K+ concentration and causing depolarization that stimulates insulin release. This doesn't make sense to me, since decreasing intracellular K+ would seemingly hyperpolarize the cell. (I can link the diagram if people don't have access to it, or need to see it)

After researching further via google, other sources state that sulfonylureas (and ATP) block outward K+ current, causing K+ to accumulate, resulting in depolarization. This makes more sense to me, and would seem to be the appropriate trigger to Ca influx and insulin release.

The name of the channel is the ATP-dep K+ channel, and it seems to be composed of 2 subunits - sulfonylurea receptor and K+ inward rectifier. The naming suggests that K+ enters the cell normally, so this further confuses me.

Members don't see this ad.
 
IX72a.png


I learned that the second mechanism you talked about was correct, not the Goodman pharm one.

P.S.The so-called "inward-rectifying potassium channels" have always given me fits.
 
Top