KATP opener (β-cell)
Pancreatic β-cell KATP channel opener (Kir6.2/SUR1)
- Hyperpolarization stops calcium entry → no insulin release
- Exactly the channel sulfonylureas CLOSE — reciprocal mechanisms, reciprocal glucose effects
- Used to RAISE glucose: hyperinsulinemic hypoglycemia, insulinoma
- Opens Kir6.2/SUR1 KATP channels in the pancreatic beta cell → the membrane hyperpolarizes → voltage-gated calcium entry stops → insulin is not released
- Exactly the channel the sulfonylureas CLOSE — the two mechanisms are reciprocal, and so are their glucose effects
- Used to RAISE glucose: hyperinsulinemic hypoglycemia, insulinoma
Drugs with this mechanism (1)
- Diazoxide — KATP channel OPENER that shuts off insulin release; the mirror image of a sulfonylurea.
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