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The Sound of Evolution
Tolbutamide
Mechanism of action:
Tolbutamide is a sulfonylurea derivative. Tolbutamide binds to and inhibits sulfonylurea receptor 1 on the membrane of pancreatic beta cells. This receptor is the regulatory subunit of the ATP-sensitive potassium channel. When tolbutamide inhibits this receptor, potassium efflux decreases, causing membrane depolarization. Depolarization then opens calcium channels, increasing calcium influx and promoting insulin release.
Reference(s):
Zhou SF et al. (2009). Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem.
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