tolbutamide

Ligand id: 6848

Name: tolbutamide

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 7
Topological polar surface area 83.65
Molecular weight 270.1
XLogP 2.68
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used as an adjunct to diet to lower the blood glucose in diabetes mellitus type 2, where dietary control has failed
Mechanism Of Action and Pharmacodynamic Effects
A sulphonylurea hypoglycemic drug which acts to stimulate insulin sectetion by pancreatic β cells. The sulfonyurea drugs appear to bind sulfonylurea receptors and it has been shown experimentally that tritiated glibenclamide can be used to pull out a 140 kDa protein identified as SUR1 (now known as ABCC8) [4]. SUR2 (ABCC9) has also been identified [1]. However, this is not the full mechanism of action and the functional channel has been characterised as a hetero-octamer formed by four SUR and four Kir6.2 (KCNJ11) subunits, with the Kir6.2 subunits forming the core ion pore and the SUR subunits providing the regulatory properties [3]. Co-expression of Kir6.2 with SUR1, reconstitutes the ATP-dependent K+ conductivity inhibited by the sulfonyureas [1].
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