tolazamide

Ligand id: 6847

Name: tolazamide

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 86.89
Molecular weight 311.13
XLogP 3.19
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 patients with non-insulin dependent diabetes mellitus whose hyperglycemia cannot be satisfactorily controlled by diet alone.
Mechanism Of Action and Pharmacodynamic Effects
A sulphonylurea hypoglycemic agent with actions and uses similar to those of chlorpropamide. 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) [3]. SUR2 (ABCC9) has also been identified [1]. However, this is not the full mechanism of action as the functional channel has been characterised as a hetero-octamer formed by four SUR and four Kir6.2 subunits, with the Kir6.2 (KCNJ11) subunits forming the core ion pore and the SUR subunits providing the regulatory properties [2]. Co-expression of Kir6.2 with SUR1, reconstitutes the ATP-dependent K+ conductivity inhibited by the sulfonyureas [1].
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