Synonyms: tolazolamide | Tolinase®
tolazamide is an approved drug (FDA (1986))
Compound class:
Synthetic organic
Comment: A sulfonylurea family drug inhibiting sulfonylurea receptor 1 (ABCC8)/Kir6.2 (KCNJ11) potassium channel activity.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
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]. |
External links |
For extended ADME data see the following: Drugs.com |