Synonyms: Diabenese® | Glucamide®
chlorpropamide is an approved drug (FDA (1958))
Compound class:
Synthetic organic
Comment: A sulfonylurea family drug inhibiting sulfonylurea receptor 1 (ABCC8)/Kir6.2 (KCNJ11)
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. |
Summary of Clinical Use |
An oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus |
Mechanism Of Action and Pharmacodynamic Effects |
Like other sulfonylureas this compound 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]. The functional β-cell channel has been characterised as a hetero-octamer formed by four SUR1 and four Kir6.2 subunits, with the Kir6.2 subunits forming the core ion pore and the SUR1 subunits providing the regulatory properties [3]. Co-expression of Kir6.2 with SUR1 reconstitutes the ATP-dependent K+ conductivity inhibited by the sulfonyureas [2]. |