Preferred Label : Glyburide;
NCIt synonyms : Glibenclamide;
NCIt definition : A sulfonamide urea derivative with antihyperglycemic activity that can potentially
be used to decrease cerebral edema. Upon administration, glyburide binds to and blocks
the sulfonylurea receptor type 1 (SUR1) subunit of the ATP-sensitive inwardly-rectifying
potassium (K(ATP)) channels on the membranes of pancreatic beta cells. This prevents
the inward current flow of positively charged potassium (K ) ions into the cell, and
induces a calcium ion (Ca2 ) influx through voltage-sensitive calcium channels, which
triggers exocytosis of insulin-containing granules. In addition, glyburide also inhibits
the SUR1-regulated nonselective cation (NC) Ca-ATP channel, melastatin 4 (transient
receptor potential cation channel subfamily M member 4; (TRPM4)), thereby preventing
capillary failure and brain swelling. SUR1-TRPM4 channels are formed by co-assembly
of SUR1 with TRPM4 in neurons, astrocytes, and capillary endothelium during cerebral
ischemia. Upon ischemia-induced ATP depletion, channels open which results in sodium
influx, cytotoxic edema formation, capillary fragmentation and necrotic cell death.
SUR1-TRPM4 is not expressed in normal, uninjured tissues.;
UNII : SX6K58TVWC;
InChIKey : ZNNLBTZKUZBEKO-UHFFFAOYSA-N;
CAS number : 10238-21-8;
Drug name : Micronase; Diabeta;
Chemical formula : C23H28ClN3O5S;
ChEBI ID : CHEBI:5441;
Origin ID : C29076;
UMLS CUI : C0017628;
Semantic type(s)
- UMLS correspondences (same concept)
- Validated automatic mappings to BTNT
- chemical_or_drug_is_metabolized_by_enzyme
- concept_is_in_subset
