loading...| Preferred Name |
Glyburide |
|
| Synonyms |
Glibenclamide Diabeta GLYBURIDE Glyburide Micronase |
|
| Definitions |
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. |
|
| ID |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C29076 |
|
| CAS_Registry |
10238-21-8 |
|
| CHEBI_ID |
CHEBI:5441 |
|
| Chemical_Formula |
C23H28ClN3O5S |
|
| code |
C29076 |
|
| Concept_In_Subset |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978 |
|
| Contributing_Source |
CTRP FDA |
|
| 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. |
|
| Display_Name |
Glyburide |
|
| FDA_UNII_Code |
SX6K58TVWC |
|
| FULL_SYN |
Glibenclamide Diabeta GLYBURIDE Glyburide Micronase |
|
| label |
Glyburide |
|
| Legacy Concept Name |
Glyburide |
|
| NCI_Drug_Dictionary_ID |
772960 |
|
| PDQ_Closed_Trial_Search_ID |
772960 |
|
| PDQ_Open_Trial_Search_ID |
772960 |
|
| Preferred_Name |
Glyburide |
|
| prefixIRI |
Thesaurus:C29076 |
|
| Semantic_Type |
Pharmacologic Substance |
|
| UMLS_CUI |
C0017628 |
|
| subClassOf |