Back to Search
Start Over
Absence of exacerbation of myocardial stunning in anesthetized dogs treated with KAD-1229, a novel hypoglycemic agent
- Source :
- European journal of pharmacology. 431(3)
- Publication Year :
- 2001
-
Abstract
- The effect of (+)-momocalcium bis[(2S,3a,7a-cis)-α-benzylhexahydro-γ-oxo-2-isoindolinebutyrate]dihydrate (KAD-1229), a novel hypoglycemic agent with a chemical structure different from that of the sulfonylureas, on myocardial stunning was assessed in anesthetized dogs by comparison with that of glibenclamide, a sulfonylurea. Even though their hypoglycemic effects were of similar magnitude, glibenclamide (1 mg/kg, i.v.), but not KAD-1229, exacerbated the myocardial stunning induced by occlusion/reperfusion of the descending coronary artery. In a receptor-binding experiment, unlabeled glibenclamide completely inhibited [3H]glibenclamide binding to the myocardium, but KAD-1229 did not. These results suggest that the difference in binding properties of KAD-1229 and glibenclamide toward cardiac sulfonylurea receptors is one of the causes of their different effects on myocardial stunning. It is likely that KAD-1229 is highly specific for pancreatic sulfonylurea receptors and is speculated to be a safer hypoglycemic agent than, at least, glibenclamide.
- Subjects :
- medicine.medical_specialty
Indoles
Potassium Channels
medicine.drug_class
Receptors, Drug
Ischemia
Myocardial Reperfusion
Isoindoles
Sulfonylurea Receptors
Binding, Competitive
Glibenclamide
Electrocardiography
Dogs
Internal medicine
Coronary Circulation
Glyburide
medicine
Animals
Hypoglycemic Agents
Potassium Channels, Inwardly Rectifying
Pharmacology
Myocardial Stunning
Myocardial stunning
biology
business.industry
Myocardium
Fissipedia
Hemodynamics
Heart
medicine.disease
biology.organism_classification
Sulfonylurea
Endocrinology
Mechanism of action
Circulatory system
Sulfonylurea receptor
ATP-Binding Cassette Transporters
medicine.symptom
business
medicine.drug
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 431
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- European journal of pharmacology
- Accession number :
- edsair.doi.dedup.....b6dda0a65b0156697bc34383392a9d07