ISSN:
1432-0428
Keywords:
Hypoglycaemic agent
;
oxirane carboxylic acid
;
rat
;
adrenalectomised rat
;
guinea pig
;
dog
;
streptozotocin-diabetic pig
;
db/db-mice
;
plasma non-esterified fatty acid
;
blood ketone bodies
;
glucose
;
lactate
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary Phenylalkyloxirane carboxylic acids and esters are a new class of potent hypoglycaemic substances. Sodium 2-[5-(4-chlorophenyl)-pentyl]-oxirane-2-carboxylate (B 807-27) produces a dosedependent hypoglycaemic effect when administered orally or intravenously to several fasted laboratory animals, i.e. rats (with and without adrenalectomy), guinea pigs, dogs, streptozotocin-treated diabetic pigs and db/db-mice. In addition, the substances have a more pronounced lowering effect on ketone bodies in the blood than any other known substance. The minimal dose for lowering blood glucose significantly in rats is 15 μmol/kg. The corresponding dose for a significant lowering of ketone bodies in the blood is 〈 2.4 μmol/kg. Hence, the substance B 807-27 is approximately five times more potent than tolbutamide and 30 times more potent than the biguanide buformin with respect to lowering blood glucose levels. B 807-27 differs from the sulphonylureas in that it fails to stimulate insulin secretion. In contrast to the biguanides, the substance decreases rather than increases blood lactate concentration and blocks both fatty acid oxidation and gluconeogenesis. The therapeutic usefulness of these compounds in diabetic man remains to be elucidated.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00282590
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