Pharmacological comparison between tolbutamide and two second generation hypoglycemic sulfonylureas (Glibenclamide and glisoxepide)

Loubatières, A; Ribes, G; Mariani, M. M.; Alric, R

doi:10.1007/bf02590661

Cited by 18 publications

(20 citation statements)

References 5 publications

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“…It has been reported that sulphonylureas are able to stimulate pancreatic ~-cell growth (Loubatieres et at., 1973), to reduce platelet stickiness (Desnoyer et at. 1972;Klaff et al, 1979) and to potentiate the action of insulin (Feinglos and Lebovitz, 1978; Pharmacokinetics of Suiphonyiurea Hypogiycaemic Drugs Lebovitz et aI., 1977).…”

Section: Other Effectsmentioning

confidence: 99%

Clinical Pharmacokinetics of Sulphonylurea Hypoglycaemic Drugs

Balant

1981

Clinical Pharmacokinetics

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Section: Other Effectsmentioning

confidence: 99%

Clinical Pharmacokinetics of Sulphonylurea Hypoglycaemic Drugs

Balant

1981

Clinical Pharmacokinetics

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“…The maximum hypoglycaemic drop obtained with each dose and each animal was plotted as a function of the logarithm of the doses (Fig. 3) and compared with those previously obtained with sulphonylureas [13]. The calculated regression lines did not significantly deviate from parallelism [14].…”

Section: Hypoglycaemic and Insulin Secretory Effects Of Hb 699mentioning

confidence: 99%

Effect of a new hypoglycaemic agent (HB 699) on the in vivo secretion of pancreatic hormones in the dog

et al. 1981

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Summary. The effects of HB 699, a non-sulphonyl urea acyl-amino-alcyl benzoic acid derivative, were studied in unanaesthetized dogs. Changes in blood glucose and plasma insulin, glucagon, pancreatic polypeptide and somatostatin were measured after a single intravenous injection. HB 699 caused hypoglycaemia and stimulated insulin secretion in a dosedependent manner. The effects of lib 699 (40 mg/ kg) on pancreatic hormone secretion were compared to those of tolbutamide given at a dose (12 mg/kg) which induced a similar maximal hypoglycaemia. Both drugs caused a similar increase in insulin release (180 + 32% for tolbutamide and 240 + 41% for HB 699) lasting for approximately l hour. Despite hypoglycaemia, plasma glucagon concentrations were unaltered by either substance. HB 699 caused a marked increase in the secretion of pancreatic polypeptide (220 _+ 60% at 30 min) for up to 2 hours, whereas tolbutamide caused no significant change in plasma pancreatic polypeptide levels. In contrast, while tolbutamide caused a significant (45 + 12%) but short-lived increase in plasma somatostatin concentrations, HB 699 had no significant effect.Key words: Acyl-amino-alcyl benzoic acid derivative, hypoglycaemic agent, insulin release, pancreatic polypeptide, glucagon, somatostatin, tolbutamide, unanaesthetized dogs.Certain acyl-amino-alcyl benzoic and phenylpropionic acid derivatives were previously described as having hypoglycaemic properties [1,2,3,4]. These substances are devoid of the structural requirements regarded as essential for the insulin releasing action of hypoglycaemic sulphonamides, the sulphamidothiodiazol and sulphonylurea groups. (Fig. 1) is identical with one part of the glibenclamide molecule, a second generation hypoglycaemic sulphonamide that has been extensively studied.In vitro studies using the isolated perfused rat pancreas have shown that HB 699 stimulates insulin release without affecting glucagon release in the presence of glucose [4,5]. In the first part of the present study the effects of liB 699 on blood glucose and plasma insulin concentrations were examined in conscious dogs. In the second part of the study the effects of HB 699 on plasma glucagon, pancreatic polypepfide (PP) and somatostatin concentrations were measured. In all experiments tolbutamide was used as a reference hypoglycaemic agent.

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“…Isoxazole is one of the top 10 % heterocycles frequently used in drug discovery , . Derivatives of this heterocycle are widespread among natural products; they are represented by antirheumatic and antiviral drugs, fungicides, and hypoglycemic agents . Isoxazole‐based sulfonamide antibiotics can be found in the World Health Organization model list of essential medicines…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 4‐Hetarylisoxazoles from Amino Acid‐Derived Halogenoximes and Push‐Pull Enamines

et al. 2018

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An approach to 4‐hetarylisoxazole‐derived amines and other related 3,4‐disubstituted isoxazoles which relies on [3+2] cycloaddition of amino acid‐derived halogenoximes and push‐pull enamines is described. The target products are obtained at gram scale in up to 81 % overall yield. The efficiency of the method is affected by the electronic properties of the enamine component at the key step.

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Pharmacological comparison between tolbutamide and two second generation hypoglycemic sulfonylureas (Glibenclamide and glisoxepide)

Cited by 18 publications

References 5 publications

Clinical Pharmacokinetics of Sulphonylurea Hypoglycaemic Drugs

Clinical Pharmacokinetics of Sulphonylurea Hypoglycaemic Drugs

Effect of a new hypoglycaemic agent (HB 699) on the in vivo secretion of pancreatic hormones in the dog

Synthesis of 4‐Hetarylisoxazoles from Amino Acid‐Derived Halogenoximes and Push‐Pull Enamines

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