Tolbutamide is a sulfonylurea agonist for secretion of insulin by beta-cells. In rat pancreatic β-cells cultured in the presence of Tolbutamide displayed increased numbers of beta-cells in a dose responsive manner with beta-cell numbers doubling at 100 μg/ml of Tolbutamide. The compound displayed inhibitory action towards beta-cells at concentrations greater than 100 μg/ml. In addition in the presence of low glucose concentrations Tolbutamide's cytotrophic action was inhibited. On isolated dog pancreas islets Tolbutamide at 180 μM stimulated the release of somatostatin, insulin and glucagon in the absence of glucose. in all situations the loss of Ca2+ eliminated all effects of Tolbutamide. The compound has been observed to mechanistically enhance the secretion of insulin by highly selective amplification of insulin secretory burst mass.
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