Tolazamide is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Tolazamide had two general classes of binding sites (i.e., high and low affinity) for normal and glycated HSA. The higher affinity sites had binding constants of around 4.3-6.0 × 104 M-1 for these interactions at pH 7.4 and 37 °C, while the lower affinity sites had binding strengths of 4.9-9.1 × 103 M-1[3]. Tolazamide in vitro alters postreceptor insulin action without influencing the receptor, and suggests insulin-stimulated hexose transport as the cellular process responsible for the hypoglycemic effect of sulfonyureas in adipose tissue[4]. Tolazamide markedly enhances ECM (extracellular matrix) synthesis and accumulation in MCs (mesangial cells) probably by stimulating GLUT1 expression, glucose transport and TGF-beta 1 secretion, irrespective of the ambient glucose concentration. This effect was dose-dependent and minimally inducible by metformin[5].
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