Pfeiffer E F
Acta Diabetol Lat. 1984 Jan-Mar;21(1):1-32. doi: 10.1007/BF02624758.
The common denominator of the numerous data collected from experimental studies on isolated organs, on healthy subjects and on diabetic patients, is a specific effect of sulfonylureas on insulin release in the presence (or absence) of glucose. However, there are significant differences in the capacity of the various chemical preparations active in that respect. There are biochemical data suggesting that the glyburide- and chlorpropamide-type of preparations are affecting sites of the B-cells that are different from both the glucose and the tolbutamide receptors. Thus, glibenclamide seems to be qualitatively different from the older sulfonylureas, being more a potentiator than a stimulator. Therefore, we called this type the representative of 'the second generation' drugs. The extra-B-cell actions of these drugs, predominantly the stimulation of somatostatin and the inhibition of glucagon, are favorably adding to these antidiabetic actions. In clinical therapy, these specific properties make it possible to diagnose and to treat patients successfully who were regarded before as being non-responsive to sulfonylureas and being insulin-dependent. On the basis of blood glucose decreases and C-peptide increases, a specific glibenclamide-glucose-response-test has been described which is a valuable medium for predicting the outcome of oral antidiabetic therapy.
从对离体器官、健康受试者和糖尿病患者进行的实验研究中收集到的大量数据的共同特点是，在有（或无）葡萄糖存在的情况下，磺脲类药物对胰岛素释放具有特定作用。然而，在这方面具有活性的各种化学制剂的作用能力存在显著差异。有生化数据表明，格列本脲和氯磺丙脲类制剂作用于β细胞的位点与葡萄糖和甲苯磺丁脲受体均不同。因此，格列本脲在性质上似乎与较老的磺脲类药物不同，它更像是一种增强剂而非刺激剂。所以，我们将这类药物称为“第二代”药物的代表。这些药物的β细胞外作用，主要是刺激生长抑素和抑制胰高血糖素，对这些抗糖尿病作用起到了有益的补充。在临床治疗中，这些特殊性质使得以前被认为对磺脲类药物无反应且依赖胰岛素的患者能够得到成功诊断和治疗。基于血糖降低和C肽增加，已经描述了一种特定的格列本脲 - 葡萄糖反应试验，它是预测口服抗糖尿病治疗效果的一种有价值的手段。
