GLP-1(7-37) is a truncated glucagon-like peptide with an EC50 value of 0.9 ± 0.1nM for GLP-1 receptors[1]. GLP-1(7-37) can bind to a specific GLP-1 receptor (GLP-1R) on pancreatic beta cells and enhance glucose-stimulated insulin secretion [2]. GLP-1(7-37) has been widely used as a model compound to develop a range of derivatives and GLP-1R agonists[3].
In vitro, GLP-1(7-37) treatment at 10nM for 30min significantly promoted cAMP generation as well as insulin secretion in Beta-TC-1 cells[4]. Pretreatment with 100nM GLP-1(7-37) for 3h enhanced the mitochondrial response to 25mM glucose stimulation in uninjured MitpHGV-MIN6 cells[5]. Treatment with 100nM GLP-1(7-37) for 10 seconds increased intracellular free calcium ions ([Ca2+]i) in COS-7 cells expressing the GLP-l receptor[6].
In vivo, GLP-1(7-37) treatment (5pmol/min/kg) via intravenous infusion (2h) into Zucker diabetic fatty (ZDF) rats transiently increased plasma insulin concentrations and normalized blood glucose concentrations[7]. Intravenous infusion of GLP-1(7-37) for 60 minutes (5pmol/min/kg) produced a transient increase in plasma insulin concentrations and a sustained slight decrease in blood glucose in fasted rats[8].
References:
[1] de Menthière C S, Chavanieu A, Grassy G, et al. Structural requirements of the N-terminal region of GLP-1-[7-37]-NH2 for receptor interaction and cAMP production[J]. European journal of medicinal chemistry, 2004, 39(6): 473-480.
[2] Vahl T P, Paty B W, Fuller B D, et al. Effects of GLP-1-(7–36) NH2, GLP-1-(7–37), and GLP-1-(9–36) NH2 on intravenous glucose tolerance and glucose-induced insulin secretion in healthy humans[J]. The Journal of Clinical Endocrinology & Metabolism, 2003, 88(4): 1772-1779.
[3] Manandhar B, Ahn J M. Glucagon-like peptide-1 (GLP-1) analogs: recent advances, new possibilities, and therapeutic implications[J]. Journal of medicinal chemistry, 2015, 58(3): 1020-1037.
[4] Fehmann H C, Habener J F. Functional receptors for the insulinotropic hormone glucagon‐like peptide‐I (7–37) on a somatostatin secreting cell line[J]. FEBS letters, 1991, 279(2): 335-340.
[5] Ogata M, Iwasaki N, Ide R, et al. GLP-1-related proteins attenuate the effects of mitochondrial membrane damage in pancreatic β cells[J]. Biochemical and Biophysical Research Communications, 2014, 447(1): 133-138.
[6] Wheeler M B, Lu M, Dillon J S, et al. Functional expression of the rat glucagon-like peptide-I receptor, evidence for coupling to both adenylyl cyclase and phospholipase-C[J]. Endocrinology, 1993, 133(1): 57-62.
[7] Hargrove D M, Nardone N A, Persson L M, et al. Glucose-dependent action of glucagon-like peptide-1 (7-37) in vivo during short-or long-term administration[J]. Metabolism, 1995, 44(9): 1231-1237.
[8] Hargrove D M, Nardone N A, Persson L M, et al. Comparison of the glucose dependency of glucagon-like peptide-1 (7–37) and glyburide in vitro and in vivo[J]. Metabolism, 1996, 45(3): 404-409.
GLP-1(7-37)是一种截短的胰高血糖素样肽，对GLP-1受体的EC50值为0.9 ± 0.1nM[1]。GLP-1(7-37)可通过与胰腺β细胞上的特异性GLP-1受体（GLP-1R）结合，增强葡萄糖刺激的胰岛素分泌[2]。GLP-1(7-37)作为模型化合物被广泛用于开发一系列衍生物和GLP-1R激动剂[3]。
在体外，10nM GLP-1(7-37)处理Beta-TC-1细胞30分钟可显著促进cAMP生成及胰岛素分泌[4]。100nM的GLP-1(7-37)预处理未受损的MitpHGV-MIN6细胞3小时能增强线粒体对25mM葡萄糖刺激的响应[5]。100nM的GLP-1(7-37)处理表达GLP-1受体的COS-7细胞10秒钟可增加细胞内游离钙离子（[Ca2+]i）浓度[6]。
在体内，Zucker糖尿病肥胖（ZDF）大鼠经静脉输注GLP-1(7-37)（5pmol/min/kg；持续2小时）可短暂升高血浆胰岛素浓度并使血糖浓度正常化[7]。禁食大鼠静脉输注GLP-1(7-37)（5pmol/min/kg；持续60分钟）能引起血浆胰岛素浓度瞬时升高及血糖持续轻度下降[8]。