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GLP-1也可能直接抑制胰高血糖素的分泌,因为与野生型对照相比,α细胞特异性GLP-1受体激动剂敲除小鼠非空腹胰高血糖素水平升高,而雌性α细胞特异性GLP-1受体激动剂敲除小鼠在外周给糖后胰高血糖素分泌增加,表现出轻度葡萄糖不耐受[66]。在使用胰岛素受体拮抗剂S961或生长抑素受体2拮抗剂CYN154806处理的离体人胰岛中,...
D.J., Husain, M. 2008. Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and independent pathways. Circulation 117:2340-2350.
^Thomas MK, Nikooienejad A, Bray R, Cui X, Wilson J, Duffin K, Milicevic Z, Haupt A, Robins DA. Dual GIP and GLP-1 Receptor Agonist Tirzepatide Improves Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes. J Clin Endocrinol Metab. 2021 Jan 23;106(2):388-396. ...
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4.Nigel H. Greig, et al;Glucagon-like peptide-1 (GLP-1) receptor agonists and neuroinflammation:Implications for neurodegenerative disease treatment. Pharmacological Research 186 (2022) 106550. 5.申港证券, GLP-1RA 药物 下一站药王. 6.智慧芽新药情报库....
图1. 胰高糖素原的组织选择性加工示意图 PCSK1:激素前转化酶1/3;PCSK2:激素前转化酶2;NTS:孤束核;GRPP:肠高血糖素相关肽;IP-1:中间肽-1;IP-2:中间肽-2;MPGF:主要胰高糖素原片段;GLP-1:胰高糖素样肽-1;GLP-2:胰高糖素样肽-2。