Angiopeptin TFA 是生长抑素的环状八肽类似物，是一种 sst2/sst5 受体部分激动剂，IC50 值分别为 0.26 nM 和 6.92 nM。Angiopeptin TFA 可以抑制生长激素释放和胰岛素样生长因子-1 (IGF-1) 产生。Angiopeptin TFA 抑制腺苷酸环化酶或刺激细胞外酸化。Angiopeptin TFA 具有用于冠状动脉粥样硬化研究的潜力。
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibit adenylate cyclase or stimulate extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research[1][2].
Angiopeptin (0.1 nM- 10 μM; for 1 h) TFA acts as a partial agonist (pEC50=6.57) with a maximum response of 423% at 3 μM on the release of tritium on CHO hsst2 cells[2].
Angiopeptin (20 and 50μg/kg; i.h.) TFA significantly inhibits neointimal formation[1].Angiopeptin (20 μg/kg; per day) TFA significantly inhibits coronary artery myointimal proliferation in cardiac allografts by appmximalely 50%[1].
[1]. Lundergan CF, et al. Peptide inhibition of myointimal proliferation by angiopeptin, a somatostatin analogue. J Am Coll Cardiol. 1991;17(6 Suppl B):132B-136B.
[2]. Alderton F, et al. Somatostatin receptor-mediated arachidonic acid mobilization: evidence for partial agonism of synthetic peptides. Br J Pharmacol. 2001;132(3):760-766.
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