Octapeptide analogs of somatostatin exhibiting greatly enhanced in vivo and in vitro inhibition of growth hormone secretion in the rat.
Octapeptide analogs of somatostatin exhibiting greatly enhanced in vivo and in vitro inhibition of growth hormone secretion in the rat.
复制标题
生长抑素的八肽类似物在体内和体外对大鼠生长激素分泌的抑制作用大大增强。
DOI：
10.1016/0006-291x(85)91895-9
复制
发表时间：
1985
影响因子：
3.1
通讯作者：
Coy,DH
中科院分区：
文献类型：
--
作者：
Murphy,WA;Heiman,ML;Lance,VA;Mezo,I;Coy,DH
用固相合成法合成了一种超活性生长抑素（SRIF）八肽（代号SMS 201-995（1））的类似物，并测定了它们抑制培养的大鼠垂体前叶细胞和戊巴比妥钠麻醉大鼠生长激素释放的能力。一个模拟：相对于母体八肽分子和14个氨基酸的SRIF分子，其表现出大大增强的体外抑制活性（>1，000倍）。这种类似物，这也是非常有效的，在体内含有酪氨酸残基，并考虑到其高的体外活性，可能是一个放射性碘化配体在受体测定的研究重要性。一个八肽逆向-反转类似物也表现出显着的SRIF样活性。合成了几种活性非常低的八肽类似物，发现它们没有SRIF拮抗剂活性。以前在体内表现出超活性的十二肽类似物也表现出高的体外活性。
Analogs of a superactive somatostatin (SRIF) octapeptide (code named SMS 201–995 (1)) were synthesized using solid-phase synthetic methodology and assayed for their ability to inhibit growth hormone release from cultured rat anterior pituitary cells and in sodium pentobarbital-anesthetized rats. One analog: exhibited greatly enhanced in vitro inhibitory activity (>1,000x) relative to both the parent octapeptide molecule and to the 14 amino acid SRIF molecule. This analog which was also very potent in vivo contains a tyrosine residue and, given its high in vitro activity, may be of investigative importance as a radioiodinated ligand in receptor assays. An octapeptide retro-inverso analog also exhibited significant SRIF-like activity. Several very low activity octapeptide analogs were synthesized and were found to be devoid of SRIF-antagonist activity. A dodecapeptide analog previously shown to be superactive in vivo also demonstrated high in vitro activity.