SMS 201-995 - A VERY POTENT AND SELECTIVE OCTAPEPTIDE ANALOG OF SOMATOSTATIN WITH PROLONGED ACTION
SMS 201-995 - A VERY POTENT AND SELECTIVE OCTAPEPTIDE ANALOG OF SOMATOSTATIN WITH PROLONGED ACTION
复制标题
DOI：
10.1016/0024-3205(82)90087-x
复制
发表时间：
1982-01-01
期刊：
影响因子：
6.1
通讯作者：
PLESS, J
中科院分区：
文献类型：
--
作者：
BAUER, W;BRINER, U;PLESS, J
生长抑素片段构象稳定的类似物被认为是基本的生物活性部分，它的逐步修饰使得类似物的合成成为可能。代号为SMS 201-995，在体外抑制生长激素的分泌的效力是天然激素的3倍，生长激素高度抵抗由纯酶和组织匀浆降解，在大鼠和恒河猴体内的生长激素活性(取决于测试系统)至少是生长抑素的20倍，生长抑素的作用时间要长得多，而且在两个物种中抑制生长激素的分泌比胰岛素的选择性要高得多。该化合物通过包括口服在内的几种给药途径有效，在实验室动物和人类中都有很好的耐受性，目前正在进行初步临床试验。
Stepwise modification of a conformationally stabilized analog of that fragment of somatostatin which had been thought to be the essential biologically active moiety has enabled synthesis of the analog .**GRAPHIC**. code-named SMS 201-995, which in vitro is 3 times more potent than the native hormone in inhibiting the secretion of growth hormone, which is highly resistent to degradation by pure enzymes and by tissue homogenates, which in vivo in rat and rhesus monkey is (depending on test system) at least 20 times more active than somatostatin, which is much longer acting, and which moreover in both species is much more selective in inhibiting the secretion of growth hormone than that of insulin. The compound is active by several routes of administration including the oral, is well tolerated both in laboratory animals and in man, and is currently undergoing preliminary clinical trial.