SMS 201–995: A very potent and selective octapeptide analogue of somatostatin with prolonged action

doi:10.1016/0024-3205(82)90087-X

Life Sciences

Volume 31, Issue 11, 13 September 1982, Pages 1133-1140

https://doi.org/10.1016/0024-3205(82)90087-X Get rights and content

Abstract

Stepwise modification of a conformationally stabilised analogue of that fragment of somatostatin which had been thought to be the essential biologically active moiety has enabled us to synthesise the analogue

H-(D)Phe-C

s-Thr(ol) code-named SMS 201–995, which

in vitro

is three 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.

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SMS 201–995: A very potent and selective octapeptide analogue of somatostatin with prolonged action

Abstract

Metabolism

Methods in Enzymology

Brain Res. Bull.

J. Med. Chem.

Nature