Chemistry and pharmacology of SMS 201-995, a long-acting octapeptide analogue of somatostatin.
Scand J Gastroenterol Suppl
; 119: 54-64, 1986.
Article
em En
| MEDLINE
| ID: mdl-2876507
ABSTRACT
Starting from a hypothetical conformation of natural somatostatin and a knowledge of the minimal fragment needed for biological activity, a process of rational design and lead optimization has led to the potent, selective, and long-acting analogue SMS 201-995, (formula see text) which selectively inhibits growth hormone secretion in several animal species for up to 6 h after subcutaneous application. In the rat, SMS inhibits GH, insulin, and glucagon 70, 3, and 23 times more potently than SRIF, resulting in GH/insulin and GH/glucagon selectivities of 20 and 3, respectively. The compound has been shown to inhibit growth of transplantable insulinomas in hamsters and to label selectively a subset of somatostatin receptors in the rat cortex. A radioactively labelled analogue has been used to visualize somatostatin receptors in a GRF-secreting human tumour. The stability and duration of action of SMS 201-995 after subcutaneous injection enable for the first time extended investigations of the clinical utility of somatostatin in various diseases.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Somatostatina
Limite:
Animals
Idioma:
En
Revista:
Scand J Gastroenterol Suppl
Ano de publicação:
1986
Tipo de documento:
Article