| 摘要 |
<p>Somatostatin analogues of formula (I) and their acid addition salts are new. (where R is H, an aminoacid or a dipeptide e.g. Ala-Gly; X1 is (L) Phe, (D) Ala or bond; X2 is (L)Phe, (D) Phe or Gly; X3 is (L) Phe, (D) Phe or a bond and the Cys groups have (L) or (D) configuration). (I) regulate the secretion of insulin, glucagon and growth hormone (GH) and may be used to regulate glycemic levels in insulin dependent and non-insulin dependent diabetes and to control acromegalia. Due to the (D) aminoacids, (I) have better resistance to proteolysis than somatostatin and have prolonged activity. (I) have little action on secretion of gastric juices and low toxicity. The activity profile of the pcds. differ from that of somatostatin and suitable cpds. may be selected for the required activity. (I) are administered as 1-5% solutions by intravenous, intramuscular or sub-cutaneous injection ot give doses of 0.1-10 mg.</p> |
