Somatostatin analogs with improved oral bioavailability

Cyclic hexapeptide analogs of somatostatin with insulin, glucagon, and growth hormone (GH) release inhibitory potencies of 50-200 times those of somatostatin have been synthesized. Replacement of the Phe-7 residue with histidine has resulted in increased oral bioavailability and duration of action....

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Bibliographic Details
Published in:	Klinische Wochenschrift Vol. 64 Suppl 7; p. 71
Main Authors:	Nutt, R F, Colton, C D, Veber, D F, Slater, E L, Saperstein, R
Format:	Journal Article
Language:	English
Published:	Germany 1986
Subjects:	Administration, Oral Amino Acid Sequence Animals Biological Availability Glucagon - metabolism Hormones - chemical synthesis Hormones - pharmacology Insulin - metabolism Insulin Secretion Peptides, Cyclic - chemical synthesis Rats Secretory Rate - drug effects Somatostatin - administration & dosage Somatostatin - analogs & derivatives Somatostatin - chemical synthesis Somatostatin - pharmacology Structure-Activity Relationship
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Summary:	Cyclic hexapeptide analogs of somatostatin with insulin, glucagon, and growth hormone (GH) release inhibitory potencies of 50-200 times those of somatostatin have been synthesized. Replacement of the Phe-7 residue with histidine has resulted in increased oral bioavailability and duration of action. Metabolic degradation of L-Trp containing analogs upon oral administration has also been overcome by incorporation of histidine. The all L-amino acid containing analog cyclo(NMePhe-His-Trp-Lys-Val-Ala) shows oral bioavailability comparable to D-Trp containing analogs.
ISSN:	0023-2173