Synthesis of a nonreducible cyclic analog of somatostatin having only growth hormone release inhibiting activity.
A nonreducible cyclic analog of somatostatin (SRIF) was prepared by a combination of solid phase and solution peptide synthesis. The compound, gamma-Abu-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Asp-OH, was tested for its effect on the release of growth hormone, glucagon and insulin in rats. It significantly suppressed pentobarbital-stimulated growth hormone release but showed no effect on arginine-stimulated glucagon or insulin release. The linear form, NH2-gamma-Abu-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Asp-OH, was also prepared and tested in vivo. It was shown to have only slight activity.
Garsky
V M
VM
Research Division, Wyeth Laboratories, Philadelphia, Pennsylvania 19101, USA.
Clark
D E
DE
Grant
N H
NH
D000595:Amino Acid Sequence; D000818:Animals; D005934:Glucagon / Q000097:blood / Q000378:metabolism; D013006:Growth Hormone / Q000097:blood / Q000378:metabolism*; D007328:Insulin / Q000097:blood / Q000378:metabolism; D000078790:Insulin Secretion; D008297:Male; D008969:Molecular Sequence Data; D051381:Rats; D013004:Somatostatin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D007328:Insulin; D013004:Somatostatin; D013006:Growth Hormone; D005934:Glucagon