Potent, highly selective inhibition of growth hormone secretion by position 4 somatostatin analogs

Endocrinology
W A MurphyD H Coy

Abstract

Aromatic position 4 somatostatin (SS) analogs were synthesized by solid phase methodology and assayed in vivo for their effects on pentobarbital-stimulated GH levels in fed rats and insulin and glucagon levels in fasted rats. [F5-Phe4]SS was approximately 3 times more active than somatostatin in inhibiting all three hormones. [Phe4,D-Trp8]SS inhibited GH about 4 times more effectively than somatostatin and was only twice as active as somatostatin in the pancreas. [rho-NH2-Phe4]SS exhibited strong selectivity toward inhibition of GH, being 4 times more potent than somatostatin in the pituitary while only about 40% as active in the pancreas. [rho-NH2-Phe4,D-Trp8]SS maintained this same degree of selectivity toward GH inhibition and exhibited a striking 15-fold increase in activity in the pituitary compared to somatostatin. All four analogs inhibited GH for a longer period of time than somatostatin when administered sc at a dose of 10 microgram/100 g BW. [rho-NH2-Phe4,D-Trp8]SS was the longest acting of these analogs, with approximately a 2-h duration of inhibition of GH. [Phe4]SS, administered iv at a dose of 50 microgram/100 g BW, also inhibited GH for approximately 2 h. These data further support the feasibility of developing l...Continue Reading

Citations

Dec 22, 1983·The New England Journal of Medicine·S Reichlin
Mar 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·R Z CaiA V Schally
Apr 1, 1987·Proceedings of the National Academy of Sciences of the United States of America·R Z CaiA V Schally
Apr 1, 1983·The Journal of Clinical Investigation·L E RosenthalK Dharmsathaphorn
Feb 29, 1984·Biochemical and Biophysical Research Communications·V A LanceD H Coy
Aug 1, 1984·Journal of Endocrinological Investigation·C RedekoppR A Donald

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