PMID: 6131906Apr 1, 1983Paper

Structure-activity relationships of somatostatin analogs in the rabbit ileum and the rat colon

The Journal of Clinical Investigation
L E RosenthalK Dharmsathaphorn

Abstract

Somatostatin increases absorption of electrolytes and inhibits diarrhea in patients with endocrine tumors and short bowel syndrome. In an attempt to develop a gut-specific somatostatin analog, each amino acid in the somatostatin molecule was replaced with L-alanine, deleted, or substituted with its D-isomer. The potency of each analog to stimulate ion transport in the rabbit ileum was then determined using the modified Ussing chamber technique. The results were compared to the ability of each analog to inhibit the stimulated release of growth hormone from cultured rat anterior pituitary cells and to inhibit the arginine-stimulated release of insulin and glucagon in the rat in vivo. Analogs that showed gut selectivity were then tested for their ion transport properties in the rat colon. (a) Substitution with L-alanine or deletion of the amino acid at position 6, 7, 8, or 9 and deletion of Threonine(10)-produced analogs with significantly reduced ion transport properties to <4% of somatostatin's action. The substitution also markedly reduced the ability of the compounds to inhibit the release of growth hormone, insulin, and glucagon. (b) Selectivity of intestinal ion transport was achieved by any one of the following alterations:...Continue Reading

References

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Citations

Feb 1, 1987·Digestive Diseases and Sciences·R N Fedorak, M Field
Nov 1, 1985·Digestive Diseases and Sciences·G Bertaccini, G Coruzzi
Jun 20, 2007·International Journal of Colorectal Disease·Amosy E M'KomaAlan J Herline
Jul 13, 1985·Lancet
Jun 7, 2000·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·A SamsonA G Butt
Mar 23, 1985·British Medical Journal·R G LongS R Bloom
Dec 1, 1996·Baillière's Clinical Gastroenterology·S K ParkT M O'Dorisio
Jan 1, 1990·The Journal of Experimental Zoology. Supplement : Published Under Auspices of the American Society of Zoologists and the Division of Comparative Physiology and Biochemistry·C A Loretz
Dec 26, 2001·Biopharmaceutics & Drug Disposition·R F ReinosoL Martínez
May 1, 1995·Scandinavian Journal of Gastroenterology·P NellgårdJ Cassuto
Dec 18, 2020·Therapeutic Advances in Endocrinology and Metabolism·Basma HarisKhalid Hussain
Apr 1, 1986·The American Journal of Physiology·S E ShoelsonH S Tager

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