Somatostatin analogs. Dissociation of brain receptor binding affinities and pituitary actions in the rat

Endocrinology
C B Srikant, Y C Patel

Abstract

We have recently demonstrated the presence of specific receptors for somatostatin (SRIF) in rat brain synaptosomal membranes which appear to mediate its action. Using this system as a radioreceptor assay, we have examined the ability of a wide range of SRIF analogs to interact with these receptors. Although structural modifications in the Trp8 moiety of SRIF resulted in significant enhancement of affinity for binding to the brain SRIF receptors, the different relative specificities of des AA1,2,4,5,12,13 D-Trp8 SRIF (oligo D-Trp8 SRIF), D-Trp8 SRIF and D-5-Br-Trp8 SRIF in the pituitary and the central nervous system (CNS) suggest that basic differences exist between SRIF receptors present in the brain and the pituitary.

Citations

Jul 4, 1998·European Journal of Pharmacology·S SiehlerD Hoyer
Dec 22, 1983·The New England Journal of Medicine·S Reichlin
Oct 12, 1981·Biochimica Et Biophysica Acta·J M ConlonK G Alberti
Sep 14, 1986·Biochemical and Biophysical Research Communications·C B Srikant, Y C Patel
Nov 19, 1981·Nature·C B Srikant, Y C Patel
Oct 15, 1985·The Journal of Comparative Neurology·G R UhlJ B Martin

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