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ID: ALA1139990
Journal: Bioorg Med Chem Lett
Title: Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.
Authors: Troxler T, Hoyer D, Langenegger D, Neumann P, Pfäffli P, Schoeffter P, Sorg D, Swoboda R, Hurth K.
Abstract: A novel class of non-peptide somatostatin receptor ligands bearing the octahydrobenzo[g]quinoline (obeline) structural element has been identified. SAR studies have been performed that led to the discovery of derivatives with high affinity (pK(d) r sst(1) > or = 9) and selectivity (> or = 150-fold for h sst(1) over h sst(2)-h sst(5)) for somatostatin receptor subtype sst(1). In a functional assay, the compounds act as antagonists at human recombinant sst(1) receptors.
CiteXplore: 17507221