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ID: ALA1140830
Journal: Bioorg Med Chem Lett
Title: Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.
Authors: Troxler T, Enz A, Hoyer D, Langenegger D, Neumann P, Pfäffli P, Schoeffter P, Hurth K.
Abstract: Non-peptidic compounds containing the octahydro-indolo[4,3-fg]quinoline (ergoline) structural element have been optimized into derivatives with high affinity (pK(d) r sst(1)>9) and selectivity (>1000-fold for h sst(1) over h sst(2)-h sst(5)) for the somatostatin sst(1) receptor. In functional assays, these ergolines act as antagonists at human recombinant sst(1) receptors. Pharmacokinetic studies in rodents reveal good oral bioavailability and brain penetration for some of these compounds.
CiteXplore: 18162395