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Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.

Troxler, Thomas J. and Enz, Albert and Hoyer, Daniel and Langenegger, Daniel and Neumann, Peter and Pfaeffli, Paul and Schoeffter, Philippe and Hurth, Konstanze (2008) Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor. Bioorganic & Medicinal Chemistry Letters, 18 (3). pp. 979-982. ISSN 1464-3405

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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:25
URI: https://oak.novartis.com/id/eprint/177

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