Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.
Tools
Tools
Troxler, Thomas J., Enz, Albert, Hoyer, Daniel, Langenegger, Daniel, Neumann, Peter, Pfaeffli, Paul, 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 |
|---|---|
| Related URLs: | |
| Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
| Keywords: | Somatostatin; GPCR; Somatostatin sst1 receptor; Selective sst1 receptor antagonists; Ergolines; Lysergic acid derivatives |
| Related URLs: | |
| Date Deposited: | 14 Dec 2009 13:50 |
| Last Modified: | 31 Jan 2013 01:03 |
| URI: | https://oak.novartis.com/id/eprint/944 |