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

Bioorg Med Chem Lett. 2008 Feb 1;18(3):979-82. doi: 10.1016/j.bmcl.2007.12.030. Epub 2007 Dec 26.


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.

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Ergolines* / chemical synthesis
  • Ergolines* / chemistry
  • Ergolines* / pharmacokinetics
  • Ergolines* / pharmacology
  • Humans
  • Molecular Structure
  • Rats
  • Receptors, Somatostatin / antagonists & inhibitors*
  • Somatostatin / physiology


  • Ergolines
  • Receptors, Somatostatin
  • Somatostatin