187218-90-2Relevant academic research and scientific papers
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists
Troxler, Thomas,Hoyer, Daniel,Langenegger, Daniel,Neumann, Peter,Pfaeffli, Paul,Schoeffter, Philippe,Sorg, Dieter,Swoboda, Robert,Hurth, Konstanze
, p. 3983 - 3987 (2008/02/13)
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 (pKd
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists
Hurth, Konstanze,Enz, Albert,Floersheim, Philipp,Gentsch, Conrad,Hoyer, Daniel,Langenegger, Daniel,Neumann, Peter,Pfaeffli, Paul,Sorg, Dieter,Swoboda, Robert,Vassout, Annick,Troxler, Thomas
, p. 3988 - 3991 (2008/09/20)
The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst1 receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst1 affinities in this series cover a range of five orders of magnitude with the best derivatives displaying subnanomolar sst1 affinities and >10,000-fold selectivities over the sst2 receptor subtype as well as promising pharmacokinetic properties.
