187219-14-3Relevant academic research and scientific papers
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 (2007)
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.
