Author/Authors :
Konstanze Hurth، نويسنده , , Albert Enz، نويسنده , , Philipp Floersheim، نويسنده , , Conrad Gentsch، نويسنده , , Daniel Hoyer، نويسنده , , Daniel Langenegger، نويسنده , , Peter Neumann، نويسنده , , Paul Pf?ffli، نويسنده , , Dieter Sorg، نويسنده , , Robert Swoboda، نويسنده , , Annick Vassout، نويسنده , , Thomas Troxler، نويسنده ,
Abstract :
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.
