title: Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.
abstract: 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 (pK(d) r sst(1) > or = 9) and selectivity (> or = 150-fold for h sst(1) over h sst(2)-h sst(5)) for somatostatin receptor subtype sst(1). In a functional assay, the compounds act as antagonists at human recombinant sst(1) receptors.
authors.affiliation: Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland. thomas.troxler@novartis.com
authors.forename: Thomas
authors.initials: T
authors.lastname: Troxler
authors.forename: Daniel
authors.initials: D
authors.lastname: Hoyer
authors.forename: Daniel
authors.initials: D
authors.lastname: Langenegger
authors.forename: Peter
authors.initials: P
authors.lastname: Neumann
authors.forename: Paul
authors.initials: P
authors.lastname: Pfäffli
authors.forename: Philippe
authors.initials: P
authors.lastname: Schoeffter
authors.forename: Dieter
authors.initials: D
authors.lastname: Sorg
authors.forename: Robert
authors.initials: R
authors.lastname: Swoboda
authors.forename: Konstanze
authors.initials: K
authors.lastname: Hurth
mesh_terms: D000818:Animals; D006801:Humans; D008164:Luminescent Proteins / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D008164:Luminescent Proteins; D017481:Receptors, Somatostatin; D011994:Recombinant Proteins; C010497:obelin