Small molecule somatostatin receptor subtype-2 antagonists.

Abstract The first potent small molecule sst2 antagonists are reported. Altering known sst2 agonist molecules yielded compounds with high sst2 binding affinity and full antagonist activity. Compound 7a , for example, displaced somatostatin binding to the sst2 receptor with an IC 50 =2.9 nM and antagonized somatostatin action with an IC 50 =29 nM.