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 IC₅₀=2.9 nM and antagonized somatostatin action with an IC₅₀=29 nM.

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