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Published October 22, 2001 | Version public
Journal Article Metadata-only

Small molecule somatostatin receptor subtype-2 antagonists

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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.

Additional Information

© 2001 Elsevier Science Ltd. Received 1 June 2001, Accepted 3 August 2001, Available online 3 September 2001.

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Eprint ID
103008
Resolver ID
CaltechAUTHORS:20200505-151220694

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Created
2020-05-05
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Updated
2021-11-16
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