Title of article
Small molecule somatostatin receptor subtype-2 antagonists
Author/Authors
Bruce A. Hay، نويسنده , , Bridget M. Cole، نويسنده , , Frank DiCapua، نويسنده , , Glen W. Kirk، نويسنده , , Marianne C. Murray، نويسنده , , Rona A. Nardone، نويسنده , , Dennis J. Pelletier، نويسنده , , Anthony P. Ricketts، نويسنده , , Alan S. Robertson، نويسنده , , Todd W. Siegel، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
4
From page
2731
To page
2734
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791718
Link To Document