Small molecule somatostatin receptor subtype-2 antagonists
| Autor: | Bridget Mccarthy Cole, Rona A. Nardone, Anthony P. Ricketts, Dennis J. Pelletier, Murray Marianne C, Hay Bruce Allan, Frank M. DiCapua, Alan Robertson, Glen W. Kirk, Todd W. Siegel |
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| Rok vydání: | 2001 |
| Předmět: |
Agonist
Models Molecular medicine.drug_class Somatostatin receptor Chemistry Organic Chemistry Clinical Biochemistry Antagonist Pharmaceutical Science Biological activity Biochemistry Small molecule Somatostatin Drug Discovery medicine Molecular Medicine Somatostatin binding Receptors Somatostatin Receptor Molecular Biology |
| Zdroj: | Bioorganicmedicinal chemistry letters. 11(20) |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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