Small molecule somatostatin receptor subtype-2 antagonists

Small molecule somatostatin receptor subtype-2 antagonists

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 soma...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-10, Vol.11 (20), p.2731-2734
Hauptverfasser: Hay, Bruce A., Cole, Bridget M., DiCapua, Frank, Kirk, Glen W., Murray, Marianne C., Nardone, Rona A., Pelletier, Dennis J., Ricketts, Anthony P., Robertson, Alan S., Siegel, Todd W.
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Medical sciences
Models, Molecular
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Receptors, Somatostatin - antagonists & inhibitors
Receptors, Somatostatin - metabolism
Somatostatin - chemistry
Somatostatin - pharmacology
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Zusammenfassung: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. The synthesis of the first small molecule sst2 antagonists is reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00568-6