Small molecule somatostatin receptor subtype-2 antagonists

Authors
Hay, BA Cole, BM DiCapua, F Kirk, GW Murray, MC Nardone, RA Pelletier, DJ Ricketts, AP Robertson, AS Siegel, TW
Citation
Ba. Hay et al., Small molecule somatostatin receptor subtype-2 antagonists, BIOORG MED, 11(20), 2001, pp. 2731-2734
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
20
Year of publication
2001
Pages
2731 - 2734
Database
ISI
SICI code
0960-894X(20011022)11:20<2731:SMSRSA>2.0.ZU;2-I
Abstract
The first potent small molecule sst2 antagonists are reported. Altering kno wn sst2 agonist molecules yielded compounds with high sst2 binding affinity and full antagonist activity. Compound 7a, for example, displaced somatost atin binding to the sst2 receptor with an IC50 = 2.9 nM and antagonized som atostatin action with an IC50 = 29 nM. (C) 2001 Elsevier Science Ltd. All r ights reserved.