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Small molecule somatostatin receptor subtype-2 antagonists

Hay, Bruce A. and Cole, Bridget M. and DiCapua, Frank and Kirk, Glen W. and Murray, Marianne C. and Nardone, Rona A. and Pelletier, Dennis J. and Ricketts, Anthony P. and Robertson, Alan S. and Siegel, Todd W. (2001) Small molecule somatostatin receptor subtype-2 antagonists. Bioorganic and Medicinal Chemistry Letters, 11 (20). pp. 2731-2734. ISSN 0960-894X. doi:10.1016/s0960-894x(01)00568-6. https://resolver.caltech.edu/CaltechAUTHORS:20200505-151220694

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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.


Item Type:Article
Related URLs:
URLURL TypeDescription
https://doi.org/10.1016/s0960-894x(01)00568-6DOIArticle
Additional Information:© 2001 Elsevier Science Ltd. Received 1 June 2001, Accepted 3 August 2001, Available online 3 September 2001.
Issue or Number:20
DOI:10.1016/s0960-894x(01)00568-6
Record Number:CaltechAUTHORS:20200505-151220694
Persistent URL:https://resolver.caltech.edu/CaltechAUTHORS:20200505-151220694
Official Citation:Bruce A. Hay, Bridget M. Cole, Frank DiCapua, Glen W. Kirk, Marianne C. Murray, Rona A. Nardone, Dennis J. Pelletier, Anthony P. Ricketts, Alan S. Robertson, Todd W. Siegel, Small molecule somatostatin receptor subtype-2 antagonists, Bioorganic & Medicinal Chemistry Letters, Volume 11, Issue 20, 2001, Pages 2731-2734, ISSN 0960-894X, https://doi.org/10.1016/S0960-894X(01)00568-6. (http://www.sciencedirect.com/science/article/pii/S0960894X01005686)
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:103008
Collection:CaltechAUTHORS
Deposited By: Tony Diaz
Deposited On:05 May 2020 22:44
Last Modified:16 Nov 2021 18:17

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