Literature DB >> 10782669

Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor.

L W Hsin1, E L Webster, G P Chrousos, P W Gold, W C Eckelman, C Contoreggi, K C Rice.   

Abstract

A series of fluoro-substituted 4-(dialkylamino)pyrrolo[2,3-d]pyrimidines was synthesized and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 11a and 11b possessed very high CRHR1 affinity (Ki=3.5, 0.91 nM, respectively). They are promising candidates for the development of 18F-containing nonpeptide PET radioligands for CRHR1.

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Year:  2000        PMID: 10782669     DOI: 10.1016/s0960-894x(00)00071-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.

Authors:  Nicholas J Lodge; Yu-Wen Li; Frederick T Chin; Douglas D Dischino; Sami S Zoghbi; Jeffrey A Deskus; Ronald J Mattson; Masao Imaizumi; Rick Pieschl; Thaddeus F Molski; Masahiro Fujita; Heidi Dulac; Robert Zaczek; Joanne J Bronson; John E Macor; Robert B Innis; Victor W Pike
Journal:  Nucl Med Biol       Date:  2014-03-29       Impact factor: 2.408

2.  PET Imaging of CRF1 with [11C]R121920 and [11C]DMP696: is the target of sufficient density?

Authors:  Gregory M Sullivan; Ramin V Parsey; J S Dileep Kumar; Victoria Arango; Suham A Kassir; Yung-Yu Huang; Norman R Simpson; Ronald L Van Heertum; J John Mann
Journal:  Nucl Med Biol       Date:  2007-03-30       Impact factor: 2.408

3.  On the role of corticotropin-releasing hormone receptors in anxiety and depression.

Authors:  Johannes M H M Reul; Florian Holsboer
Journal:  Dialogues Clin Neurosci       Date:  2002-03       Impact factor: 5.986

  3 in total

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