Literature DB >> 11212103

The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type.

X Tian1, L W Hsin, E L Webster, C Contoreggi, G P Chrousos, P W Gold, K Habib, A Ayala, W C Eckelman, A E Jacobson, K C Rice.   

Abstract

A high-affinity radioligand for CRHR1 has been prepared that can serve as a template for the development of SPECT imaging agents. The 5-chloro-N-cyclopropylmethyl-N-(2,6-dichloro-4-iodophenyl)-2-methyl-N-propylpyrimidine-4,6-diamine (6b, Ki = 14 nM), and the corresponding 4-bromophenyl analogue (6a, Ki = 21 nM), were synthesized in four steps from compound 3.

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Year:  2001        PMID: 11212103     DOI: 10.1016/s0960-894x(00)00661-2

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


  3 in total

1.  Synthesis, F-18 radiolabeling, and microPET evaluation of 3-(2,4-dichlorophenyl)-N-alkyl-N-fluoroalkyl-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-amines as ligands of the corticotropin-releasing factor type-1 (CRF1) receptor.

Authors:  Jeffrey S Stehouwer; Matthew S Birnbaum; Ronald J Voll; Michael J Owens; Susan J Plott; Chase H Bourke; Michael A Wassef; Clinton D Kilts; Mark M Goodman
Journal:  Bioorg Med Chem       Date:  2015-06-19       Impact factor: 3.641

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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