Literature DB >> 12904058

Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2.

Elaine Jagoda1, Carlo Contoreggi, Mei-Jing Lee, Chih-Hao K Kao, Lawrence P Szajek, Sam Listwak, Philip Gold, George Chrousos, Elisabeth Greiner, B Moon Kim, Arthur E Jacobson, Kenner C Rice, William Eckelman.   

Abstract

A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood-brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases.

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Year:  2003        PMID： 12904058     DOI： 10.1021/jm034077k

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  10 in total

1.  Corticotropin-releasing factor 1 antagonists selectively reduce ethanol self-administration in ethanol-dependent rats.

Authors:  Cindy K Funk; Eric P Zorrilla; Mei-Jing Lee; Kenner C Rice; George F Koob
Journal:  Biol Psychiatry       Date:  2006-07-28       Impact factor: 13.382

2.  Dissociation between opioid and CRF1 antagonist sensitive drinking in Sardinian alcohol-preferring rats.

Authors:  Valentina Sabino; Pietro Cottone; George F Koob; Luca Steardo; Mei J Lee; Kenner C Rice; Eric P Zorrilla
Journal:  Psychopharmacology (Berl)       Date:  2006-10-18       Impact factor: 4.530

3.  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

4.  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

Review 5.  Role of corticotropin-releasing factor in drug addiction: potential for pharmacological intervention.

Authors:  Marian L Logrip; George F Koob; Eric P Zorrilla
Journal:  CNS Drugs       Date:  2011-04       Impact factor: 5.749

6.  [(76) Br]BMK-152, a nonpeptide analogue, with high affinity and low nonspecific binding for the corticotropin-releasing factor type 1 receptor.

Authors:  Elaine M Jagoda; Lixin Lang; Karen McCullough; Carlo Contoreggi; B Moon Kim; Ying Ma; Kenner C Rice; Lawrence P Szajek; William C Eckelman; Dale O Kiesewetter
Journal:  Synapse       Date:  2011-04-11       Impact factor: 2.562

7.  Corticotropin-releasing factor-1 receptor antagonists decrease heroin self-administration in long- but not short-access rats.

Authors:  Thomas N Greenwell; Cindy K Funk; Pietro Cottone; Heather N Richardson; Scott A Chen; Kenner C Rice; Eric P Zorrilla; George F Koob
Journal:  Addict Biol       Date:  2009-04       Impact factor: 4.280

8.  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

9.  Synthesis, binding affinity, radiolabeling, and microPET evaluation of 4-(2-substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as ligands for brain corticotropin-releasing factor type-1 (CRF1) receptors.

Authors:  Jeffrey S Stehouwer; Chase H Bourke; Michael J Owens; Ronald J Voll; Clinton D Kilts; Mark M Goodman
Journal:  Bioorg Med Chem Lett       Date:  2015-10-08       Impact factor: 2.823

10.  Role of BNST CRFR1 Receptors in Incubation of Fentanyl Seeking.

Authors:  Utsav Gyawali; David A Martin; Agnieszka Sulima; Kenner C Rice; Donna J Calu
Journal:  Front Behav Neurosci       Date:  2020-08-28       Impact factor: 3.558
  10 in total

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