Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand:  Synthesis of [76Br]MJL-1-109-2

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...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2003-08, Vol.46 (17), p.3559-3562
Main Authors: Jagoda, Elaine, Contoreggi, Carlo, Lee, Mei-Jing, Kao, Chih-Hao K, Szajek, Lawrence P, Listwak, Sam, Gold, Philip, Chrousos, George, Greiner, Elisabeth, Kim, B. Moon, Jacobson, Arthur E, Rice, Kenner C, Eckelman, William
Format: Article
Language:English
Subjects:
Animals
Autoradiography
Biological and medical sciences
Blood-Brain Barrier
Brain - metabolism
Bromine Radioisotopes
Contrast media. Radiopharmaceuticals
In Vitro Techniques
Ligands
Medical sciences
Pharmacology. Drug treatments
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - metabolism
Radiopharmaceuticals - pharmacokinetics
Rats
Rats, Sprague-Dawley
Receptors, Corticotropin-Releasing Hormone - metabolism
Tissue Distribution
Triazines - chemical synthesis
Triazines - metabolism
Triazines - pharmacokinetics
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm034077k