Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]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 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.
Jagoda
Elaine
E
PET Department, Warren G. Magnuson Clinical Center, National Institutes of Health, 10 Center Drive, Bethesda, MD 20892, USA.
Contoreggi
Carlo
C
Lee
Mei-Jing
MJ
Kao
Chih-Hao K
CH
Szajek
Lawrence P
LP
Listwak
Sam
S
Gold
Philip
P
Chrousos
George
G
Greiner
Elisabeth
E
Kim
B Moon
BM
Jacobson
Arthur E
AE
Rice
Kenner C
KC
Eckelman
William
W
D000818:Animals; D001345:Autoradiography; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism; D001967:Bromine Radioisotopes; D066298:In Vitro Techniques; D008024:Ligands; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D018019:Receptors, Corticotropin-Releasing Hormone / Q000378:metabolism*; D014018:Tissue Distribution; D014227:Triazines / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D000099052:CRF Receptor, Type 1
D001967:Bromine Radioisotopes; D008024:Ligands; C476980:MJL 1-109-2; D019275:Radiopharmaceuticals; D018019:Receptors, Corticotropin-Releasing Hormone; D014227:Triazines; D000099052:CRF Receptor, Type 1