title: Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2.
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.
authors.affiliation: PET Department, Warren G. Magnuson Clinical Center, National Institutes of Health, 10 Center Drive, Bethesda, MD 20892, USA.
authors.forename: Elaine
authors.initials: E
authors.lastname: Jagoda
authors.forename: Carlo
authors.initials: C
authors.lastname: Contoreggi
authors.forename: Mei-Jing
authors.initials: MJ
authors.lastname: Lee
authors.forename: Chih-Hao K
authors.initials: CH
authors.lastname: Kao
authors.forename: Lawrence P
authors.initials: LP
authors.lastname: Szajek
authors.forename: Sam
authors.initials: S
authors.lastname: Listwak
authors.forename: Philip
authors.initials: P
authors.lastname: Gold
authors.forename: George
authors.initials: G
authors.lastname: Chrousos
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Greiner
authors.forename: B Moon
authors.initials: BM
authors.lastname: Kim
authors.forename: Arthur E
authors.initials: AE
authors.lastname: Jacobson
authors.forename: Kenner C
authors.initials: KC
authors.lastname: Rice
authors.forename: William
authors.initials: W
authors.lastname: Eckelman
mesh_terms: 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
chemical_list: D001967:Bromine Radioisotopes; D008024:Ligands; C476980:MJL 1-109-2; D019275:Radiopharmaceuticals; D018019:Receptors, Corticotropin-Releasing Hormone; D014227:Triazines; D000099052:CRF Receptor, Type 1