Synthesis and evaluation in monkey of two sensitive C-11-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo

• Published in: Journal of medicinal chemistry Vol. 51; no. 1; pp. 17 - 30
• Main Authors: Briard, Emmanuelle, Zoghbi, Sami S., Imaizumi, Masao, Gourley, Jonathan P., Shetty, H. Umesha, Hong, Jinsoo, Cropley, Vanessa, Fujita, Masahiro, Innis, Robert B., Pike, Victor W.
• Format: Journal Article
• Language: English
• Published: WASHINGTON Amer Chemical Soc 10.01.2008
• Subjects: Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; VISUALIZATION; PROTEIN 18 KDA; RADIOSYNTHESIS; MICROGLIA; RADIOLIGANDS; TISSUE; BINDING-SITES; DERIVATIVES; PET; CARBOXAMIDE

We sought to develop C-11-labeled ligands for sensitive imaging of brain peripheral benzodiazepine receptors (PBR) in vivo. Two aryloxyanilides with high affinity for PBR were identified and synthesized, namely, N-acetyl-N-(2-methoxycarbonylbenzyl)-2-phenoxyaniline (3, PBR01) and N-(2-methoxybenzyI)...