Synthesis and Evaluation of Radioligands for Imaging Brain Nociceptin/Orphanin FQ Peptide (NOP) Receptors with Positron Emission Tomography

• Published in: Journal of medicinal chemistry Vol. 54; no. 8; pp. 2687 - 2700
• Main Authors: Pike, Victor W, Rash, Karen S, Chen, Zhaogen, Pedregal, Concepción, Statnick, Michael A, Kimura, Yasuyuki, Hong, Jinsoo, Zoghbi, Sami S, Fujita, Masahiro, Toledo, Miguel A, Diaz, Nuria, Gackenheimer, Susan L, Tauscher, Johannes T, Barth, Vanessa N, Innis, Robert B
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 28.04.2011; Amer Chemical Soc
• Subjects: Animals; Brain - diagnostic imaging; Chemistry, Medicinal; Chromatography, Liquid; Haplorhini; Life Sciences & Biomedicine; Magnetic Resonance Spectroscopy; Nociceptin; Opioid Peptides - metabolism; Pharmacology & Pharmacy; Positron-Emission Tomography; Radioligand Assay; Rats; Science & Technology; Stereoisomerism; Tandem Mass Spectrometry; AUTORADIOGRAPHIC LOCALIZATION; ORPHANIN-FQ; ANTAGONIST SB-612111; OPIOID RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; IN-VIVO; DOPAMINE D2; BINDING-SITES; RADIOTRACERS; OCCUPANCY

Positron emission tomography (PET) coupled to an effective radioligand could provide an important tool for understanding possible links between neuropsychiatric disorders and brain NOP (nociceptin/orphanin FQ peptide) receptors. We sought to develop such a PET radioligand. High-affinity NOP ligands...