title: Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[11C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine.
abstract: Three potent and selective 11C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.
authors.affiliation: Hammersmith Imanet Ltd, Cyclotron Building, Du Cane Road, London W12 ONN, UK. erik.arstad@csc.mrc.ac.uk
authors.forename: Erik
authors.initials: E
authors.lastname: Arstad
authors.forename: Stefan
authors.initials: S
authors.lastname: Platzer
authors.forename: Achim
authors.initials: A
authors.lastname: Berthele
authors.forename: Lyn S
authors.initials: LS
authors.lastname: Pilowsky
authors.forename: Sajinder K
authors.initials: SK
authors.lastname: Luthra
authors.forename: Hans-Jürgen
authors.initials: HJ
authors.lastname: Wester
authors.forename: Gjermund
authors.initials: G
authors.lastname: Henriksen
mesh_terms: D000578:Amidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000840:Anisoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002247:Carbon Isotopes; D008024:Ligands; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D049268:Positron-Emission Tomography / Q000379:methods*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
chemical_list: D000578:Amidines; D000840:Anisoles; D002247:Carbon Isotopes; D008024:Ligands; C514595:N-(2-methoxy)benzyl 4-trifluomethoxyphenylamidine; C121001:NR2B NMDA receptor; D016194:Receptors, N-Methyl-D-Aspartate