title: Synthesis and in vitro characterization of trans- and cis-[(18)F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoropiperidine-1-carboxylates as new potential PET radiotracer candidates for the NR2B subtype N-methyl-D-aspartate receptor.
abstract: Diastereoisomeric compounds [(18)F]cis- and [(18)F]trans-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoro-piperidine-1-carboxylates were successfully synthesized as new subtype-selective PET radiotracers for imaging the NR2B subunit containing NMDA receptors. Rat brain section autoradiographies demonstrated a high specific binding in NR2B/NMDA receptor rich regions for both radioligands. The measured logD(7.4) values as well as B(max)/K(d) ratios indicated that both radiotracers possess the adequate properties required for PET radiotracers.
authors.affiliation: CEA, I2BM, LDM-TEP, Centre Cyceron, F-14074 Caen, France.
authors.forename: Radouane
authors.initials: R
authors.lastname: Koudih
authors.forename: Gwénaëlle
authors.initials: G
authors.lastname: Gilbert
authors.forename: Martine
authors.initials: M
authors.lastname: Dhilly
authors.forename: Ahmed
authors.initials: A
authors.lastname: Abbas
authors.forename: Louisa
authors.initials: L
authors.lastname: Barré
authors.forename: Danièle
authors.initials: D
authors.lastname: Debruyne
authors.forename: Franck
authors.initials: F
authors.lastname: Sobrio
mesh_terms: D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D060326:Chemistry Techniques, Synthetic; D008297:Male; D010880:Piperidines / Q000737:chemistry; D049268:Positron-Emission Tomography / Q000379:methods*; D011849:Radioactive Tracers; D011854:Radiochemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D002264:Carboxylic Acids; C121001:NR2B NMDA receptor; D010880:Piperidines; D011849:Radioactive Tracers; D016194:Receptors, N-Methyl-D-Aspartate; C032727:piperidine