title: Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.
abstract: A series of reboxetine analogs was synthesized and evaluated for in vitro binding as racemic mixtures. The best candidate (INER) was synthesized as the optically pure (S,S) enantiomer, labeled with iodine-123 and its in vivo binding determined by SPECT imaging in baboons. The in vivo specificity, selectivity, and kinetics of [123I]INER make it a promising agent for imaging NET in vivo by noninvasive SPECT imaging.
authors.affiliation: Institute for Degenerative Diseases, New Haven, CT 06520, USA. gtamagnan@indd.org
authors.forename: Gilles D
authors.initials: GD
authors.lastname: Tamagnan
authors.forename: Eric
authors.initials: E
authors.lastname: Brenner
authors.forename: David
authors.initials: D
authors.lastname: Alagille
authors.forename: Julie K
authors.initials: JK
authors.lastname: Staley
authors.forename: Colin
authors.initials: C
authors.lastname: Haile
authors.forename: Andrei
authors.initials: A
authors.lastname: Koren
authors.forename: Michelle
authors.initials: M
authors.lastname: Early
authors.forename: Ronald M
authors.initials: RM
authors.lastname: Baldwin
authors.forename: Frank I
authors.initials: FI
authors.lastname: Tarazi
authors.forename: Ross J
authors.initials: RJ
authors.lastname: Baldessarini
authors.forename: Nachwa
authors.initials: N
authors.lastname: Jarkas
authors.forename: Mark M
authors.initials: MM
authors.lastname: Goodman
authors.forename: John P
authors.initials: JP
authors.lastname: Seibyl
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D005260:Female; D007202:Indicators and Reagents; D009025:Morpholines / Q000138:chemical synthesis* / Q000494:pharmacology*; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000378:metabolism*; D010215:Papio; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D000077593:Reboxetine; D013237:Stereoisomerism; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: C518627:(123I)INER; D018759:Adrenergic Uptake Inhibitors; D007202:Indicators and Reagents; D009025:Morpholines; D050484:Norepinephrine Plasma Membrane Transport Proteins; D019275:Radiopharmaceuticals; D000077593:Reboxetine