Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.
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.
Tamagnan
Gilles D
GD
Institute for Degenerative Diseases, New Haven, CT 06520, USA. gtamagnan@indd.org
Brenner
Eric
E
Alagille
David
D
Staley
Julie K
JK
Haile
Colin
C
Koren
Andrei
A
Early
Michelle
M
Baldwin
Ronald M
RM
Tarazi
Frank I
FI
Baldessarini
Ross J
RJ
Jarkas
Nachwa
N
Goodman
Mark M
MM
Seibyl
John P
JP
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
C518627:(123I)INER; D018759:Adrenergic Uptake Inhibitors; D007202:Indicators and Reagents; D009025:Morpholines; D050484:Norepinephrine Plasma Membrane Transport Proteins; D019275:Radiopharmaceuticals; D000077593:Reboxetine