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Novel radiolabeled O 6 -benzylguanine (O 6 -BG) derivatives, 2-amino-6-O-( 11 C)-((methoxymethyl)benzyloxy)-9-methyl purines (( 11 C) p -O 6 -AMMP, 1a ; ( 11 C) m -O 6 -AMMP, 1b ; ( 11 C) o -O 6 -AMMP, 1c ), 2-amino-6-O-benzyloxy-9-( 11 C)-((methoxycarbonyl)methyl)purine (( 11 C)ABMMP, 2 ), and...
N-(1-napthyl)-N′-(3-( 123 I)-iodophenyl)-N-methylguanidine (( 123 I)CNS 1261) is a novel SPET ligand developed for imaging the NMDA receptor intra-channel MK 801/PCP/ketamine site. Data was acquired in 7 healthy volunteers after bolus injection of ( 123 I)CNS 1261. Kinetic modeling showed...
The objective of this study was to develop a method for labeling internalizing monoclonal antibodies (mAbs) such as those reactive to the anti-epidermal growth factor receptor variant III (EGFRvIII) with the α-particle emitting radionuclide 211 At. Based on previous work utilizing the...
The two estrogen receptor subtypes, ERα and ERβ, play important roles in breast cancer. To develop an ERα imaging agent, we synthesized fluoropropyl pyrazole triol (FPPT, 2), an analog of our ERα-selective ligand PPT. FPPT retains the high ERα binding selectivity of its parent PPT. We...
A novel procedure for the high-yield preparation of Re-188 radiopharmaceuticals containing a terminal Re≡N multiple bond is described. This method involves the reaction of ( 188 Re)(ReO 4 ) − with N -methyl S -methyl dithiocarbazate (DTCZ), as donor of nitrido nitrogen atoms, sodium oxalate...
Various aliphatic and aromatic ( 75 Se)selenoethers were prepared at the no-carrier-added (n.c.a.) level using a new radiosynthetic pathway, based on the formation of alkyl( 75 Se)selenocyanates as intermediates. Using one-pot model reactions of elemental 75 Se, sodium cyanide and various...
A systematic comparative investigation into the in vitro radiochemical stabilities of model compounds containing radioiodinated β-iodoethoxyl units and derivatives thereof, as well as those of similar compounds lacking a β-oxygen to serve as control references, was undertaken. The...
In order to optimize radiocopper labeling of anti-L1-CAM antibody chCE7, five bifunctional copper chelators were synthesized and characterized (CPTA-N-hydoxysuccinimide, DO3A-L-p-isothiocyanato-phenylalanine, DOTA-PA-L-p-isocyanato-phenylalanine, DOTA-glycyl-L-p-isocyanato-phenylalanine and...
Nucleophilic ( 18 F)fluorination of some halo- and mesyloxyalkanes to the corresponding ( 18 F)fluoroalkanes with fluoride-18 obtained from an 18 O(p,n) ( 18 F)F reaction, using an ionic liquid as a reaction medium, has been studied as a new method for fluorine-18 labeling. Of the various ionic...
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