Journal of Labelled Compounds and Radiopharmaceuticals 1997: Vol 40 Table of Contents

19 Pages·1997·0.73 MB·English

Journal of Labelled Compounds and Radiopharmaceuticals—Vol. XL
Papers - Table of Contents
I>1 Automated Synthesis of "F-Labelcd FK960 (A/-Acetyl-l-Piperazinyl)-p-Fluorobenzamide Monohydrate). I
Murakami. Y.. Nishimura, S., Noda, A., Harada, N. and Tsukada, H.
1-2 Fluorine-18 Labeled Oligodeoxynucleotides for In Vivo PET Imaging. 4
Doll6. F.. Kuhnast, B., Terrazino, S.. Tavitian, B., Hinnen, F., Vaufrey, F. and Crouzel, C.
1-3 Synthesis of a F-18 Labelled Analog of Anti-Tumor Prostaglandin D7-PGA1 Methyl Ester. 7
Haradahira. T.. Hasegawa, Y., Furuta, K., Suzuki. M.. Watanabe, Y. and Suzuki, K.
1-4 Radiochemical Synthesis of 4-Ruorobenzylamino Conjugate of 2-Nitroimidazole I-Acetic Acid 9
(PK 110) as a Potential Hypoxia Imaging Agent.
Garg. P.K. and Zalutsky, M.R.
1-5 ["FlHalothane Photolabeling of Isolated Proteins. II
Tavlor. M.D. and Nickles, R.J.
1-6 New Approaches to Electrophilic Radiofluorination. 14
Steinbach. J.. Fischer, C.. Neubert, K. and Johannsen, B.
1-7 Synthesis of a Fluorinated Analogue of L-Threo-3-(3,4-Dihydroxyphtnyl)serine: 6-Fluoro-L-Threo-DOPS. 17
Lambin. D.. Lemaire, C., Plenevaux, A., Damhaut, P. and Luxen, A.
1-8 Synthesis of (R)- and (S)-9-|(3-[“F]Fluoro-l-Hydroxy-Propoxy)methyl}guanine: Radiopharmaceuticals 20
for Gene Therapy.
Monclus. M.. Luxen, A., Cool. V., Damhaut, P., Scurins, A.-L., Havet, K., Baudson, N., Van Naemen, J.,
Velu, T. and Goldman, S.
1-9 Simple Synthesis of [F-18]2’-Fluoro-3’,5‘-Di-0-Acetyl-2’-Deoxyarabino-6-N-Acetyladenine for Detecting 23
Tumors; A Prodrug of Fluoroadenosine.
Jeong. J.M.. Lee. Y.J.. Kim, C., Chang. Y.S.. Kim, Y.J., Lee, D.S., Chung, J.-K., Lee. M.C.. Koh. C.-S.,
Cho, J.-H., Yang. D.J.
I-IO Potential Dopamine D4 Receptor Imaging Agents: ["F]Fluoromethylated I-Phenyl-3- 26
(Aminomethyl)pyrroles and 7-Azaindole Analog.
Oh. S.J.. Choe, Y.S., Kim. S.E., Choi. Y.. Lee, K.H.. Ha, H.J.. Kim, B.-T., Ue. K.C. and Chi, D.Y.
I-ll Reductive Alkylation of Amines with ["F]Fluorobenzaldehyde and Sodium Cyanoborohydride: Scope and 29
Limitations of a Useful Radiosynthetic Reaction.
Negash, K., Waterhouse. R.N. and VanBrocklin. H.F.
1-12 A Rapid Catalytic Method for the Conversion of (4-"F]Fluoroiodobenzene to ["FJArylamines and to 32
StereodeFined ["F]Fluorophenylallylamines.
Lasne. M.-C.. Allain-Barbier, L. and Marriire, E.
1-13 Synthesis of Ether-Linked Analogs of ["F]Fluorinated Diacylglycerols. 35
Hatano. K.. Itoh, K. and Ido, T.
1-14 Specific Radioactivity and Radiochemical Yield in Electrophilic Fluorination: Case Study with ['*F]CFT. 38
Bergman. J.. Lehikonen, P. and Solin, O.
1-15 ["F]Fluorobenzyltrozamicol; An Efficient Synthetic Approach. 40
Negash, K., Morton, T.E. and VanBrocklin. H.F.
1-16 Labeling of ['*F]Fliilicasone Propionate with {"F]Fluoroiodoinethane. 43
Zheng. L. and Berridge, M.S.
1-17 Synthesis of [F-18]-l-Amino-3-Fluorocyclopentane-l-Carboxylic Acid (FACPC) and (F-18]-1-Amino-3- 46
Fluorocyclohexane-1-Carboxylic Acid (FACHC) for In Vivo Studies of Amino Acid Transpon by PET.
Shoup. T.M. and Goodman, M.M.
xix
XX Contents
1*18 Synthesis of (“F]-Difluoromcthylene and Trifluoromethylated Aromatic Compounds Using ['*F]-Labcled 48
Tetrabutylammonium Dihydrogen Trifluoride.
Josse. O.. Marchand-Brynaert, J. and Labar, D.
1-19 Direct N.C.A. "p-Fluorination of Halo- and Alkylarenes via Corresponding Diphenyiodonium Salts. SO
Gail, R., Hocke, C. and Coenen. H.H.
I>20 Convenient Synthesis Route to N.C.A. "p-Labclled Sympathomimctics Based on Norepinephrine. S3
Ermert. J.. Hamacher, K. and Coenen, H.H.
I>21 Synthesis of [P-181-PIuoroetanidazole • A New Nitroimidazole Tracer of Hypoxia. S6
Tewson. T.J.
I>22 Synthesis of the Stereoisomers of [P-18]-Pluoropropanoloi, a Tracer for the P-Adrenergic Receptor. S8
Tewson. T.J. and Stekhova, S.
1-23 Development of a Radiosynthesis for 3’-(P-18]Pluoro-3’-Deoxynucleosidcs. 60
Grierson. J.R.. Shields, A.P. and Eary, J.P.
1-24 Novel Synthesis of the Enantiomers of N,\-Dibenzyl-a-Bromo-P-Alanine Benzyl Ester, Precursors for 63
['*P]PBAL and Purification and Pormulation of l'*P]PBAL.
Prenant. C.. Brady, P., Luthra, S.K., Namolingam, V., Sergis, A.N. and Price, P.M.
1-25 Synthesis of Substituted Diaryliodonium Salts and Investigation of Their Reactions with No-Carrier-Added 6S
["PlPluoride.
Shah. A.. Widdowson, D.A. and Pike, V.W.
1-26 An Unexpected Rearrangement in the Reaction of 2-0-Methane-Sulfonyl-P-D-Mannopyranose with 68
["pJPluoride.
De Groot. T.. Bormans, G., Mortelmans, L. and Verbruggen, A.
I- 27 Development of P-18 Labeled 2-Nitroimidazole Analogs as Hypoxia Imaging Agents. 70
Shiue. C.-Y.. Shiue, G.G., Lim, J.-L., Labar, D., Baird, I., James, B., Skov, K., Dolbier, B., Koch, C. and
Alavi, A.
II- l 2-[’‘Br]Bromophenyl-Metapyronc. (l-(2-[’‘Br)Bromophenyl-2-methyl-2-(3-pyridyl)-l- 73
propanone. Synthesis and Biodistribution.
Loc'h. C.. Zolle, I., Damani, L.A., Halldin, C., Mitterhauser, M. and Mazifere, B.
11-2 Investigation of nirfo-Carboranes as Hydrophilic Pendant Groups for Astatination of Biomolecules. 76
Applications to an Astatinated Biotin Derivative.
Wilbur. D.S.. Hamlin, D.K., Poulon, C.P., Zalutsky, M.R. and Pathare, P.M.
11-3 Development of Norepinephrine Transporter (NET) Binding Radiopharmaceutical for Detecting 79
Myocardial Disease: Heterogeneity of NET DisUibution in Myocardium of Diabetic Rats and Evaluation of
fR)-2-Iodotomoxetine as a Ligand for NET.
lida. Y.. Kiyono, Y., Tamaki, N., Magata, Y., Konishi, J., Yokoyama, A. and Saji, H.
II-4 Regiospecific Synthesis of 3,3’-((2-['^I]Iodo-l,l’-Biphenyl)-4,4’-Diylbis(Azo))Bis[4-Amino-l- 81
Naphtalenesulphonic AcidjDisodium Salt.
Kabalka, G.W., Akula. M.R. and Zhang, Z.Y.
II-5 Synthesis of 9-Amino-7['*’l]Iodo-l,2,3,4-Tetrahydroacridine: A Radiotracer for Mapping 83
Acetylcholinesterase.
Akula. M.R. and Kabalka, G.W.
II-6 Synthesis and Characterization of lodinated Adenosine Derivatives as Selective A| and Aj Receptor 85
Imaging Agents.
Zhuang. Z.-P.. Kung, M.-P., Liang, B. and Kung, H.P.
II-7 Cyclic Amide Derivatives of 4-(2’-Methoxy-)phenyl-l-[2'-(N-2”-Pyridinyl-)-(p-lodobenzamido-]- 88
ethylpiperazine (/7-MPPI) as 5-HT| a Receptor Ligands.
Zhuang. Z.-P.. Kung, M.-P., Mu, M. and Kung, H.P.
Contents xxi
II-8 Preparation of 5-(*’'l]Iodo- (['^'l]FlAU) and 5-[*"At]Astato-l-(2-Deoxy-2-Ruoro-P-D- 91
ArabinofuranosyOuracil ([’"At]FAAU) by a Halodestannylation Reaction.
Vaidvanathan. G.. Affleck, D.J., Welsh, P., Li, J., Schoultz, B.W. and Zalutsky, M.R.
II-9 Synthesis of a Lipophilic, Radioiodinated Ligand with High Affinity to Amyloid Protein in Alzheimers 94
Disease Brain Tissue.
Mathis. C.A.. Mahmood, K., Debnath, M.L. and Klunk, W.E.
IMO Organotin Derivatives Anchored to Insoluble Polymers. Application to the Labelling of 2-('^l)- 96
lodolisuride.
Berthommier, E., Chalon, S., Delmond, B., Dumartin, G., Marchi, F., Mauclaire. L. and Pereyre, M.
IMl Synthesis and Biological Evaluation of 3-(2-Fluoroethyl)-8-[4-[2’-(4'-('“l]Iodothienyl))-4-Oxobutyl]-1- 97
Phenyl-1,3,8-Triazaspiro[4,S]Decan-4-one (FE41TS); A New Potent and Selective Dopamine D2 Receptor
Antagonist for SPECT.
Shi. B.. Kilts, C., Lambert, P., Ely, T., Camp, V. and Goodman, M.M.
1M2 Synthesis of ['“l]N-Methyl-3-(2-Hydroxy-5-lodopent-4-Enyl)-4-Acetoxypiperidine, An Acetylcholine 100
Analogue.
Ueda. T.. Irie, T., Fukushi, K., Namba, H., lyo, M., Takaloku, K., Yomoda, 1.. Ni.shiura, M. and
Nagatsuka, S.
11-13 Synthesis and Quality Assurance of Radioiodinated 2'-Fluoro-2’-Deoxy- l-P-D-Arabinofuranosyl-S- 103
[•I]lodo-Uracil.
Balatoni, J.A., Finn. R.D.. Tjuvajev, J.G., Larson, S.M. and Blasberg, R.G.
11-14 Preparation and Biological Characterization of a New Generation of Biotin Derivatives; (3- 104
HalogenobenzoyOnorbiotinamide (XBB) and ((5-HaIogeno-3-Pyridinyl)carbonyl)norbiotinamide (XPB),
Labeled with Iodine or Astatine.
Foulon. C.F.. Alston, K.L. and Zalutsky, M.R.
11-15 N.C.A. Radioiodination of Weakly Activated Arenes Using Thallium-Tris(trifluoroacetate). 107
Mennicke, E., Henneken, H., Holschbach. M. and Coenen, H.H.
11-16 Reactions of Diary liodonium Saits with No-Canier-Added [^^Br]Bromide and ("C]Cyanide. 109
McCarron. J.A.. Dowsett, K. and Pike, V.W.
11-17 Preparation and Evaluation of N-Acetylated Anthracycline Analogues for Radiolabelling with Iodine-124 III
and Bromine-76: Potetial PET Radiotracers for the In Vivo Assessment of Multidrug Resistance.
Sosabowski. J.. Zweit, J., Coley, H., Sosabowski, M.H., Wilbur, D.S, Hamlin, D., Camochan, P. and
Judson, I.
11-18 Investigation of Chemical Purity and Stability of Iodine-131 Metaiodobenzylguanidine. 114
Trtic. T.. Maksin, T., Vuksanovic, L. and Zagar, I.
11-19 Preparation of 4- and 6-[’‘Br]Bromometaraminol, Two PET Tracers for the Adrenergic Nerve 117
System.
Langer. O.. Dolld, F., Loc'h, C., Halldin, C., Coulon, C., Vaufrey, F., Crouzel, C., NJgren, K. and
Maziire, B.
11-20 Synthesis of N-Succinimidyl-4-[^^Br]Bromobenzoate and its Use in Conjugation to Proteins and S'- 120
Modified Oligonucleotides.
Yngve. U.. Hedberg, E., Tolmachev, V. and Lingstrom, B.
11-21 Labelling of Boron Containing Compounds with Halogen Isotopes. 122
Tolmachev. V.. Lundqvist, H., Sivaev, I., Orlova, A., Sjoberg, S., Olsson, P. and Gedda, L.
11-22 In Vivo Evaluation of Closo-Dodecaborate as a Linker for Attachment of Iodine Isotopes to 125
Radiopharmaceuticals.
Tolmachev. V.. Lundqvist, H., Carlsson, J., Sivaev, I., Orlova, A. and Sundin, A.
11-23 Rapid Preparation of S-['^I]Iodo-2’-Deoxyuridine by lododestannylation. 128
Koziorowski. J. and Weinreich, R.
xxii Contents
IIM A Comparison of Plasma Protein Binding of the Renal-Radiopharmaceuticals. 129
Okarvi. S.M.. Gretasdottir, J., Bake, B. and Volkmann, R.
III-2 Application of the Deuterium Isotope Effect to Enhance PET Signal by Impeding Tracer Metabolism; 130
Synthesis of Deuterium and Fluorine-18 Dual-Labeled Altanserin and its Nitro Precursor.
Tan. P.-Z.. Baldwin, R. M., Soufer, R., Van Dyck, C. H., Charney, D.S. and Innis R.B.
III-3 Radiometabolites of ['*F]Altanserin in Rats and Humans: 4-(p-['*F]Fluorobenzoyl)Piperidine and 133
l‘*F]Altanserinol.
Baldwin, R.M., Tan. P.-Z.. Van Dyck, C. H., Al-Tikriti, M., Amici, L., Roth, B., Khan, N., Soufer, R.,
Charney, D.S. and Innis, R. B.
111-4 A Radiotracer Technique For Determining Apparent pKa of Receptor-Binding Ligands. 136
Zoghbi. S. S.. Baldwin, R.M., Seibyl, J., Charney, D.S., and Innis, R.B.
III-5 Achieving Balanced Resolution in Radiopharmacological Studies: Tc-Labeled BMS 194,796. 139
Nickles. R.J.. Taylor, M.D., Mulnix, T.L., Roberts, A.D., Schueller, M.J., Kulago, A.A., deJesus, O.T.,
Brown, W.D., Whitesell, L.F., Carlson, K.C. and Stone, C.K.
III-6 Metabolism of Radioiodinated Benzamide Derivatives BZA and IMBA. 142
Mohammed, A., Lehmann, W.D. and Eisenhut. M.
III-7 Metabolism of No Carrier Added 2-[’*F]Fluoro-L-Tyrosine in Free Moving Rats. 145
Aerts. J.. Plenevaux, A., Lemaire, C., Brihaye, C. and Luxen, A.
III-8 Tissue Distribution, Autoradiography and Metabolism in Rats of p-['*F]MPPF: 5-HTia Antagonist. 148
Plenevaux. A.. Aerts, J., Lemaire, C., Brihaye, C., Le Bars, D., Mekhsian, P., Weissman, D., Pujol, J.F.,
Comar, D. and Luxen, A.
III-9 The Metabolite Pattern of ['^IjEpidepride in Human Plasma Determined with a Gradient HPLC Method. 151
Bergstrom. K.A.. Halldin, C., Yu, M.X., Swahn, C.-G., Akerman, K.K., Hiltunen, J., Tiihonen, J., Kuikka,
J.T., Lassen, N., Widebeck, C. and Farde, L.
IIMO Metabolite Pattern of Radioiodinated E-(R,R)-IQNP in Rodent and Primate Plasma. 154
Bergstrom. K.A.. McPherson, D.W., Halldin, C., Greenbaum, M., Hiltunen, J., Swahn, C.-G., Ito, H.,
Ginovart, N., Hall, H., Larsson, S., Schnell, P.-O., (Russ) Knapp Jr., F.F. and Farde, L.
III-ll Localization of Nicotinic Acetylcholine Receptors in Human Brain Using ['*F]Norchlorofluoroepibatidine 157
with Autoradiography and a Phosphor-Imaging Plate.
Ding. Y.-S.. Brady, D., Gatley, S.J., Dewey, S.L., Fowler, J.S., Volkow, N.D., Liang, F., Carrol, F.I. and
Kuhar, M.J.
III-12 Effect of Insulin on Extracellular Kinetics and Tissue Metabolism of Dcoxyglucose in Rats: In Vivo Study 159
Using Microdialysis and ['*F]FDG.
Haaoaranta. M.. Paul, R., Grbnroos, T., Bergman, J., Aalto, S., Minn, H. and Solin, O.
IIM3 Synthesis of Two Radiolabeled Metabolites of ("F] Altanserin: ["F)3-[2-[4-(4-Fluorophenylmethanol)-l- 161
Piperidinyl]ethyl)-2,3-Dihydro-2-Thioxo-4-( 1 H)-Quinazolinone and ['*F)4-(4-Fluoro-Benzoyl)piperidine.
Mason. N.S.. Haung, Y., Holt, D.P., Perevuznik, J.J., Lopresti, B.J. and Mathis, C.A.
III-14 Choice of Chromatographic Methods for the Routine Analysis of Partially Acety lated 2- 163
[ ‘ *F]Fluorodeoxy glucose.
Gee. A.D.. Bender, D., Rasmussen, I., Stocks-Gee, G., Larsen, V. and Larsen, H.
III-15 Distribution and Metabolism of the Antitumour Agent [''CJDACA in Nude Mice Bearing Human Tumour 166
Xenografts of Glioma, U87MG and Non-Melanotic Melanoma, A375M.
Osman. S.. Rowlinson-Busza, G., Luthra, S.K., Brown, G.D., Brady, F., Baguley, B.C., Denny, W.A. and
Price, P.M.
IIM6 Distribution and Metabolism of [3-N-"C-Methyl]Temozolamide in Nude Mice Bearing Human Tumour 168
Xenografts of Glioma, U87MG, U373 and Non-Melanotic Melanoma, A375M.
Osman. S.. Rowlinson-Busza, G., Luthra, S.K., Brown, G.D., Brady, F., Stevens, M.F G., Jones. T. and
Price, P.M.
Contents xxiii
III-17 Fate and Metabolism of the Prospective Myocardial apAdrenoceptor Radioligand, [A/-Methylamido- 170
"C]GB67. in Rat.
Osman. S.. Law, M.P., Davenport, R.J., Pike, V.W., Giardinik, D., Gulini, U., Quaglia, W. and Camici,
P.G.
III-18 [Carbonyl-"C]WAY*10063S - Characterisation of the Appearance of Radioactive Metabolites in Rat, 173
Monkey and Human Plasma and Uptake of an Identified Radioactive Metabolite in Monkey Brain.
Osman. S.. Lundkvist, C., Pike, V.W., Halldin, C., McCarron, J.A., Swahn, C.-G., Ginovart, N., Luthra,
S.K., Farde, L. and Grasby, P.M.
III-19 Biodistribution and Metabolism of [£irer-"C]Propionyl-L-Camitine in Rats and Human Subjects. 176
Osman. S.. Law, M.P., Davenport, R.J., Pike, Rosen, S.D. and Camici, P.G.
III-20 Labelling of a Lipophilic Metabolite of ["CJRaclopride and Investigation of its Brain Uptake in a 179
Cynomolgus Monkey with PET.
Swahn. C.-G.. Halldin, C., Lundkvist, C., Olsson, H., Karlsson, P. and Farde, L.
III-21 Labelling of p-CIT-FP with Fluorine-18 Avoids Formation of Lipophilic Lablled Labelled Metabolites. 182
Lundkvist. C.. Halldin, C., Ginovart, N., Swahn, C.-G. and Farde, L.
III-22 Identification of the Major Metabolites of In-111 -DTPA-D-Phe-1 -Octreotide Formed In Vitro. 185
Lanahan. M.V.. Bass, L.A., Duncan, J.R., Erion, J.L., Srinavasan, A., Schmidt, M.A. and Anderson, C.J.
111-23 Analysis of Liver Metabolites of Copper Radiopharmaceuticals In Vivo. 187
Bass. L.A.. McCarthy, D.W., Gitlin, J.D., Anderson, C.J. and Welch, M.J.
III-24 Species Specific Metabolism Differences of the Nitric Oxide Synthase Inhibitor S-2-(''FlFluoroethyl- 190
Isothiourea ({‘‘FjFEITU).
McCarthy. T.J. and Welch, M.J.
III-25 PET as a Biopharmaceutical Tool • Intranasal and Inhaled Administration of ["CjZanamivir, An Influenza 193
Virus Neuraminidase Inhibitor.
Westerberg. G.. Bergstrom, M., Cass; L.M., Dandiker, Y. and LUngstrom, B.
111-26 Attomole Level Capillary-LC-MS Analysis I9S
Hvllbrant. B.. Tyrefors, N., Markides, K. and LSngstrom, B.
Ill-27 LC-Radio-UV Coupled to MS for Irtiproved Sensitivity and Selectivity in Analysis of PET- 197
Radiopharmaceuticals.
Hvllbrant. B.. Tyrefors, N., Markides, K. and L;Ingstrbm, B.
111-28 Extraction of "C-Labelled Metabolites in Tissue Using Supercritical Ammonia. 199
Jacobson, G.B., Gustavsson. S.-A.. Moulder, R., Lu, L., Bergstrom, M., Markides, K.E. and LUngsUrom, B.
III-29 Bioanalysis of Dopamine and Metabolitesin Blood Following Administration of "C-L-DOPA or "C-6- 202
Fluoro-L-DOPA in Monkey and Man.
Torstenson. R.. Hartvig, P., Lindner, K.-J., Tedroff, J., Nilsson, A., Bastani, S., Fasth, K.-J. and
Lingstrdm, B.
III- 30 Tracing Oxygen Metabolism by Use of the Positron Emitter Oxygen-15. 205
Watanabe. Y.. Hyllbrant, B. and Lingstrom, B.
rV-1 Remote Controlled Preparation of [alpha-"C]-3,4-Dimeihoxybenzyl Bromide - A Convenient Alkylating 208
Intermediate in [beta-"C]-L.DOPA Synthesis
Mosevich. I.K.. Kuznetsova, O.F., Fedorova, O.S. and Korsakov, M.V.
IV- 2 Improved (‘^NJAmmonia Yield from Water Targets Using Methane Gas 211
Krasikova. R.S.. Fedorova, O.S., Korsakov, M.V., Landmeier Bennington, B. and Berridge, M.S.
IV-3 Traces in Fluorine Containing Impurities in the Mannose Triflate and their Adverse Effect on the 214
Radiochemical Yield of 2-'*FDG
Chirakal. R.
IV-4 Radionuclidic Contaminants in "F-Fluoride Produced Using a High-Pressure Water Target and Their 217
Adverse Effect on the Production of 2-'*FDG
Chirakal. R.. Lui, E., Culbert, P.A., Webber, C., Chen, J.J., Firnau, G., Coates, G. and Nahmias, C.
xxtv Contents
IV-S Improvements to the Robotic Synthesis of ["F]FDG and Considerations on the Base-Assited Hydrolysis of 219
the Intermediate 2-['‘F]Fluoro-l,3.4,6-Tetra-0-Acetyl-D-Glucose.
Boeni. A.. Pascali, C., Iwata, R., Schiavini, M., Cucchetti, G., De Sanctis, V., Decise, D., Crippa, F.,
Chiesa, C. and Bombardieri, E.
IV>6 A Convenient Semi-Automated System for Optimising the Recovering of Aqueous ["F]Fluoride from 222
Target
Pascali. C.. Bogni, A., Remonti, F., Decise, D., Cucchetti, G., De Sanctis, V., Schiavini, M., Crippa, F.,
Chiesa, C. and Bombardieri, E.
IV-7 Preparation of ["C]Labelled Methyl Iodide Using HI Adsorbed on Alumina and Silica. 225
Koviics. Z.. Sarkadi, 6. and Szelecs6nyi, F.
IV-8 Optimal Polymer-Supported ['*F]Fluorinating Agents for On-Column Preparation of 2-Deoxy-2- 227
[' F]FIuoro-D-Glucose.
Ohsaki. K.. Endo, Y., Yamazaki, S., Tomoi, M. and Iwata, R.
IV-9 Optimisation of ['*F]FDG-Production Using Commercially Available SPE-Cartridges. 229
Ziilsu-a. S.. Medema, J., Elsinga, P.H., Notohamiprodjo, G. and Vaalburg, W.
IV-10 In-Target Production of ['^N]Ammonia Using a Circulating Target In Combination with a Bolus Delivery 232
System.
Medema. J.. Elsinga, P.H. and Vaalburg, W.
IV-11 Chemometrical Optimisation of the Single Mode Cavity Assisted Synthesis of L-[l-"C]Tyrosine. 235
Luurtsema. G.. Elsinga, P.H. and Vaalburg, W.
IV-12 Microwave Improved Synthesis of p-["F]MPPF, 5-HTia Antagonist and PET Studies on Cat Brain. 238
Le Bars. D.. Ginovart, N., Lemaire, C., PIcnevaux, A., Aeits, J., Pujol, J.F., Luxen, A. and Comar, D.
IV-13 New Multi-Purpose Autosynthesis Apparatus for Production of Radiopharmaceuticals. 240
Yang. D.J.. Tansey, W., Wallace, S., Inoue, T., Dobbs, F.R., Cherif, A., Kim, E.E. and Podoloff, D.A.
IV-14 Study on Automated Syntheses of l^["C]Amino Acids Using Immobilized Enzyme Columns. 243
Sasaki. M.. Ikemoto, M., Haradahira, T., Tanaka, A., Watanabe,Y. and Suzuki, K.
IV-IS Excitation Function Measurement of '“'Ar(p,3n)’*K Reaction and a New Production System for a Saline 246
Solution of ”K*.
Nagatsu, K., Kubodera, A. and Suzuki. K.
IV-16 A Complete Remote Control System for Reliable Routine Production of ["FJAItanserin. 249
Tan. P.-Z.. Baldwin, R. M., Soufer, R., Garg, P.K., Charney, D. S. and Innis R. B.
IV-17 Preparation of Radiochemically Pure "C-Propyl Iodide and "C-Ethyl iodide Using a Gas Chromatographic 252
Column for Labeling PET Tracers.
Ishii. S.. Ishiwata, K., Shinoda, M., Maekawa, S., Yamamoto, H. and Senda, M.
rV-18 Automated Production of Carrier-Free Radiolanthanides. 254
Dadachova. E.. Izard, M. and Mirzadeh, S.
IV-19 Synthesis of ['*F]FDG with Alkaline Hydrolysis on a Low Polarity Solid Phase Support. 256
Lemaire. C„ Damhaut, P.. Lauricella, B., Morelle, J.-L., Monclus, M., Van Naemen, J., Mulleneers, E.,
Aerts, J., Plenevaux, A., Brihaye, C. and Luxen, A.
IV-20 Simplified Purification and Synthesis of '*F-Setoperone. 258
Adam. M.J.. Lu, S., Jivan, S. and Huser, J.
IV-21 A Simplified Purification of ‘ ‘C-Methylphenidate Using lon-Exchangc- and C-18 SEP PAKs. 259
Adam. M.J.. Lu, S., Huser, J. and Ding, Y.-S.
IV.22 A High-Yield '’'Os/'’""Ir Generator. 260
Packard. A.B.. Day, P.J. and Treves, S.T.
IV-23 A Kit Formulation for Preparation of [’’^TcJTRODAT-1: A New Dopamine Transporter Imaging Agent. 263
Kung. M.-P.. Plossl, K., Meegalla, S.K. and Kung, H.F.
Contents XXV
IV>2S Development of a Routine System for the Production of ‘^Zn/^^u Generator at Low Energy Compact 269
Cyclotron.
Szelecs6nvi. F.. Sziics, Z. and Fenyvesi, A.
IV-27 Solid Phase Supported Reaction of N.C.A. H"CN with Arabinose: A Simplified Synthesis of [l-"C]Glu- 273
cose.
Bender. D. and Gee, A.D.
lV-28 Mechanisms Involved in the Production of Nitrogen-13 Labeled Ammonia in a Cryogenic Target. 275
Firouzbahkt. M.L.. Schlyer, D.J., Ferrieri, R.A., Wolf, A.P. and Fowler, J.S.
IV-29 New Starategies in Designing Ultra-Microscale Syntheses Using Methyl Iodide. 277
Ferrieri. R.A.. Garcia, E., Fowler, J.S. and Wolf, A.P.
IV-30 Spectroscopic Studies of Hot-Atom Processes in Nitrogen Gas Targets During Proton Bombardment. 280
Solin. O.. Hkllsten, U., Aho, K. and Lindblom, P.
IV-31 Production of Astatine-211 via the ^Bi(a,2n)^"At Reaction with Curved Natural Bismuth Internal 283
Targets.
Wieland. B.W.. Schoultz, B.W., Larsen, R.H. and Zalutsky, M.R.
IV-32 Separation of [‘*F]Fluoride from ["0]Water and Single-Vessel Synthesis of 2-['*FlFluoro-2-Deoxy-D- 286
Glucose Using Kryptofix* 2.2.2.
Zhang. Z.Y.. Zigler, S.S. and Kabalka, G.W.
IV-33 Automatic Determination of Rf Values in TLC Analyses. 289
Mikecz. P.. T6th, G., Dodd, M., Chaloner, F. and Sharp, P.F.
IV-34 Production of ('^N]NH3 from Methane - Revival of an Old Method. 291
Mikecz. P.. Dodd, M., Chaloner, F. and Sharp, P.F.
IV-35 Refinements and Improvements for Bisinuth-213 Production and Use as a Targeted Therapeutic 293
Radiopharmaceutical.
Finn. R.D.. McDevitt, M., Scheinberg, D., Jurcic, J., Larson, S.M., Sgouros, G., Humm, J., Curcio, M.,
Brechbiel, M., Gansow, O., Geerlings Sr., M., Apostolidis, C. and Molinet, R.
IV-37 New Nuclear Data Relevant to the Production of the Positron Emitting Radioisotopes '^1 and '**1. 297
Oaim. S.M.. Hohn, A., Scholten, B., Tdrkinyi, F., Kovics, Z., Tdkdcs, S. and Coenen, H.H.
IV-38 Production of ”Co and ^’Co via (p, x) Ractions on ’*Ni. 299
Reimer, P., Oaim. S.M.. Blessing, G., Spellerberg, S. and Coenen, H.H.
IV-39 Rapid Synthesis and Purification of "C-Labelled Benzyl Iodides Using a CIS-Solid Phase Matrix. 301
Gee. A.D.
IV-40 The Use of Vented Sterile Filters in the Automation of Preparative HPLC Injections. 304
Gee. A.D. and Bender, D.
IV-41 A Simplified Production of High Specific Radioactivity ["C]Labelled Phosgene, "COCIj. 306
Link. J.M. and Krohn, K.
IV-42 A Simply Automated Process for "C-Carboxylation Reactions Leading to "C.Labelled 309
Radiopharmaceuticals in High Specific Radioactivity.
Davenport, R.J., McCanon. J.A.. Dowsett, K., Turton, D.R., Poole, K.G. and Pike, V.W.
lV-43 Production of 'At-Labeled Humanized Anti-TAC Using an Internal and External Bismuth Target. 312
Schwartz. U.P.. Plascjak, P., Beitzel, M.P., Gansow, O.A., Eckelman, W.C. and Waldmann, T.A.
IV-45 The Adaptation of Hydrogen-Bond-Assisted Alkylation to Robotic Preparation of ["CjFlumazenil. 317
Fedorova. O.S.. Krasikova, R.N., Korsakov, M.V., Nigren, K., Maziire, B. and Halldin, C.
IV-46 A HEPA-Filtered Air Controlled Automated System for Methyltriflate. Production and Methylation of 320
PET Radioligands.
Larsen. P.. Sandell, J., Printz, G., Johnstrbm, P., Lundkvist, C., Nilsson, S.-O., Stone-Elander, S., Swahn,
C.-G., Sbderholm, P., Thorell, J.-O. and Halldin, C.
XXVI Contents
rV-47 Synthesis of (“C] Acetone and ["C]Carazolol on Nuclear Interface PET Tracer Synthesizer. 323
Soloviev. D.. Matarrese, M., Berridge, M., Neutro, F., Galli Kienie, M. and Fazio, F.
IV-48 High Purity Production and Potential Applications of Copper-60 and Copper-61. 325
Bass. L.A.. McCarthy, D.W., Jones, L.A., Cutler, P.D., Shefer, R.E., Klinkowstein, R.E., Schwartz, S.W.,
Cutler, C.S., Lewis, J.S., Anderson, C.J. and Welch, M.J.
IV-49 On-Line Production of ["CJCyanogen Bromide. 328
Westerberg. G. and Lingstrdm, B.
IV- 50 A New Synthesis of FDG Suitable for Regional Distribution with Productions of Over 2 Ci FDG Using the 330
FDG Microlab.
Ulin. J.. DahlsU'dm, K. and Kiselev, M.
V>1 Preclinical Development of Holmium-166 Microspheres, A Potential Radiopharmaceutical for Intrahepatic 332
Liver Tumour Therapy; Radiolabelling, Animal Distribution and Radiation Dose Estimation.
Naidovski. L.. Hetherington, E., Dadachova, K., Izard, B., Belbin, K., Klemp, P.F.B., Martindale, A.A.
and Turner, J.H.
V- 2 Investigation of Biotin Dimers and Trimers for Increasing the Quantity of Radioactivity on Cancer Cells in 335
Tumor Pretargeting, /n Vitro Demonstration of Streptavidin Cross-Linking.
Wilbur. D.S.. Hamlin, D.K., Pathare, P.M. and Weerawarna, S.A.
V-3 Radiosynthesis of Tamoxifen Analogues for Imaging Endometrial Disease. 338
Cherif. A.. Delpassand, E.S., Wallace, S., Cromeens, D., Zareneyrizi, F., Podoloff, D.A. and Yang, D.J.
V-4 Bi-213 for Alpha-Particle-Mediated Radioimmunotherapy 341
Boll, R.A., Mirzadeh. S.. Kennel, S.J., DePaoli, D.W. and Webb, O.F.
V-5 Synthesis and /n Vivo Evaluaton of "C-Labeled Ethionine and Propionine as Tumor Detecting Agents by 344
PET: A Pilot Study for Development of '*F-Labeled Methionine Analogs.
Ishiwata. K.. Kasahara, C., Hatano, K., Ishi, S. and Senda, M.
V-6 Production and Quality Assurance of 5-['^I]Iodo-2'-Deoxyuridine for Functional Imaging of Cell 346
Proliferation In Vivo.
Weinreich. R.. Wyer, L., Crompton, N., Gunther, I., Roeicke, U., Leenders, K.L., Knust, E.J., Finn, R.D.
and Blasberg, R.G.
V-7 Carbon-8 Radiofluorination of Purines: A General Approach to Probe Design for Gene Therapy in 348
Humans.
Barrio. J.R.. Namavari, M., Srinavasan, A., Gambhir, S., Cherry, S., Herschman, H., Phelps, M.E. and
Satyamurthy, N.
V-8 PET Imaging Agents for Hypoxic Tumor: F-18 Labeled Niuoimidazole Analogues. 349
Jeong. J.M.. Lee. Y.J.. Kim, C.. Chang, Y.S.. Kim. Y.J.. Lee. D.S., Chung, J.-K., Lee. M.C., Koh, C.-S.,
Cho, J.-H. and Yang, D.J.
V-9 Synthesis of (R)-(-)-4’-Cyano-3-((4-['“l]Iodophenyl)sulfonyl]-2-Hydroxy-2-Methyl-3’- 351
(trifluoromethyOpropionanilide: A Potential SPECT Agent for Evaluating Prostate Cancer.
Kabalka, G.W., Akula. M.R.. Zhang, Z.Y.. Dalton, J.T., Kirkovsky, L. and Miller. D.D.
V-10 Genetic Induction of Somatostatin Receptor in Tumor Cells Enhances Binding and Localization of 353
Radiolabelled Somatostatin.
Buchsbaum. D.J.. Rogers, B.E., Raben, D., McLean. S., Laffoon, K., Myracle, A., Grimes, C., Carpenter,
T., Bright, S., Olsen, C. and Curiel, D.T.
V-11 Platinum-195m Radiopharmaceuticals for Therapy. 354
Packard. A.B.. Spaeth, K., Kronauge. J.F. and Mirzadeh, S.
V-12 Synthesis and Preliminary Evaluation of ^"At-Labeled Bisphosphonates; Promising a-Particle Emitting 357
Agents for the Treatment of Bone Tumors.
Murud, K.M., Larsen. R.H.. Hoff, P., Bruland, 0.S. and Zalutsky, M.R.
CoiiUr.ts xxvii
V-13 Development of '“Ho-Ho, Fe-Hydroxide (HFH) and '“Ho-Hydroxyapatite (HA) for Radioembolization 360
Therapy of Liver.
Aneelbereer. P.. Kvatemik, H. and Casta, J.
V>14 Preparation of a-Particle Emitting Radiopharmaceuticals for Radiotherapy: Radiolytic Degradation of an 363
^"At-Labeied Acylation Agent and its Stannyl Precursor.
Schoultz. B.W.. Larsen, R.H. and Zalutsky, M.R.
V-15 Indium-111 Labeled Indium(III)-DTPA-Folate as a Radiopharmaceutical for Targeting Tumor-Associated 36S
Folate Receptors: The Effect of Tumor Size on Targeting Selectivity and Radiochemical Analysis of
Excreted Tracer.
Mathias. C.J.. Waters, D.J., Wang, S., Low, P.S. and Green, M.A.
V-16 Biodistribution of Lipophilic Monocationic ^^Ga-Bis(salicylaldimine) Radiotracers, ^^^c-SESTAMIBI, 368
and “F-FDG in an MDA-435 Mammary Tumor Mouse Model.
Mathias. C.J.. Wey, S.-P., Sledge Jr., G.W. and Green, M.A.
V-17 An Improved Radiosynthesis of 4-["C-carf>on>'/)Temozolomide Using ("C-corbo/iy/lMethylisocyanate. 371
Brown, G.D., Brady, F.. Luthra, S.K., Prenant, C., Stevens, M.F.G., Sergis, A.N. and Price, P.M.
V-18 Labelling of Defroxamine Folate with Zirconium-89: A Potential Tumour Targeting PET 372
Radiopharmaceutical.
Sosabowski. M.H.. Sosabowski, J. and Zweit, J.
V-19 Synthesis of ['^I]Iodoaminoglutethimide, A Possible Radioligand for the Visaualisation of the Aromatase 37S
Enzyme in Breast Carcinoma by SPECT.
De Vos. F.. Vandewiele, C., Siegers, G. and Dierckx, R.
V-20 Synthesis and In Vivo Biodistribution of the Tyrosine Kinase Inhibitor, [Methoxy-'‘C]PD 153035. 377
Johnstrom. P.. Fredriksson, A., Thorell, J.-O., Hassan, M., Kogner, P., Borgstrdm, P., Ingvar, M. and
Stone-Elander, S.
V-21 Preclinical Evaluation of 4-['*F]Fluoroprolines as Tracers for Tumor Imaging: Diastereomeric Effects on 380
Metabolism and Uptake.
Wester. H.J.. Hertz, M., Senekowitsch-Schmidtke, R., Hamacher, K., Schwaiger, M. and Stdeklin, G.
V-22 RDG-Peptides for Tumor Targeting: Biological Evaluation of Radioiodinated Analoges and Introduction 383
of a Novel Glycosylated Peptide with Improved Biokinetics.
Haubner. R.. Wester, H.J., Senekowitsch-Schmidtke, R., Diefenbach, B., Kessler, H., Stdeklin, G. and
Schwaiger, M.
V-23 Determination of Tumor Dosimeu^ for Copper-64-TETA-Octreotide by PET Imaging in a Tumor-Bearing 386
Rat Model.
Lewis. J.S.. Jones, L.A., Cutler, P.D., McCarthy, D.W., Bass, L.A., Lanahan, M.V., Schwartz, S.W. and
Anderson, C.J.
V-24 Evaluation of Cu-64-Labeled Segments of Type-IV Collagen as Tumor Imaging Agents. 389
Edwards. W.B.. Anderson, C.J., Fields, C.G., Fields, G.B. and Welch, M.J.
V-25 ^^Br-Bromodeoxyuridine as a Proliferation Marker with PET - Preclinical Validation Studies. 391
Fasth, K.-J., Bergstrom. M.. Hedberg, E., Cheng, A., Lu, L., Wu, F., Bergstrom, E., Tolmachev, V. and
Lingstrdm, B.
V-26 Radiolabelled DNA Interacting Compounds. 394
Henssen. C.. Carlsson, J., Koziorowski, J. and Sjdberg, S.
V-27 Synthesis of Carbon-11 Labeled l-Amino-3-[2-(7-(2-Hydroxyethyl)-l,7-Dicarba-WDO-Dodecaboran(12)- 395
yl)ethyl]cyclobutanecarboxylic Acid: A PET Agent for Use in BNfTT Treatment Planning.
Srivastava, R.R., Kabalka. G.W. and Longford, C.P.D.
V-28 Synthesis of MAG-Taxol Labelled with Carbon-14 in the Polymeric Chain. 397
Giribone. D.. Orzi, F. and Fontana, E.
V-29 High Specific Activity Radiohalogenation of Organotin DNA. 400
Dougan. H.. Hobbs, J.B., Weitz, J.I. and Lyster, D.M.
Contents
VI>1 Labelling Characteristics of Phosphorus-Nitrogen Based Bifunctional Ligands. 404
Okarvi. S.M.. Angelov, C.M., Suresh, M.R. and Cavell, R.G.
VI-2 Labelling Characteristics of Different Thiol Protective Groups for MAG3. 40.S
Okarvi. S.M.
VI-3 A New Potential Myocardial Perfusion Imaging Agent ’’"TcN-MIBI. 406
Wang. X.. Zhang, X. and Zhang, J.
VI-5 Usefulness of X-Ray Absorption Spectroscopy in the Characterization of Technetium and Rhenium- 411
Labelled Peptides.
Jankowskv. R.. Johannsen, B., Noll, B., Spies, H., Dinkelborg, L.M., Hilger, C.S. and Semmler, W.
VI-6 Derivatives of 6-Methyl-8a-Amino-Ergoline: Synthesis and Affinity to the Dopamine-D2 Receptor. 414
Spies. H.. Noll, B., Noll, S., Brust, P., Syhre, R. and Johannsen, B.
VI-7 Syntheses of N-(2-Diethylaminoethyl)benzamides Suitable for ”"Tc Complexation. 416
Titsch, U., Mohammed, A., Wagner, S., Oberdorfer, R. and Eisenhut. M.
VI-8 Effect of Different Acylating Agents on pi of anti-Tac dsFv and Renal Uptake of Acylated Tc-99m 419
Labeled Anti-Tac dsFv.
Kim. I.S.. Yoo, T.M., Kim, M.-K., Kobayashi, H., Le, N., Han, E.S., Wang, Q.-C., Pastan, I., Carrasquilio,
J.A. and Paik, C.H.
VI-9 Acylation with Glycolate Lowers pi of Anti-Tac dsFv and Reduces Renal Uptake of Its Tc-99m Label. 422
Kim. I.S.. Yoo, T.M., Kobayashi, H., Kim, M.-K., Le, N., Wang, Q.-C., Pastan, I., Carrasquilio, J.A. and
Paik, C.H.
VI-10 Use of Tc-99m-MAG3-Biocytin Scintigraphy to Study the Hepatobiliary Function and Related In Vivo 425
Biochemistry.
Kim. M.-K.. Song, B.J., Seidel, J., Soh, Y., Kim, I.S., Le, N., Kobayashi, H., Green, M.V., Carrasquilio,
J.A. and Paik, C.H.
VI-II Specificity of Diastereomers of [’*^c]TRODAT-l as Dopamine Transporter Imaging Agents. 428
Pldssl. K.. Meegalla, S.K., Stevenson, D.A., Mu, M., Kung, M.-P. and Kung, H.F.
VI-12 Synthesis and Characterization of Tc-99m Labeled Imidazo[l,Sa][l,4]Benzodiazepine Derivatives as 431
Potential CNS Benzodiazepine Receptor Imaging Agents.
Ova. S.. Kung, M.-P., Mu, M. and Kung, H.F.
VI-13 Structure-Activity Relationship of [’’"TcJTRODAT-1 Derivatives as New Dopamine Transporter Imaging 434
Agents.
Meegalla. S.K.. Plbssl, K.. Kung, M.-P., Mu, M. and Kung. H.F.
VI-14 Synthesis and Characterization of a [*’*"Tc]SCH23390 Derivative as a Selective Dopamine Dj Receptor 437
Imaging Agent.
Chumoradit. S.. Kung, M.-P., Mu, M., Hou, C. and Kung, H.F.
VI-15 ’’"Tc-EIBI Uptake in Multidrug-Resistant Tumor Cell Lines and Xenografts. 439
Barbarics. E.. Croop, J.M., Cohen, D., Chan, C., Davison. A. and Jones, A.G.
VI-16 Synthesis and Properties of (MCl3(CO)3]^' (M = Tc, Re) as a Versatile Source of the “/flc-M(CO)3” Moiety 442
for Application in Radiopharmacy. Reactions with Sulfur Containing Ligands.
Albeiio. R.. Schibli, R., Egli, A., Abram, U., Hiibener, R., Kaden, T.A., Pietzsch, H.-J. and Schubiger, P.A.
VI-17 The Remarkable Coordination Properties of the “/ac-M(CO)3” Moiety of [MBr3(CO)3]*' (M = Tc, Re). 443
Substitution Behaviour with Nitrogen Donors in View of an Application in Radiopharmacy.
Egli. A.. Alberto, R., Schibli, R., Schaffland, A.O., Abram, U., Abram, S., Kaden, J.A; and Schubiger,
P.A.
VI-18 In Vivo Studies of Tc-99m Complexes Derived from New Water-Soluble 444
Dithio(hydroxymethyl)bisphosphines (P2S2).
Smith, C.J., Katti. K.V.. Higginbotham, C., Volkert, W.A. and Kctring, A.R.