[131I]iodotropapride: a cerebral dopamine D2 receptor ligand.

Poster (1990, August 26)

Imaging serotonin-S2 receptors in humans with PET and the selective S2 antagonist [18F]altanserin. Preliminary results.

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1990, June 19), 31

Synthesis and tissue distribution of four Se-labeled tertiary amines, potential brain pH imaging agents.

in International Journal of Radiation Applications and Instrumentation. Part B : Nuclear Medicine and Biology (1990), 17(6), 601-7

Four new tertiary amines: bis(3-N,N-dimethyl aminopropyl)selenide (PROMOSE), bis(3-N-(morpholino)propyl)selenide, N-methyl-selenomorpholine and N-phenyl-selenomorpholine structurally related to MOSE ... [more ▼]

Four new tertiary amines: bis(3-N,N-dimethyl aminopropyl)selenide (PROMOSE), bis(3-N-(morpholino)propyl)selenide, N-methyl-selenomorpholine and N-phenyl-selenomorpholine structurally related to MOSE proposed by Kung and Blau, have been labeled through a radiochemical procedure suitable for both 75Se and 73Se. The radiochemical yields of the carrier added synthesis ranged between 64 and 85% for the four 75Se labelings and was 64% EOB time corrected for [73Se]PROMOSE. The chemical and radiochemical purities were higher than 99% after chromatographic purifications. The n-octanol/phosphate buffer partition coefficients (P) were measured at various pH (6.5-8) for each compound and the tissue distributions of PROMOSE in rats were also carried out. The experimental results showed a good correlation between the P = f(pH) function and the in vivo behaviour of the considered compound. PROMOSE was selected for further investigations as a brain pH indicator. [less ▲]

Synthesis of (R)-(-)- and (S)-(+)-4-fluorodeprenyl and (R)-(-)- and (S)-(+)-[N-11C-methyl]-4-fluorodeprenyl and positron emission tomography studies in baboon brain.

in Journal of Medicinal Chemistry (1990), 33(7), 2015-9

(R)-(-)- and (S)-(+)-alpha-methyl-beta-4-(fluorophenyl)-N-methyl-N- propynylethylamine [R)-(-)- and (S)-(+)-4-fluorodeprenyl) were synthesized via the reaction of 4-fluorobenzaldehyde with nitroethane ... [more ▼]

(R)-(-)- and (S)-(+)-alpha-methyl-beta-4-(fluorophenyl)-N-methyl-N- propynylethylamine [R)-(-)- and (S)-(+)-4-fluorodeprenyl) were synthesized via the reaction of 4-fluorobenzaldehyde with nitroethane followed by reduction with lithium aluminum hydride to produce racemic 4-fluoroamphetamine, which was resolved by recrystallization with L- or D-N-acetylleucine to yield (R)-(-)-4-fluoroamphetamine or (S)-(+)-4-fluoroamphetamine in greater than 96% enantiomeric excesses and in yields of 42 and 39%, respectively. Alkylation with propargyl bromide gave (R)-(-)- or (S)-(+)-4-fluoronordeprenyl which was reductively methylated (Borch conditions) to produce (R)-(-)- or (S)-(+)-4-fluorodeprenyl. Alkylation of (R)-(-)- or (S)-(+)-4-fluoronordeprenyl with carbon-11 labeled methyl iodide gave (R)-(-)- or (S)-(+)-[N-11C-methyl]-4-fluorodeprenyl in a radiochemical yield of 30-40%. Comparative PET studies of the two labeled enantiomers in baboons showed a significantly lower retention of radioactivity in the striatum for the (S)-(+) enantiomer relative to the (R)-(-) enantiomer. [less ▲]

Synthesis of carbon-11 and fluorine-18 labeled 4-fluorodeprenyl as probes for functional monoamine oxidase.

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1989), 30

Evaluation of [73Se]PROMOSE as a tracer of the human cerebral pH.

Poster (1988, October 10)

Fast chemical synthesis of [75Se]L-selenomethionine.

in International Journal of Radiation Applications and Instrumentation. Part A : Applied Radiation and Isotopes (1987), 38(1), 59-61

A fast chemical synthesis of high specific activity [75Se]L-selenomethionine (10 Ci/mmol--370 GBq/mmol) is described with a view to 73Se labeling and PET studies. The overall radiochemical yield of the ... [more ▼]

A fast chemical synthesis of high specific activity [75Se]L-selenomethionine (10 Ci/mmol--370 GBq/mmol) is described with a view to 73Se labeling and PET studies. The overall radiochemical yield of the preparation is better than 80%. The purification method uses commercially available reverse phase HPLC columns and 9% NaCl as mobile phase. The final labeled compound is obtained in less than 3 h and the chemical, radiochemical and optical purities of the L-isomer are higher than 99.0%. [less ▲]

New trends in selenium-labeled compounds synthesis.

in Journal of Labelled Compounds & Radiopharmaceuticals (1982), 19