NCA synthesis of an N-w-[18F]fluoroethyl analog of altanserine, a serotonine S2 receptor ligand.

in Journal of Labelled Compounds & Radiopharmaceuticals (1991), 30

NCA asymmetric synthesis of 6-[18F]fluoro-L-dopa.

in Journal of Labelled Compounds & Radiopharmaceuticals (1991), 30

Synthesis and preliminary animal studies of [131I]iodotropapride: a cerebral dopamine D2 receptor ligand.

in Journal of Labelled Compounds & Radiopharmaceuticals (1991), 30

Serotonine-S2 receptor imaging with [18F]altanserin and PET. Results in young normal controls.

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1991), 32

2 and 4-[18F]fluorotropapride, two specific D2 receptor ligand for PET.

in European Journal of Nuclear Medicine (1991), 18

Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats.

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1991), 32(12), 2266-72

No-carrier-added [18F]altanserin was synthesized by nucleophilic substitution of the corresponding nitro compound with [18F]fluoride in the presence of kryptofix 222 and K2CO3. After purification by ... [more ▼]

No-carrier-added [18F]altanserin was synthesized by nucleophilic substitution of the corresponding nitro compound with [18F]fluoride in the presence of kryptofix 222 and K2CO3. After purification by preparative HPLC, [18F]altanserin was produced in less than 2 hr with a radiochemical yield of 10% (EOS) and a specific activity of 0.8-1.3 Ci/mumol. In rats, the tracer localized rapidly in the whole brain (0.5% ID/g organ) with a high binding to the frontal cortex. The frontal cortex/cerebellum ratio increased with time and reached a plateau of 11 at 2 hr postinjection. This uptake in S2 receptor regions was saturable and could be blocked by pretreatment with various S2 antagonists. This radiopharmaceutical appears to be more selective for S2 receptor sites than other ligands available today and allows the study of S2 receptors under in vivo conditions. [less ▲]

[18F]Altansérine: nouveau radioligand des récepteurs sérotoninergiques pour la tomographie par émission de positons (TEP)

Poster (1990, August 22)

No-carrier-added regioselective preparation of 6-[18F]fluoro-L-dopa

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1990), 31(7), 1247-1251

Chemical processing for production of no-carrier-added selenium-73 from germanium and arsenic targets and synthesis of L-2-amino-4-([73Se]methylseleno) butyric acid (L-[73Se]selenomethionine).

in International Journal of Radiation Applications and Instrumentation. Part A : Applied Radiation and Isotopes (1990), 41(9), 829-38

The Ge(4He, xn) and 75As(p, 3n) reactions were compared as the best potential routes for routine production of selenium-73 (73Se) for medical applications. With 26 MeV alpha particles, available with ... [more ▼]

The Ge(4He, xn) and 75As(p, 3n) reactions were compared as the best potential routes for routine production of selenium-73 (73Se) for medical applications. With 26 MeV alpha particles, available with compact cyclotrons, the first reaction required an enriched 70Ge target of sodium metagermanate to give a production yield of 1 mCi/microAh (0.037 GBq/microAh) in a 105 mg/cm2 target. With 55 MeV protons the As(p, 3n) reaction on natural arsenic yielded 20 mCi/microAh (0.74 GBq/microAh) in a 685 mg/cm2 target. A simple method was developed and optimized for both targets in order to isolate and purify the no-carrier-added selenium in the elemental form with a radiochemical yield greater than 75% in less than 90 min. An automated radiochemical processing unit has been designed for the routine production of 100-150 mCi (3.7-5.5 GBq) batches of carrier-free 73Se ready for radiopharmaceutical labeling. 30 mCi (1.11 GBq) (EOS) of L-2-amino-4-([73Se]methylseleno) butyric acid (L-[73Se]selenomethionine) ready for injection with a specific activity of 5 Ci/mmol (185 GBq/mmol) (EOS) were obtained through a fast chemical synthesis. Radiation absorbed dose estimates for L-[73Se]selenomethionine have been determined. A value of 0.70 rem/mCi (0.19 mSv/MBq) administered was calculated for the risk from irradiation in man. The first human PET investigation with [73Se]selenomethionine showed a very good delineation between liver and pancreas. [less ▲]

A New Route for the Synthesis of [18f]Fluoroaromatic Substituted Amino Acids: No Carrier Added L-P-[18f]Fluorophenylalanine

in International Journal of Radiation Applications and Instrumentation. Part A : Applied Radiation and Isotopes (1987), 38(12), 1033-8

L-p-[18F]fluorophenylalanine was designed as a potential marker for probing protein synthesis in the human brain by positron emission tomography. This radiotracer has been synthesized using nucleophilic ... [more ▼]

L-p-[18F]fluorophenylalanine was designed as a potential marker for probing protein synthesis in the human brain by positron emission tomography. This radiotracer has been synthesized using nucleophilic displacement of the activated nitro group of p-nitrobenzaldehyde by NCA 18F- obtained from the 18O (p, n) reaction on enriched water. The L-form of the [18F]fluoroamino acid can be separated on an analytical scale chiral column. A typical production run of 22.2 GBq (600 mCi) of 18F obtained after a 10 microA.h bombardment of 18 MeV protons on 99.8% 18O-enriched water leads to a batch of 1.11 GBq (30 mCi) of NCA L-p-[18F]fluorophenylalanine after a total synthesis time of 120 min. [less ▲]