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The synthesis of 1-(5-chloro-2-{2-[(2R)-4-(4-[18F]fluorobenzyl)-2-methylpiperazin-1-yl]-2-oxoethoxy}phenyl)urea ([18F]4), a potent nonpeptide CCR1 antagonist, is described as a module-assisted two-step one-pot procedure. The final product was obtained utilizing the reductive amination of the formed 4-[18F]fluorobenzaldehyde (2) with a piperazine derivative 3 and sodium cyanoborohydride. After HPLC purification of the final product [18F]4, its solid phase extraction, formulation and sterile filtration, the isolated (not decay-corrected) radiochemical yields of [18F]4 were between 7 and 13% (n=28). The time of the entire manufacturing process did not exceed 95 min. The radiochemical purity of [18F]4 was higher than 95%, the chemical purity ⩾60% and the enantiomeric purity >99.5%. The specific radioactivity was in the range of 59–226 GBq/µmol at starting radioactivities of 23.6–65.0 GBq [18F]fluoride. Copyright © 2006 John Wiley & Sons, Ltd.

V Snieckus [Queen's University, Canada]—The Directed Ortho Metalation—Cross Coupling Symbiosis in Aromatic Synthesis. N Geach, GP Randall, CJ Winfield [Scynexis, UK]—Isotopically Labelled 4-Formylimidazole. A Studer [Marburg University, Germany]—New Concepts in Tin-Free Radical Chemistry. AC Spivey, C Noban [Imperial College London, UK]. T Jones [Sheffield University, UK], GJ Ellames, A Kohler [Sanofi-Synthelabo, UK], H Wadsworth [Amersham Biosciences, UK]—Opportunities for Isotope Labelling via Solid Phase Synthesis with Organogermanium Linkers. J Rieke-Zapp [Aventis Pharma, Germany]—Optimization of Reaction Conditions on mg-Scale by Use of Screening Devices. S Stone-Elander [Karolinska Institute, Sweden]—Rerouting Radiochemistry with Microwaves. J Goehl, B Perry, D Leuck, J Windels, M Marx [EaglePicher Pharmaceutical, USA]—GMP and Radiolabelled Syntheses of Capsaicin. J Kruger, B Manmontri, G Fels [Paderborn University, Germany]—H/D-Exchange in Aromatic Systems Using Transition Metal Catalysis. F Wust, T Kniess, R Bergmann [Research Centre Rossendorf, Germany]—Synthesis of a11C-Labelled Nonsteroidal Glucocorticoid Receptor Ligand as Potential Radiotracer for Imaging Brain Glucocorticoid Receptors with Positron Emission Tomography (PET). P Mading, F Fuchtner [Research Centre Rossendorf, Germany], CS Hilger [Schering AG, Germany]. M Halks-Miller, R Horuk [Berlix Biosciences, USA]—18F-Labelling of a Potent Nonpeptide CCR1 Antagonist for the Diagnosis of the Alzheimer's Disease. L Matei, C Postolache, V Fugaru, E Condac, A Dinischiotu, M Costache [Bukarest University, Romania]—Use of [1,2-3H] Testosterone in 5α- Reductase Enzymatic Activity Dosing in Dermal Fibroblast Cultures from Polycystic Ovarian Patients. L Matei, C Postolache, V Fugaru [Bukarest University, Romania]—Synthesis and Stability Studies of Acyclovir Labelled with Tritium. J Atzrodt, V Derdau [Aventis Pharma, Germany]—Studies on Directed Ortho-Metalation (DoM) as Convenient Tool for the Synthesis of Labeled Compounds.

Rat C-6 glioma cells were grown on a sponge foam matrix in an organ culture system and the cell cycle parameters, including the growth fraction (GF), were assessed after autoradiography. the zones of growth consisted of a compact upper layer (UL) at the gaseous interface, a central necrotic layer and a deeper lower layer (LL) which invaded the matrix. the fraction of continuously labeled mitoses (FCLM) was similar in both the UL and LL cells. the derivatives of the FCLM curves obtained in three experiments gave an average modal TG2 of 5 hr. A mathematical model relating GF, TG2, TC and labeling index as a function of time, LI(t), was devised for cells in a steady state exposed continuously to tritiated thymidine and was applied to data obtained from UL cells. A mean GF of 9% (range: 8–10%) and a mean cell cycle time (TC') of 27 hr (range: 13–47 hr) were obtained. the mean TS was calculated to be 11 hr (range: 8–16 hr) by the method of grain counts per mitotic figure or grain index (GI). Knowledge of TS permitted alternative calculation of the cell cycle time from the equation TS/TC= LI(0)/GF: this gave a mean cell cycle time (TC) of 29 hr (range: 20–45 hr). Except for the GF, the cell kinetics were comparable to those of the same cell line grown in monolayer culture. the GF in the in vitro system described is in the lower range reported in some human malignant gliomas in vivo.

Neonatal rat brain astrocyte secondary cultures were established on nitrocellulose membrane filters (13-mm diameter Millipore disk) and on plastic coverslips in serum-supplemented medium. On these substrata, cultured astrocytes changed their shape from flat and polygonal to stellate in the absence of hormones or growth factor supplements. Cultures became confluent after 4 days, and astrocytes on nitrocellulose filters continued to differentiate morphologically and biochemically, as evidenced by extensive cytoplasmic process formation and glial fibrillary acid protein (GFAP) accumulation. Cultures were immunostained for GFAP and vimentin. mRNAs to GFAP, vimentin, alpha and beta tubulin, and actin also were detected by in situ hybridization with biotinylated cDNA probes. The astrocyte culture method on nitrocellulose provides a simple, versatile means of comparing undifferentiated, morphologically mature, reactive, and neoplastic astrocytes in vitro.