Microfluidic radiosynthesis of [¹⁸F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors

• Thomas Lee Collier,
• Steven H. Liang,
• J. John Mann,
• Neil Vasdev and
• J. S. Dileep Kumar

Beilstein J. Org. Chem. 2017, 13, 2922–2927, doi:10.3762/bjoc.13.285

• ). Agonist properties of FEMPT on 5-HT1AR were estimated by [35S]GTPγS binding in membranes of CHO cells which stably express human 5-HT1AR. A dose-dependent increase in [35S]GTPγS binding was induced by FEMPT. Maximal FEMPT stimulated [35S]GTPγS binding Emax was 100% of that seen with 5-HT and an EC50 of 85

The Shono-type electroorganic oxidation of unfunctionalised amides. Carbon–carbon bond formation via electrogenerated N-acyliminium ions

• Alan M. Jones and
• Craig E. Banks

Beilstein J. Org. Chem. 2014, 10, 3056–3072, doi:10.3762/bjoc.10.323

• analogues prepared (Scheme 23; 98–100) showed competitive binding of the native ligand with IC50’s = 32, 80, 5 µM using a radioiodinated peptide binding to the NK1 receptor in Chinese Hamster Ovary (CHO) cells (native ligand IC50 = 0.3 nM). The preparation of arginine mimetics is an ongoing challenge for

New GABA amides activating GABA_A-receptors

• Peter Raster,
• Andreas Späth,
• Svetlana Bultakova,
• Pau Gorostiza,
• Burkhard König and
• Piotr Bregestovski

Beilstein J. Org. Chem. 2013, 9, 406–410, doi:10.3762/bjoc.9.42

• of Catalonia (IBEC) and Institució Catalana de Recerca i Estudis Avançats (ICREA), 08028 Barcelona, Spain 10.3762/bjoc.9.42 Abstract We have prepared a series of new and some literature-reported GABA-amides and determined their effect on the activation of GABAA-receptors expressed in CHO cells

• GABAA-receptor channels in whole-cell patch-clamp recordings. New GABA-amides, however, gave moderate activation responses with a clear structure–activity relationship suggesting some of these compounds as promising molecular tools for the functional analysis of GABAA-receptors. Keywords: CHO-cells

• compounds was tested by using CHO cells transiently expressing GABAA-receptors in the configuration (α1-GFP + β2 + γ2Long). To analyze the functional properties of the compounds, we performed monitoring of ionic currents using whole-cell patch-clamp techniques. First, concentration-response curves for GABA

Bioorthogonal metabolic glycoengineering of human larynx carcinoma (HEp-2) cells targeting sialic acid

• Arne Homann,
• Riaz-ul Qamar,
• Sevnur Serim,
• Petra Dersch and
• Jürgen Seibel

Beilstein J. Org. Chem. 2010, 6, No. 24, doi:10.3762/bjoc.6.24

• processes involved in infection, inflammation or tumor formation [1]. Recent studies have shown that the surface of a T-cell line (Jurkat), Chinese hamster ovary (CHO) cells, cervical adenocarcinoma (HeLa) cells as well as many other cell types can be labelled with bioorthogonal, that is metabolically inert