Influence of d-glutamine and d-glutamic acid sequences in optical peptide probes targeted against the cholecystokinin-2/gastrin-receptor on binding affinity, specificity and pharmacokinetic properties.

Background: Image-based diagnosis of tumours can be advanced and improved by targeted strategies addressing malignant molecular structures. A promising molecular target is the cholecystokinin-2-receptor (CCK2R) which can be targeted by high-affinity peptides called minigastrins. Here we present how the imaging properties of minigastrins tagged with near-infrared fluorescence (NIRF) dyes can be modulated by the introduction of different spacer sequences.

Multifactorial diagnostic NIR imaging of CCK2R expressing tumors.

Optical imaging-based diagnostics identify malignancies based on molecular changes instead of morphological criteria in a non-invasive, irradiation free process. The aim of this study was to improve imaging efficiency by the development of a new Cholecystokinin-2-receptor targeted fluorescent peptide that matches the clinical needs regarding biodistribution and pharmacokinetics while displaying superior target specificity. Furthermore we performed multifactorial imaging of Cholecystokinin-2-receptor and tumor metabolism, since simultaneous targeting of various tumor biomarkers could intensely increase tumor identification and characterization.

Diagnosis of peritonitis using near-infrared optical imaging of in vivo labeled monocytes-macrophages.

Peritonitis is an inflammatory process characterized by massive monocytes-macrophages infiltration. Since early diagnosis is important for a successful therapeutic outcome, the feasibility for a selective labeling and imaging of macrophages for highly sensitive optical imaging was assessed. After in vitro incubation of mouse macrophages J774A.

A chromoreactand for optical sensing of amphetamines.

A bisazo dye is presented that undergoes a reversible chemical reaction with amphetamine in thin layers of plasticised PVC and changes its colour from blue to red. The sensitivity of the dye in the polymer layer covers the range from 0.3 to 30 mmol L(-1) amphetamine with a limit of detection of 0.

Benzotriazole-Mediated Conversions of para-H-Substituted Pyrylium, Benzo[b]pyrylium, and Xanthylium Salts into para-Position Functionalized Derivatives (An Indirect Electrophilic Substitution of Electron-Deficient Heteroaromatics).

4H-Substituted pyrylium 9, benzo[b]pyrylium 15, and xanthylium salts 22 react with benzotriazole to give the corresponding 4H-(benzotriazol-1-yl)pyrans 10, benzo[b]pyrans 16, or xanthenes 23. Novel anion precursors 10, 16, and 23 undergo smooth lithiations at the positions alpha to the benzotriazol-1-yl function, i.e.