Automated Synthesis of 68Ga-Labeled DOTA-MGS8 and Preclinical Characterization of Cholecystokinin-2 Receptor Targeting

The new minigastrin analog DOTA-MGS8 targeting the cholecystokinin-2 receptor (CCK2R) used in this study displays the combination of two site-specific modifications within the C-terminal receptor binding sequence together with an additional N-terminal amino acid substitution preventing fast metabolic degradation. Within this study, the preparation of ⁶⁸Ga-labeled DOTA-MGS8 was validated using an automated synthesis module, describing the specifications and analytical methods for quality control for possible clinical use. In addition, preclinical studies were carried out to characterize the targeting potential. [⁶⁸Ga]Ga-DOTA-MGS8 showed a high receptor-specific cell internalization into AR42J rat pancreatic cells (~40%) with physiological expression of rat CCK2R as well as A431-CCK2R cells transfected to stably express human CCK2R (~47%). A favorable biodistribution profile was observed in BALB/c nude mice xenografted with A431-CCK2R cells and mock-transfected A431 cells as control. The high tumor uptake of ~27% IA/g together with low background activity and limited uptake in non-target tissue confirms the potential for high-sensitivity positron emission tomography of stabilized MG analogs in patients with MTC and other CCK2R-related malignancies.     

Alternating π‐conjugated block copolymers with precise block length

A Sonogashira polycondensation reaction has been used to synthesize copolymers consisting of alternating oligo(p‐phenyleneethynylene) with a precise block length as an electron‐rich component and 1,4‐bis(2‐phenylene‐2‐cyanovinylene)benzene or 2,6‐bis(2‐pyridinylene‐ethynylene)pyridine as an electron‐poor component. The copolymers differ in the length of the phenyleneethynylene block (trimer or pentamer) and the content of the electron‐poor component. The length of the phenyleneethynylene block has no influence on the maximum wavelength. The electron‐poor cyano‐block component lowers the optical band‐gap energy of the copolymers. The value is equivalent to that of poly(cyano‐phenylenevinylene) (CN‐PPV) (2.3–2.4 eV). © 2005 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 43: 3574–3587, 2005     

Combined use of small-angle neutron scattering and atom probe tomography for the analysis of precipitates in a Fe-15 m% Co-25 m% Mo alloy

Atom probe tomography (APT) measurements were conducted to analyze nm-sized precipitates in a Fe-25 m% Co-15 m% Mo model alloy. Calculation of isoconcentration surfaces and application of cluster-search algorithms yielded the chemical compositions of matrix and precipitates. Small-angle neutron scattering (SANS) was performed in order to calculate the ratio of magnetic to nuclear scattering. This so-called A-ratio was compared with values calculated from the chemical information derived from the atom probe data. For this, the magnetism of the precipitates has to be taken into account. Ab-initio studies have been carried out to determine the magnetic moment of the precipitate phase. The results show that the extremely fine precipitates are ferromagnetic and exhibit near-equilibrium composition. In the very early stage of decomposition, however, the composition is different from near-equilibrium. The influences of the magnetism of the precipitates as well as of artifacts from atom probe measurements on the obtained results are discussed.     

Programmed Multiple C-H Bond Functionalization of the Privileged 4-hydroxyquinoline Template

The introduction of substituents on bare heterocyclic scaffolds can selectively be achieved by directed C−H functionalization. However, such methods have only occasionally been used, in an iterative manner, to decorate various positions of a medicinal scaffold to build chemical libraries. We herein report the multiple, site selective, metal-catalyzed C−H functionalization of a “programmed” 4-hydroxyquinoline. This medicinally privileged template indeed possesses multiple reactive sites for diversity-oriented functionalization, of which four were targeted. The C-2 and C-8 decorations were directed by an N-oxide, before taking benefit of an O-carbamoyl protection at C-4 to perform a Fries rearrangement and install a carboxamide at C-3. This also released the carbonyl group of 4-quinolones, the ultimate directing group to functionalize position 5. Our study highlights the power of multiple C−H functionalization to generate diversity in a biologically relevant library, after showing its strong antimalarial potential.     

Transportation of megawatt millijoule laser pulses via optical fibers?

Laser ignition is considered to be one of the most promising future concepts for internal combustion engines. It combines the legally required reduction of pollutant emissions and higher engine efficiencies. The igniting plasma is generated by a focused pulsed laser beam. Having pulse durations of a few nanoseconds, the pulse energy E _p for reliable ignition amounts to the order of 10 mJ. Different methods of laser ignition with an emphasis on fiber-based systems will be discussed and evaluated.     

The Bonebrake Theological Seminary: Top-Secret Manhattan Project Site

We discuss the top-secret Manhattan Project site established at the Bonebrake Theological Seminary in 1943 in Dayton, Ohio, where research on polonium and its production was carried out. The polonium produced there was then transported to Los Alamos to be used in a polonium–beryllium neutron source whose purpose was to ignite the plutonium implosion bomb that would be dropped on Nagasaki, Japan, on August 9, 1945. Our account is based primarily on the recollections of John J. Sopka, research physicist at the Bonebrake laboratory.     

Amino acid functionalisation of water soluble carbon nanotubes

High solubility of SWNTs and MWNTs in water is obtained by organic functionalisation; derivatisation with N-protected glycine is also easily achieved.     

A high statistics measurement of the Lambda(+)(c) lifetime

A high statistics measurement of the Lambda(+)(c) lifetime from the Fermilab fixed-target FOCUS photoproduction experiment is presented. We describe the analysis technique with particular attention to the determination of the systematic uncertainty. The measured value of 204.6 +/- 3.4 (stat) +/- 2.5 (syst) fs from 8034 +/- 122 Lambda(+)(c)-->pK(-)pi(+) decays represents a significant improvement over the present world average.     

On the geometry of master-slave synchronization

In 1990, Pecora and Carroll reported the observation that one can synchronize the orbits of two identical dynamical systems, which may be chaotic, by feeding state variables of one of them to the other one with no feedback, a phenomenon often called master-slave synchronization. We report here some results on the theory of master-slave synchronization for maps and flows, which are all inspired by a similar geometric and coordinate independent point of view to the one introduced in master-slave synchronization by Tresser, Worfolk, and Bass. Our results are variations on the theme that projection often can compensate for expansion.(c) 2002 American Institute of Physics.