A novel synthesis of 1,4-diarylpiperazines

1,4-Diarylpiperazines are readily prepared, generally in good yields, by the reaction of substituted aromatic amines with two thirds of an equivalent of tris(2-chloroethyl)phosphate.     

Investigating the vortex melting phenomenon in BSCCO crystals using magneto-optical imaging technique

Using a novel differential magneto-optical imaging technique we investigate the phenomenon of vortex lattice melting in crystals of Bi₂Sr₂CaCu₂O₈ (BSCCO). The images of melting reveal complex patterns in the formation and evolution of the vortex solid-liquid interface with varying field (H)/temperature (T). We believe that the complex melting patterns are due to a random distribution of material disorder/inhomogeneities across the sample, which create fluctuations in the local melting temperature or field value. To study the fluctuations in the local melting temperature/field, we have constructed maps of the melting landscape T _m(H, r), viz., the melting temperature (T _m) at a given location (r) in the sample at a given field (H). A study of these melting landscapes reveals an unexpected feature: the melting landscape is not fixed, but changes rather dramatically with varying field and temperature along the melting line. It is concluded that the changes in both the scale and shape of the landscape result from the competing contributions of different types of quenched disorder which have opposite effects on the local melting transition.     

Energy dependence of multiplicity in proton-nucleus collisions and models of multiparticle production

This is a continuation of our earlier investigation (Gurtuet al 1974Phys. Lett. 50 B 391) on multiparticle production in proton-nucleus collisions based on an exposure of emulsion stack to 200 GeV/c beam at the NAL. It is found that the ratioR _em = 〈n _s〉/〈n _ch〉, where 〈n _ch〉 is the charged particle multiplicity in pp-collisions, increases slowly from about 1 at 10 GeV/c to 1·6 at 68 GeV/c and attains a constant value of 1·71 ± 0·04 in the region 200 to 8000 GeV/c. Furthermore,R _em = 1·71 implies an effectiveA-dependence ofR _A =A ^0.18,i.e., a very weak dependence. Predictions ofR _em on various models are discussed and compared with the emulsion data. Data seem to favour models of hadron-nucleon collisions in which production of particles takes place through adouble step mechanism,e.g., diffractive excitation, hydrodynamical and energy flux cascade as opposed to models which envisage instantaneous production.     

Resonance in quantum dot fluorescence in a photonic bandgap liquid crystal host

Microcavity resonance is demonstrated in nanocrystal quantum dot fluorescence in a one-dimensional (1D) chiral photonic bandgap cholesteric-liquid crystal host under cw excitation. The resonance demonstrates coupling between quantum dot fluorescence and the cholesteric microcavity. Observed at a band edge of a photonic stop band, this resonance has circular polarization due to microcavity chirality with 4.9 times intensity enhancement in comparison with polarization of the opposite handedness. The circular-polarization dissymmetry factor g(e) of this resonance is ~1.3. We also demonstrate photon antibunching of a single quantum dot in a similar glassy cholesteric microcavity. These results are important in cholesteric-laser research, in which so far only dyes were used, as well as for room-temperature single-photon source applications.     

Tri-partite complex for axonal transport drug delivery achieves pharmacological effect

Background

Targeted delivery of pharmaceutical agents into selected populations of CNS (Central Nervous System) neurons is an extremely compelling goal. Currently, systemic methods are generally used for delivery of pain medications, anti-virals for treatment of dermatomal infections, anti-spasmodics, and neuroprotectants. Systemic side effects or undesirable effects on parts of the CNS that are not involved in the pathology limit efficacy and limit clinical utility for many classes of pharmaceuticals. Axonal transport from the periphery offers a possible selective route, but there has been little progress towards design of agents that can accomplish targeted delivery via this intraneural route. To achieve this goal, we developed a tripartite molecular construction concept involving an axonal transport facilitator molecule, a polymer linker, and a large number of drug molecules conjugated to the linker, then sought to evaluate its neurobiology and pharmacological behavior.

Results

We developed chemical synthesis methodologies for assembling these tripartite complexes using a variety of axonal transport facilitators including nerve growth factor, wheat germ agglutinin, and synthetic facilitators derived from phage display work. Loading of up to 100 drug molecules per complex was achieved. Conjugation methods were used that allowed the drugs to be released in active form inside the cell body after transport. Intramuscular and intradermal injection proved effective for introducing pharmacologically effective doses into selected populations of CNS neurons. Pharmacological efficacy with gabapentin in a paw withdrawal latency model revealed a ten fold increase in half life and a 300 fold decrease in necessary dose relative to systemic administration for gabapentin when the drug was delivered by axonal transport using the tripartite vehicle.

Conclusion

Specific targeting of selected subpopulations of CNS neurons for drug delivery by axonal transport holds great promise. The data shown here provide a basic framework for the intraneural pharmacology of this tripartite complex. The pharmacologically efficacious drug delivery demonstrated here verify the fundamental feasibility of using axonal transport for targeted drug delivery.     

Synthesis of some trifluoroethyl-substituted derivatives of aniline

A new procedure is presented for the preparation of N-trifluoroethylanilines by reaction of the appropriate aniline with ethyl trifluoroacetate or trifluoroacetic anhydride, followed by reduction with diborane in tetrahydrofuran. Yields are high unless the aniline carriers a carboyxl, carbonyl, olefin, or o-nitro substituent. several new N-substituted trifluoroacetamides and trifluoroethylanilines are reported.     

Nuclear charge radius of 12Be

The nuclear charge radius of (12)Be was precisely determined using the technique of collinear laser spectroscopy on the 2s(1/2)→2p(1/2,3/2) transition in the Be(+) ion. The mean square charge radius increases from (10)Be to (12)Be by δ(10,12)=0.69(5) fm(2) compared to δ(10,11)=0.49(5) fm(2) for the one-neutron halo isotope ^{11}Be. Calculations in the fermionic molecular dynamics approach show a strong sensitivity of the charge radius to the structure of ^{12}Be. The experimental charge radius is consistent with a breakdown of the N=8 shell closure.     

Nuclear charge radii of (21-32)Mg

Charge radii of all magnesium isotopes in the sd shell have been measured, revealing evolution of the nuclear shape throughout two prominent regions of assumed deformation centered on (24)Mg and (32)Mg. A striking correspondence is found between the nuclear charge radius and the neutron shell structure. The importance of cluster configurations towards N=8 and collectivity near N=20 is discussed in the framework of the fermionic molecular dynamics model. These essential results have been made possible by the first application of laser-induced nuclear orientation for isotope shift measurements.