Evaluation of N-alkyl derivatives of radioiodinated spiperone as radioligands for in vivo dopamine D2 receptor studies: effects of lipophilicity and receptor affinity on the in vivo biodistribution.

A series of radioiodinated spiperone (2'-ISP) derivatives bearing amide N-alkyl substituents (N-methyl-2'-ISP, N-ethyl-2'-ISP, and N-propyl-2'-ISP) were synthesized and evaluated as potential singlet photon emission computed tomographic radiopharmaceuticals for visualizing dopaminergic receptors. The lipophilicity of these ligands (i.e., the partition coefficient for octanol-phosphate buffer) increased as the chain length increased. Investigation of blood-brain barrier permeability in rats showed a parabolic relationship between the brain uptake index and the partition coefficient. In vitro competitive binding studies showed that the relative affinity for the dopamine D2 receptor was in the order of N-propyl-2'-ISP greater than 2'-ISP greater than N-methyl-2'-ISP approximately N-ethyl-2'-ISP. In vivo biodistribution studies showed that the initial brain uptake correlated fairly well with the brain uptake index and that the kinetics of the radioactivity specifically bound to the striatum were strongly influenced by the dopamine receptor binding affinity of the compounds. Thus, the in vivo behavior of these N-alkylated 2'-ISP derivatives involved a complex interplay between receptor affinity, lipophilicity, and blood-brain barrier permeability.     

Light-excited superhydrophilicity of amorphous TiO2 thin films deposited in an aqueous peroxotitanate solution

We report on the photoinduced superhydrophilicity of the surface of amorphous TiO2. Amorphous TiO2 thin films were prepared on self-assembled monolayers by the peroxotitanate-complex deposition (PCD) and liquid-phase deposition (LPD) methods. The surface morphology and topography were characterized in detail. The contact angles were 34 degrees and 66 degrees for the as-deposited thin films through the PCD and LPD methods, respectively, which slowly increased to about 70 degrees and 73 degrees after being stored in air. After irradiation by UV light, the contact angle vanished and the surface exhibited superhydrophilicity. The superhydrophilicity and hydrophobicity could be switched by alternatively exposing the surface to UV light and drying in an atmosphere filled with organic gases. Although the oxidation of the contamination on the surface has effects on the increase in hydrophilicity, the X-ray photoelectron spectroscopy results suggested that the superhydrophilicity was also related to the transformation of the Ti-OH groups to groups that have dangling bonds. This paper indicates that an amorphous TiO2 thin film does not need to be heated to obtain superhydrophilicity; such a self-cleaning surface can be achieved at room temperature by our newly developed environmentally friendly method.     

Hydrogen absorption and Li inclusion in a Pd cathode in LiOH solution

The amount of electrochemically absorbed hydrogen and lithium in a Pd cathode during electrolysis was measured quantitatively in LiOH solution. The electrode potential was also measured by the current interruption method. Inclusion of Li in Pd was found even at the potential of −0.22 V vs. RHE. This potential is far more positive than the reported UPD potential. Since Li was detected up to a depth of 200 nm, this phenomenon is not a simple UPD. The deposition of Li onto Pd and the formation of Pd---Li alloy are likely to occur at a much more positive potential than expected. The [H]/[Pd] ratio decreased gradually after 50 h electrolysis at a current density greater than 5 mA cm⁻².     

Selective determination of tryptophan-containing peptides through precolumn derivatization and liquid chromatography using intramolecular fluorescence resonance energy transfer detection.

A selective and sensitive fluorometric determination method for native fluorescent peptides has been developed. This method is based on intramolecular fluorescence resonance energy transfer (FRET) detection in a liquid chromatography (LC) system following precolumn derivatization of the amino groups of tryptophan (Trp)-containing peptides. In this detection process, we monitored the FRET from the native fluorescent Trp moieties (donor) to the derivatized fluorophore (acceptor). From a screening study involving 10 fluorescent reagents, we found that o-phthalaldehyde (OPA) generated FRET most effectively. The OPA derivatives of the native fluorescent peptides emitted OPA fluorescence (445 nm) through an intramolecular FRET process when they were excited at the excitation maximum wavelength of the Trp-containing peptides (280 nm). The generation of FRET was confirmed through comparison with the analysis of a non-fluorescent peptide (C-reactive protein fragment (77 - 82)) performed using LC and a three-dimensional fluorescence detection system. We were able to separate the OPA derivatives of the Trp-containing peptides when performing LC on a reversed-phase column. The detection limits (signal-to-noise ratio = 3) for the Trp-containing peptides, at a 20-microL injection volume, were 41 - 180 fmol. The sensitivity of the intramolecular FRET-forming derivatization method is higher than that of the system that takes advantage of the conventional detection of OPA derivatives. Moreover, native non-fluorescent amines and peptides in the sample monitored at FRET detection are weaker than those of conventional fluorescence detection.     

Critical behavior in random-spin systems with long-range interactions

Effects of the potential range of the interaction to critical behaviors of quenched random-spin systems are investigated in the limit M → 0 of the MN-component models by means of the renormalization-group theories. As static critical phenomena the stability of the fixed points is investigated and the critical exponents (η, γ, , crossover index) and the equation of state are derived. These phenomena are different from those in pure systems, for the positive specific heat exponent of the pure Heisenberg system.     

Differential real-space renormalization of thed-Dimensional Gaussian model

With the aid of the differential real-space method we derive exact renormalization group (RG) equations for the Gaussian model ind dimensions. The equations involved + 1 spatially dependent nearest-neighbor interactions. We locate a critical fixed point and obtain the exact thermal critical indexy _T = 2. A special trajectory of the full nonlinear RG transformation is found and the free energy of the corresponding initial state calculated.Supported by Deutsche Forschungsgemeinschaft through Sonderforschungsbereich 130 Ferroelektrika.     

Critical exponent η of isotropic spin systems with long and short-range interactions

Critical phenomena, in particular, the critical exponent η, in isotropic N-component spin systems with long and short range interactions are discussed in the regions of the weakly long-range, the intermediate-range, and the long-range potentials. The expressions for η in these three regions are derived and their stability is discussed.