Comparative pharmacokinetics of 67Ga among the different routes of injection

The pharmacokinetic study of 67Ga-citrate (67Ga) following intravenous (i.v.), subcutaneous (s.c.) and intraperitoneal (i.p.) injection was performed in anesthetized rats using the repeated blood sampling method by cannulation technique into the external jugular vein. The disappearance of 67Ga from the blood following i.v. and s.c. injection was best fit a three-exponential equation. There was no significant difference between the areas under the curves following i.v. and s.c. injection of 67Ga. In the case of i.p. injection, the disappearance of 67Ga from the blood was described by a two-exponential equation. However, the maximum blood radioactivity was very low, and the disappearance rate of 67Ga from the blood was extremely slow compared to the other routes of injection. The conclusion from these results was that s.c. injection was as suitable as i.v. injection, but i.p. injection was not appropriate for the distribution study of 67Ga such as scintigraphy or autoradiography. However, i.p. route may be available for a special experiment which needs the long-time retention of 67Ga in the blood.     

Chemical release control: Carbamates of 3-vinylphenyl and 2-methacryloyloxyethyl isocyanates and perfume and herbicide alcohols

Polymerizable carbamates were synthesized from 3-vinylphenyl and 2-methacryloyloxyethyl isocyanates and perfume and herbicide alcohols, such as 2-phenethyl alcohol, citronellol, geraniol, 1-menthol, borneol, and 2-(2,4-dichlorophenoxy)- and 2-(2,4,5-trichlorophenoxy)ethyl alcohols. Copolymerization of these carbamate monomers and N-vinyl-2-pyrrolidone with AIBN in dioxane gave respective copolymers. Hydrolyses of both monomers and copolymers, however, required severe acid conditions, although different chemical structures gave different hydrolytic behaviors.     

Concomitant increase in putrescine incorporation with transferrin uptake into rat reticulocytes.

Concomitant increase in putrescine incorporation with transferrin uptake into rat reticulocytes was found. [14C]Putrescine incorporation occurred in the presence of transferrin at 37 degrees C. The subcellular distribution of incorporated [14C]putrescine showed that the incorporation in the plasma membrane time dependently increased. Both 125I-labeled transferrin uptake and [14C]putrescine incorporation decreased when ethylene glycol bis(2-aminoethyl ether)-N,N,N',N'-tetraacetic acid was added, while it increased with the addition of A23187.     

Presence of peroxyradicals in cigarette smoke and the scavenging effect of shikonin, a naphthoquinone pigment

Using a new method having been developed for the purpose of quantitative determination for peroxyradicals, the presence of peroxyradicals was proved in cigarette smoke. In brief, peroxyradicals in cigarette smoke were measured by ESR spectrometry coupled to non-reductive scavenging of 1,1-diphenyl-2-picrylhydrazyl (DPPH). As a result, peroxyradicals were found to be major reactive oxygen species (ROS) since the concentration of peroxyradicals recovered from cigarette smoke was much higher than that of any of other ROS (superoxide and hydroxyl radical) and nitric oxide. Furthermore, several antioxidants (ascorbic acid, reduced glutathione, epigallocatechin gallate, shikonin) were examined for scavenging activity against peroxyradicals in the cigarette smoke. Among them shikonin alone exerted the scavenging activity, suggesting that shikonin is promising antioxidant for cigarette filters because of its effectiveness against broad range of ROS including peroxyradicals, heat resistance, nonvolatility and high affinity to the filter.     

Interaction between amphiphiles and water molecules in concentrated bilayer aqueous colloids

Interaction between amphiphiles and water molecules in micelle or bilayer structure has been investigated using aqueous colloids of various amphiphiles through the rheological data and the spin-lattice relaxation timeT ₁ of the proton of water molecule.T ₁ of the water proton has been measured by the inversion recovery method and determined as a single exponential relaxation process.The chemical shift of the water proton is almost independent of the amphiphilic concentration; however, it shifts toward a higher magnetic field with increasing temperature in a way similar to that in pure water and in the amphiphilic aqueous systems. These facts mean that there is no significant difference in the magnetic field environment of the water protons in these systems.The water molecule is not necessarily bound in the fully developed micelle or bilayer (rod-like or lamella) structure which induces the high viscosity or high rigidity of the colloidal system. On the other hand, the water molecule is bound in the micelle colloids of amphoteric amphiphiles or amphiphiles whose molecular assembly creates a relatively strong electrostatic field. The activation entropy of the bound water is negative and this suggests that water molecules assume some ordered structure in the bound state.     

Synthesis of 2-, 4- and 5-(2-alkylcarbamoyl-1-methylvinyl)-7-alkyloxybenzo[b]furans and their leukotriene B4 receptor antagonistic activity

Variable benzo[b]furan derivatives having (E)- and (Z)-2-alkylcarbamoyl-1-methylvinyl groups at the 2-, 4- and 5-positions and a carboxylpropoxy or (1-phenyl)ethoxy group at the 7-position were prepared to find novel and selective leukotriene B4(LTB4) receptor antagonists. (E)-2-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4v) showed selective inhibition to the human BLT2 receptor (hBLT2). On the other hand, (E)-2-acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (7v) inhibited both human BLT(1) receptor (hBLT1) and hBLT2. The (E)-2-(2-diethylcarbamoyl-1-methylvinyl) group lay on approximately the same plane as the benzo[b]furan ring, whereas the (E)-4-(2-diethylcarbamoyl-1-methylvinyl) group had the torsion angle (45.7 degree) from the benzo[b]furan ring plane. However, the (Z)-(2-alkylcarbamoyl-1-methylvinyl)benzo[b]furans were inactive. The inhibitory activity depended on the conformation of the 2-diethylcarbamoyl-1-methylvinyl group.     

Level structure of the doubly odd nucleus 112In from the (p,nγ) reaction

Properties of the levels in ¹¹²In have been studied with the reaction ¹¹²Cd(p, nγ)¹¹²In. The level scheme of ¹¹²In below 1300 keV was constructed from the γ-ray excitation functions and γγ coincidences. In ¹¹²In, 22 excited states were observed and spins and parities of 8 excited states were newly assigned or restricted by comparing the measured angular distributions and linear polarizations of the deexciting γ-rays as well as the excitation functions of the residual levels with the predictions of the statistical compound nucleus model. Possible configurations of the low-lying levels are discussed in terms of their decay properties and the systematics of the excited states in the neighbouring doubly odd In isotopes.