Prediction of the binding mode of imidacloprid and related compounds to house-fly head acetylcholine receptors using three-dimensional QSAR analysis

The binding activity of imidacloprid and related compounds to nicotinic acetylcholine receptors (nAChR) of house flies was measured by use of radioactive α-bungarotoxin as a ligand. Variations in the activity were examined three-dimensionally using comparative molecular field analysis (CoMFA). The CoMFA results suggest that one conformer among the four stable ones is active and provide support for one of the proposed binding models for this class of compound, in which the nitrogen atom of the pyridine ring and the nitrogen atom at the 1-position of the imidazolidine ring interact with the hydrogen-donating and electron-rich sites of nAChR, respectively. The CoMFA field map showed that the nitroimino moiety and a portion of the imidazolidine ring were mainly surrounded by a sterically and electrostatically sensitive region of nAChR. © 1998 Society of Chemical Industry     

Effect of glimepiride and nateglinide on serum insulin and glucose concentration in healthy cats

Glimepiride and nateglinide are two common oral hypoglycemic agents currently being used with humans suffering from Type 2 diabetes mellitus. Neither drug has been tested with cats thus far and it is currently unknown whether either of these drugs exert any effect in cats or not. The objective of this study was to determine the effect of glimepiride and nateglinide on glucose and insulin responses in healthy control cats, in order to determine their potential use in diabetic cats. The intravenous glucose tolerance tests was carried out since it is an excellent test for evaluating pancreatic β-cell function for insulin secretion. Alterations in the insulin secretion pattern can be perceived as the earliest sign of β-cell dysfunction in many species, including cats. Nateglinide demonstrated a quick action/short duration type effect with serum glucose nadiring and insulin response peaking at 60 and 20 minutes, respectively. Alternatively, glimepiride is medium-to-long acting with serum glucose nadiring and insulin response peaking at 180 minutes and 60 minutes, respectively. Nateglinide’s potency was evident allowing it to induce a 1.5–2 higher preliminary insulin peak (3.7?±?1.1 pg/ml) than glimepiride’s (2.5?±?0.1 pg/ml), albeit only for a short period of time. Because glimepiride and nateglinide have a shared mode of action, no significant differences in overall glucose AUC_0-360min (24,435?±?2,940 versus 24,782?±?2,354 mg min/dl) and insulin AUC_0-360min (410?±?192 versus 460?±?159) in healthy control cats were observed. These findings may provide useful information when choosing a hypoglycemic drug suited for the treatment of diabetic cats depending on the degree of diabetes mellitus the cat is suffering from.     

Effects of β‐carotene‐enriched dry carrots on β‐carotene status and colostral immunoglobulin in β‐carotene‐deficient Japanese Black cows

Data from 18 β‐carotene‐deficient Japanese Black cows were collected to clarify the effects of feeding β‐carotene‐enriched dry carrots on β‐carotene status and colostral immunoglobulin (Ig) in cows. Cows were assigned to control or carrot groups from 3 weeks before the expected calving date to parturition, and supplemental β‐carotene from dry carrots was 138 mg/day in the carrot group. Plasma β‐carotene concentrations in the control and carrot groups at parturition were 95 and 120 μg/dL, and feeding dry carrots slightly improved plasma β‐carotene at parturition. Feeding dry carrots increased colostral IgA concentrations in cows and tended to increase colostral IgG₁, but colostral IgM, IgG₂, β‐carotene and vitamin A were not affected by the treatment. Feeding dry carrots had no effects on plasma IgG₁, IgA and IgM concentrations in cows, but plasma IgG₁ concentrations decreased rapidly from 3 weeks before the expected calving date to parturition. These results indicate that feeding β‐carotene‐enriched dry carrots is effective to enhance colostral IgA and IgG₁ concentrations in β‐carotene‐deficient cows.     

Solute diffusion into cell walls in solution-impregnated wood under conditioning process III: effect of relative humidity schedule on solute diffusion into shrinking cell walls

This study has focused on solute diffusing into cell walls in solution-impregnated wood under conditioning, process of evaporating solvent. The purpose of this paper was to clarify the RH- (relative humidity-) schedule that promotes the solute diffusion into shrinking cell walls during conditioning. The wood samples impregnated with a 20 mass% aqueous solution of polyethylene glycol (PEG1540) was conditioned with a temperature of 40?°C to the equilibrium point at the RH where the samples swelled maximally. The samples were subsequently conditioned at 40?°C under the schedules including four ways of RH-decrease steps where the cell walls shrunk. The amount of solute (PEGs) diffused into cell walls during the conditioning logarithmically increased with increasing the number of the RH-decrease steps. This was well explained by the theoretical model that describes the solute diffusion into shrinking cell walls. It is clarified from the model that the RH, or moisture content of the sample, should be decreased as gradually as possible to increase the total amount of diffused solute into shrinking cell walls, and that the amount of diffused solute is smaller for the lower moisture content. The model also suggests that effect of change in RH schedule on change in total amount of diffused solute does not depend on solute diffusivity in the sample under drying in a vacuum over phosphorous pentoxide, and that impregnated wood should be conditioned under natural convection rather than forced convection for promoting the diffusion into shrinking cell walls.     

Winter nitrate uptake by the temperate deciduous tree <Emphasis Type="Italic">Quercus serrata</Emphasis>

Winter nitrogen use in deciduous species is largely uncharacterized. We investigated nitrate uptake in the fine roots of a deciduous oak (Quercus serrata Thunb. ex. Murray). We conducted a ¹⁵N-labeling experiment using saplings of Q. serrata in the winter. During three weeks of labeled nitrate application, the concentration of ¹⁵N in the fine roots increased significantly. The amount of nitrogen absorbed, as nitrate, was 1.16 ± 1.02 mg N g DW⁻¹, equivalent to 7.6 ± 5.8% of the total nitrogen content. Our results indicate that Q. serrata saplings have significant potential for nitrate uptake in the fine roots in midwinter (i.e., in the absence of leaves). Although a significant amount of nitrogen applied as nitrate was accumulated, nitrate concentration in the fine roots remained low during the labeling period. Furthermore, significant nitrate reductase activity was detected. These data suggest that Q. serrata saplings can assimilate nitrate in the fine roots in midwinter.