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At least 19 recordsLinked to original sources
PubMed1984

Nasal drug delivery system of a quaternary ammonium compound: clofilium tosylate.

The blood levels of the [14C]clofilium ion in rats after various routes of administration of clofilium tosylate were compared. The results indicate that the blood levels after nasal administration were not statistically different from levels after intravenous administration (p greater than 0.05). Administration by the oral route resulted in considerably lower blood levels. Nasal administration of clofilium tosylate appeared to be superior to oral administration. Histological examinations of nasal mucosa were conducted. At the lower concentration, mild necrosis was observed, and large areas of mucosa were unaffected. However, necrosis of large areas of mucosa occurred after exposure to the higher concentration. Levels of radioactivity in heart, liver, lung, and kidney tissue, as a function of time, were also studied. Unlike the blood levels after nasal administration, the levels of radioactivity were persistent in heart tissue. The data suggest that the [14C]clofilium ion and/or metabolite concentrate in the heart and that blood levels of radioactivity may not be an accurate index of cardiac levels or biological response.

Administration, Intranasal↗
PubMed1975

Inhibition by 6-O-tosyl galactosides of beta-galactoside phosphorylation and transport by the lactose phosphotransferase system of Staphylococcus aureus.

The effect of various galactose derivatives, substituted at C-6, on the phosphoenolpyruvate:beta-galactoside phosphotransferase system of Staphylococcus aureus was studied. Cells were grown by an improved procedure, which resulted in a 5- to 10-fold increase in cell yield. The four protein components of the system were separated. A membrane fraction containing negligible levels of the soluble components was prepared by alternate cycles of sonic treatment and differential centrifugation. The in vitro system reconstituted from these fractions was used to test the ability of the galactose derivatives to inhibit the phosphorylation of lactose analogs, under conditions where the membrane-bound component, Enzyme IIlac, was rate limiting. Derivaites in which the hydroxyl group of C-6 was missing, or replaced by a fluoro, O-methyl, or carboxyl group had no affinity for Enzyme IIlac, as judged by their inability to inhibit phosphorylation. Surprisingly, derivatives containing arylsulfonyl groups at C-6 were potent inhibitors; the O-tosyl compound has an apparent affinity five times that of galactose. The arylsulfonyl substitution in an absolute requirement; neither O-benzyl or O-methanesulfonyl derivatives were inhibitory. The specificity of the inhibition by tosyl derivatives parallels that of unsubstituted substrates; tosyl galactosides of the beta configuration were inhibitory, but those of the alpha configuration were not. The tosyl derivatives also strongly inhibited the uptake of lactose analogs into whole cells; the requirement for the arylsulfonyl moiety was again observed. The chemical analogy between the tosyl galactosides and possible intermediates in the transport-phosphorylation step catalyzed by Enzyme IIlac provides a possible explanation for the unexpected properties of these derivatives.

Bacterial Proteins↗
PubMed1985

[Synthesis of N-alpha-benzyloxycarbonyl-4-amidinophenylalanine amides as thrombin inhibitors].

Based on 4-cyanophenylalanine, the title compounds had been obtained by benzyloxycarbonylation of the amino group, subsequent formation of the activated ester by 4-nitrophenol, its aminolysis and at least change of the cyano function to the amidine function via thiocarbamides and thioimid acid esters. The inhibitor effect against thrombin of the pyrrolidid 16 is analogous to those of the adequate N alpha-tosyl compound.

Chemical Phenomena↗
PubMed1996

An inactivating inward-rectifying K current present in prolactin cells from the pituitary of lactating rats.

Primary cultures containing a high percentage of lactotrophs were obtained by dissociating the pituitary of rats following 14-18 days of lactation. Lactotrophs with a distinctive appearance were recorded after 1-35 days in vitro and identified by immunocytochemical staining for prolactin. Whole-cell voltage clamp measurements in isotonic KCl solution from a holding potential of -40 mV revealed the presence of inward-rectifying K currents with a time-dependent, Na(+)-independent inactivation at potentials negative to -60 mV. The time for complete inactivation was strikingly different between lactotrophs, varying between 1 sec and more than 5 sec at -120 mV, and was not related to time in culture. The reversal potential shifted 59 mV (25 degree C) for a tenfold change in external K+ concentration, demonstrating the selectivity of the channel for K+ over Na+. The inward-rectifying K current was blocked by 5 mM Ba2+ and partially blocked by 10 mM TEA. Chloramine-T (1 and 2 mM) produced a total block of the inward-rectifying K current in lactotrophs. Thyrotropin-releasing hormone (500 nM) significantly reduced the inward-rectifying K current in about half of the lactotrophs. This current is similar to the inward-rectifying K current previously characterized in clonal somatomammotrophic pituitary cells (GH3B6). The variability of the rate of inactivation of this current in lactotrophs and its responsiveness to TRH is discussed.

Animals↗
PubMed1991

High-performance liquid chromatographic determination of glyphosate and (aminomethyl)phosphonic acid in human serum after conversion into p-toluenesulphonyl derivatives.

We have developed a simple, highly sensitive and fast assay method for determining glyphosate and its major metabolite, (aminomethyl)phosphonic acid (AMPA), in serum by high-performance liquid chromatography with ultraviolet detection. Both compounds were successfully extracted with an anion-exchange resin column and allowed to react with p-toluenesulphonyl chloride. The detection limits were 0.3 microgram/ml for glyphosate and 0.2 microgram/ml for AMPA. Recoveries of glyphosate and AMPA spiked to serum were ca. 75% and ca. 88%, respectively. We are convinced that this procedure, in practice, allows medical examiners to analyse both compounds in the serum of poisoned patients within a short time.

Chromatography, High Pressure Liquid↗
PubMed1999

Redox agents regulate ion channel activity in vacuoles from higher plant cells.

The ability of redox agents to modulate certain characteristics of voltage- and calcium-activated channels has been recently investigated in a variety of animal cells. We report here the first evidence that redox agents regulate the activation of ion channels in the tonoplast of higher plants. Using the patch-clamp technique, we have demonstrated that, in tonoplasts from the leaves of the marine seagrass Posidonia oceanica and the root of the sugar beet, a variety of sulphydryl reducing agents, added at the cytoplasmic side of the vacuole, reversibly favoured the activation of the voltage-dependent slow vacuolar (SV) channel. Antioxidants, like dithiothreitol (DTT) and the reduced form of glutathione, gave a reversible increase of the voltage-activated current and faster kinetics of channel activation. Other reducing agents, such as ascorbic acid, also increased the SV currents, although to a lesser extent in comparison with DTT and glutathione, while the oxidising agent chloramine-T irreversibly abolished the activity of the channel. Single channel experiments demonstrated that DTT reversibly increased the open probability of the channel, leaving the conductance unaltered. The regulation of channel activation by glutathione may correlate ion transport with other crucial mechanisms that in plants control turgor regulation, response to oxidative stresses, detoxification and resistance to heavy metals.

Ascorbic Acid↗
PubMed1979

Discriminant--analytical investigation on the structural dependence of hyperglycemic and hypoglycemic activity in a series of substituted o-toluenesulfonylthioureas and o-toluenesulfonylureas.

The influence of a series of substituted o-toluenesulfonylthioureas and o-toluenesulfonylureas on the level of blood sugar was investigated in rats. According to the observed response the compounds were divided into three classes corresponding to hypoglycemic, hyperglycemic, and no activity. The distribution of the compounds over these classes can be described by discriminant functions using substituent constants, RM values, and indicator variables. Most important for the separation of classes are hydrophobic and/or steric properties as well as the presence or absence of the thiomide group. The results indicate that two different mechanisms of action with opposite effect overlap in the case of the series studied.

Animals↗