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At least 793 records · Page 44Linked to original sources
PubMed2000

Abolition of endothelium-dependent relaxation in the rat aorta by tetraoctylammonium ions.

Quaternary ammonium ions are common pharmacological probes used to study the kinetic properties of K+ channels in smooth muscle cells. On the other hand, some ammonium compounds cause vasorelaxation through unknown mechanisms. The main aim of this study was to examine a unique role of endothelium in the vascular response to tetraoctylammonium ions (TOA+) in the isolated rat aorta. Changes in contractile force were measured by force transducers and total tissue content of cGMP was measured by radioimmunoassay. Endothelial cytosolic Ca2+ ([Ca2+]i) was assessed by laser scanning confocal microscopy.

Acetylcholine↗
PubMedDate not supplied

[The antistaphylococcal activity of thionium in in vitro experiments].

The paper deals with the experimental study of antistaphylococcal properties of thionium--a derivative of bis-quarternary ammonium compounds. High bactericide activity of the preparation is revealed as a result; it is preserved under high contents of protein substances in the media. The sensitivity of staphylococcal strains to thionium is not affected by the initial sensitivity of microorganisms to antibiotics. The preparations interaction with benzylpenicillin and gentamycin has been studied. Synergist effect of sub-bacteriostatic doses of thionium with the mentioned antibiotics has been found. Effect of benzylpenicillin increases 4-32 times, that of gentamycin--64-512 times independent of the primary sensitivity to these antibiotics. The further study of a new antistaphylococcal preparation is advisable.

Anti-Bacterial Agents↗
PubMed1989

Variations in demethylation of N-methylnaltrexone in mice, rats, dogs, and humans.

1. Rats and mice have a greater capacity than dogs or humans to N-demethylate the quaternary ammonium compound, N-methylnaltrexone. 2. In dogs, following the i.v. administration of N-[14C-methyl]methylnaltrexone, 50% of the radioactivity was excreted in the urine and an additional 30% in the faeces within 120 h. 3. In humans following the i.v. administration of 14C-N-methylnaltrexone, 40-60% of the radioactivity was excreted in the urine within the first 24 h. The plasma radioactivity-time curves indicated a biphasic decay and a short distribution phase between 6 and 9 min. with a longer elimination phase between 238 and 1320 min.

Aged↗
PubMed1984

Some properties of the thiamine uptake system in isolated rat hepatocytes.

A kinetic study of [14C]thiamine uptake over a concentration range from 0.1 microM to 4 mM was performed in isolated rat hepatocytes. The results showed that two processes contribute to the entry in rat hepatocytes: a low affinity process with a Kt of 34.1 microM and Vmax of 20.8 pmol/10(5) cells per 30 s and a high affinity process with a Kt of 1.26 microM and Vmax of 1.21 pmol/10(5) cells per 30 s. The uptake of thiamine by the high affinity process was concentrative and reduced in a betaine medium or K+ medium. Both ouabain and 2,4-dinitrophenol decreased the thiamine uptake by the high affinity process. These findings indicate that the transport of thiamine via a high affinity process is dependent on Na+ and biological energy. The uptake of thiamine was strongly inhibited by thiamine analogs such as dimethialium and chloroethylthiamine. Among quarternary ammonium compounds other than thiamine derivatives, choline and acetylcholine significantly inhibited thiamine uptake by rat liver cells, whereas betaine and carnitine did not. A kinetic study of thiamine uptake by rat hepatocytes preloaded with pyrithiamine, a potent inhibitor of thiamine pyrophosphokinase, revealed that the biphasic property of thiamine uptake disappeared and a single carrier system for thiamine with a Kt of 40.5 microM, which was similar to the Kt value of the low affinity process, was retained. These results strongly suggest that thiamine transport system in rat liver cells is closely connected with thiamine pyrophosphokinase, which accelerates the uptake rat of thiamine by pyrophosphorylation at physiological concentrations of thiamine.

2,4-Dinitrophenol↗
PubMed1999

Canalicular membrane transport is primarily responsible for the difference in hepatobiliary excretion of triethylmethylammonium and tributylmethylammonium in rats.

Two structurally similar quaternary ammonium compounds, triethylmethylammonium (TEMA, M(r) 116) and tributylmethylammonium (TBuMA, M(r) 200) were used as model compounds to identify the unit process of hepatobiliary excretion that is responsible for markedly different biliary excretion of organic cations (OCs). Cumulative biliary excretion (in percentage of dose; i.v., 12 micromol/kg) was 0.17 for TEMA and 34.5 for TBuMA. In vivo uptake clearance into the liver was 0.686 +/- 0.020 ml/min for TEMA and 0.421 +/- 0.028 ml/min for TBuMA. When the uptake clearance was examined in an isolated hepatocyte system, comparable clearance between TEMA and TBuMA was obtained, consistent with the in vivo result. These observations suggest that uptake into the liver is not the major determinant for the difference in biliary excretion of the OCs. Coadministration of colchicine, an inhibitor of microtubule formation, had no effect on biliary excretion of the model compounds, and the primary site of subcellular distribution of the OCs appears to be the cytosol, suggesting that intracellular movement does not play a major role in the markedly different biliary excretion of the OCs. In contrast, in vivo excretion clearance across the canalicular membrane for TBuMA was 180-fold greater than that for TEMA, and in vitro efflux clearance of TBuMA was smaller than that of TEMA (p <.01), indicative of involvement of these processes in the markedly different biliary excretion of the OCs. Therefore, these data indicate that canalicular transport is primarily responsible for the markedly different biliary excretion of TEMA and TBuMA.

Algorithms↗
PubMed2005

The antibacterial action of cloths and sanitizers and the use of environmental alternatives in food industries.

The use of cleaning cloths in food industries has been implicated in the spread and growth of infective bacteria. Generic cloths sanitized with hot water at 75 degrees C and chemical sanitizers such as quaternary ammonium compounds (QAC) and hypochlorites currently used in food industries were compared with environmentally conscious alternatives such as fiber cloths sanitized with hot water at 75 degrees C. The results indicated that concentrations of Staphylococcus aureus and Escherichia coli on the fiber cloths were significantly lower than concentrations of bacteria on most of the generic cloths sanitized with hot water at 75 degrees C or a chemical sanitizer. Concentrations of bacteria on the fiber cloths sanitized with hot water at 75 degrees C also were lower than concentrations on cloths sanitized with chemical sanitizers. Concentrations of bacteria on the generic cloths, however, were significantly increased.

Anti-Bacterial Agents↗
PubMedDate not supplied

DNA binding properties of minor groove binders and their influence on the topoisomerase II cleavage reaction.

We present titrations of the human delta beta-globin gene region with DNA minor groove binders netropsin, bisnetropsin, distamycin, chromomycin and four bis-quaternary ammonium compounds in the presence of calf thymus topoisomerase II and DNase I. With increasing ligand concentration, stimulation and inhibition of enzyme activity were detected and quantitatively evaluated. Additionally we show a second type of stimulation, the appearance of strong new topoisomerase II cleavage sites at high ligand concentrations. The specific binding sites of the minor groove binders of the DNA sequence and their microscopic binding constants were determined from DNase I footprints. A binding mechanism for minor groove binders is proposed in order to explain these results especially when ligand concentration is increased.

Animals↗
PubMed1993

The permeability of the cGMP-activated channel to organic cations in retinal rods of the tiger salamander.

1. The permeability of the channel activated by guanosine 3',5'-cyclic monophosphate (cGMP) to many organic monovalent cations was determined by recording macroscopic currents in excised inside-out patches of plasma membrane from isolated retinal rod outer segments of the tiger salamander. 2. Current-voltage relations were measured when the NaCl of the bathing medium was replaced by salts of organic cations. Permeability ratios relative to Na+ ions were calculated with the Goldman-Hodgkin-Katz potential equation from the measured changes of reversal potentials. 3. Hydroxylammonium+, hydrazinium+ and methylammonium+, which are molecules of very similar shape and size, permeate the channel with very different permeability ratios: 5.92, 1.99 and 0.60 respectively. 4. Methylated and ethylated ammonium+ compounds were investigated. It was found that, not only methylammonium+, but also dimethylammonium+ and ethylammonium+ were permeant with permeability ratios of 0.6, 0.14 and 0.16 respectively. Trimethylammonium+, tetramethylammonium+, diethylammonium+, triethylammonium+, and tetraethylammonium+ were not permeant. 5. Guanidinium+ and its derivatives formamidinium+, aminoguanidinium+, acetamidinium+ and methylguanidinium+ were all permeant with permeability ratios 1.12, 1.00, 0.63, 0.36 and 0.33 respectively. 6. The cGMP-activated channel was found to be permeable to at least thirteen organic cations. Molecular models of the permeant cations indicate that the cross-section of the narrowest part of the pore must be at least as large as a rectangle of 0.38 x 0.5 nm dimensions.

Ambystoma↗
PubMed1983

Channel-blocking activity is a possible mechanism for a selective ganglionic blockade.

The actions of bis-ammonium compounds (BAC) on the ionic channels activated by acetylcholine (ACh) were studied in voltage-clamped neurones of rabbit isolated superior cervical ganglion. The kinetics of binding of BAC to open channels was estimated from shortening of the decay of fast excitatory postsynaptic current. The kinetics of dissociation of BAC from open channels was estimated from the kinetics of restoring of second response to double-pulse application of ACh in presence of BAC. The ganglion-blocking activities of BAC correlated with the rate constants of their binding to open channels. It was concluded that selective ganglion-blocking actions of BAC were determined by their channel-blocking activities.

Acetylcholine↗
PubMed1998

Characterization of In40 of Enterobacter aerogenes BM2688, a class 1 integron with two new gene cassettes, cmlA2 and qacF.

Enterobacter aerogenes BM2688, which is resistant to multiple antibiotics, and its aminoglycoside-susceptible derivative BM2688-1 were isolated from the same clinical sample. Strain BM2688 harbored plasmid pIP833, which carries a class 1 integron, In40, containing (in addition to qacEDelta1 and sul1, which are characteristic of class 1 integrons) four gene cassettes: aac(6')-Ib, qacF, cmlA2, and oxa-9. The cmlA2 gene had 83.7% identity with the previously described nonenzymatic chloramphenicol resistance cmlA1 gene. The qacF gene conferred resistance to quaternary ammonium compounds and displayed a high degree of similarity with qacE (67.8% identity) which, however, has been found as part of a cassette with a very different 59-base element. The oxa-9 gene was not expressed due to a lack of promoter sequences. Study of the antibiotic-susceptible derivative BM2688-1 indicated that a 3,148-bp deletion between the 3' end of the aac(6')-Ib gene and the 3' conserved segment of In40 was responsible for the loss of resistance. The occurrence of this DNA rearrangement, which did not involve homologous sequences, suggests that the In40 integrase could promote recombination at secondary sites.

Amino Acid Sequence↗
PubMed1991

Delayed-rectifier potassium channel activity in isolated membrane patches of guinea pig ventricular myocytes.

When the patch-clamp technique was used, a slowly activating, time-dependent outward current was identified in both cell-attached and excised membrane patches obtained from guinea pig ventricular myocytes. This macroscopic patch current was present in approximately 50% of patches studied and could be observed both in the presence and absence of unitary single channel activity (i.e., ATP-sensitive K+ channels). The time course of activation of the patch current resembled that of the whole cell delayed-rectifier K+ current (IK) recorded under similar ionic conditions, and the patch current and IK were activated over a similar membrane potential range. The time-dependent patch current could be eliminated when the Nernst potential for K+ equaled that of the pulse voltage. The patch current was inhibited by external addition of the tertiary ammonium compound LY 97241 (50 microM) and was augmented after internal application of the catalytic subunit of adenosine 3',5'-cyclic monophosphate-dependent protein kinase (500 nM). Deactivating tail currents with kinetics similar to those of IK could be recorded to cell-attached and excised patches. Unitary single channel events underlying the time-dependent patch current could not be resolved despite various attempts to increase single channel conductance. Thus our results suggest that a major component of delayed rectification in guinea pig ventricular cells is due to the activity of a high-density, extremely low conductance K+ channel.

Adenosine Triphosphate↗
PubMed1991

Pharmacological studies on otilonium bromide.

Otilonium bromide (OB) is a quaternary ammonium compound characterized by a long aliphatic chain. Its chemical properties are responsible for both a poor penetration in CNS and a prolonged binding to cell membranes. OB is a spasmolytic agent which acts by modifying Ca++ fluxes from extra and intracellular sites. It has been documented that iv administration (10 mg/kg) of OB causes a marked reduction of colonic motility lasting from 2 to 3 hours, whereas an inhibition of upper GI motor activity is present only at higher dosages. In conclusion, OB seems to exert its activity mainly on distal GI tract, and its spasmolytic effect may be due to its ability to inhibit Ca++ fluxes and to a direct action of the drug on the contractile proteins of the smooth muscle.

Animals↗
PubMed1977

Determination of oxyphenonium bromide in plasma and urine by means of ion-pair extraction, derivatization and gas chromatography-electron-capture detection.

A sensitive and selective method for the determination of the quaternary ammonium compound oxyphenonium bromide (Antrenyl), a drug with strong anticholinergic properties, in human plasma and urine is described. The method is based on ion-pair extraction of the cation with perchlorate, a re-extraction according to ion-pair principles with tetrapentylammonium as the counter ion, hydrolysis to cyclohexylphenylglycolic acid, derivatization of this acid to its pentafluorobenzyl ester and determination of the ester by gas chromatography and electron-capture detection. Quantitation is possible down to 2 ng/ml of oxyphenonium bromide using 1 ml of plasma and down to 200 ng/ml using 0.1 ml of urine. The method described can also be applied to other anticholinergic drugs with an ester function.

Animals↗
PubMed2004

The efficacy of cleaning products on food industry surfaces.

The increased incidence of foodborne illness and the growing use of chemical sanitizers in the food industry led the authors to an investigation of alternative, chemical-free methods of sanitizing surfaces using fiber cloths with hot water. The sanitizing performance of kitchen fiber cloths and all-purpose fiber cloths sanitized with hot water at 167 degrees F (75 degrees C) was compared with that of generic cloths such as antibacterial cloths and cleaning cloths sanitized with hot water at 167 degrees F (75 degrees C) or chemical sanitizers--quaternary ammonium compound (QAC) and hypochlorite. The QAC sanitizer resulted in the lowest overall concentrations of Staphylococcus aureus and Escherichia coli. The sanitizing performance of the kitchen fiber cloths was similar to that of the antibacterial cloths (S. aureus: p = .144; E. coli: p = .120) and cleaning cloths (S. aureus: p = .297; E. coli: p = .062) sanitized with QAC. Use of the fiber cloths resulted in lower concentrations of bacteria on stainless-steel kitchen surfaces, compared with the use of the generic cloths sanitized with hot water at 167 degrees F (75 degrees C). Concentrations of bacteria on the surfaces after use of the all-purpose fiber cloths were similar to concentrations of bacteria after use of the generic cloths sanitized with hypochlorite.

Disinfection↗
PubMedDate not supplied

A statewide characterization of hospital infection control practices and practitioners.

Selected features of infection control programs among the 163 general hospitals in Tennessee were surveyed in 1976 and 1979. Each hospital but one had a designated infection control practitioner. Three-fourths of the hospitals had fewer than 200 beds and most were in rural areas. The practitioners in these small hospitals worked in an isolated professional milieu: few (4%) had attended a basic training course or were members of a national (11%) or local (16%) infection control association. They also had significantly less access to standard infection control resource publications than did practitioners in large hospitals. Use of aqueous quaternary ammonium compounds for disinfection was reported by 37% of all hospitals in 1979; 68% of hospitals routinely performed bacteriologic cultures of personnel or the environment. In contrast, only 3% of hospitals did not have a policy specifying the use of sterile closed-system drainage of indwelling bladder catheters. Although these practices varied somewhat by hospital size, the differences were not statistically significant. Modest improvement in each parameter was noted since 1976. Pathology was the most common medical specialty (34%) among chairman of infection control committees; internal medicine and pediatrics accounted for only 13%. The practice of routine microbiologic monitoring was significantly more common among hospitals with chairmen who were pathologists. The implications of these findings for national priorities in hospital infection control are discussed.

Bacteria↗
PubMed2004

Unique inner pore properties of BK channels revealed by quaternary ammonium block.

Potassium channels have a very wide distribution of single-channel conductance, with BK type Ca(2+)-activated K(+) channels having by far the largest. Even though crystallographic views of K(+) channel pores have become available, the structural basis underlying BK channels' large conductance has not been completely understood. In this study we use intracellularly applied quaternary ammonium compounds to probe the pore of BK channels. We show that molecules as large as decyltriethylammonium (C(10)) and tetrabutylammonium (TBA) have much faster block and unblock rates in BK channels when compared with any other tested K(+) channel types. Additionally, our results suggest that at repolarization large QA molecules may be trapped inside blocked BK channels without slowing the overall process of deactivation. Based on these findings we propose that BK channels may differ from other K(+) channels in its geometrical design at the inner mouth, with an enlarged cavity and inner pore providing less spatially restricted access to the cytoplasmic solution. These features could potentially contribute to the large conductance of BK channels.

Animals↗
PubMed1992

Prejunctional muscarine receptors in the rabbit ear artery differ from M1, M2 and M3 muscarine receptors.

The ability of several selective muscarine receptor antagonists to inhibit the effect of carbachol on prejunctional muscarine receptors on sympathetic nerve endings in the rabbit isolated ear artery was investigated to characterise the receptor subtype involved. Carbachol did not reduce responses to exogenous noradrenaline and the inhibitory effect of carbachol on responses to nerve stimulation was unaffected by hexamethonium (10 microM) indicating that the effect of the muscarine agonist was exerted prejunctionally and was not modulated by nicotine receptor stimulation. The dissociation constants or apparent dissociation constants obtained using (+/-)-benzhexol (pKB; 6.63), (R)-benzhexol methiodide (8.11), dicyclomine (5.86), (+/-)-telenzepine (7.34), AF-DX 116 (6.95), himbacine (7.60), (+/-)-hexahydrosiladiphenidol (5.39) and a bisquaternary ammonium compound, heptane-1,7-bis(dimethyl-3'-phthalimidopropyl ammonium bromide) (5.84), indicate that the muscarine receptor subtype involved is not of the M1, M2 or M3 subtype.

Animals↗
PubMed1989

Antimicrobial activity of environmental surface disinfectants in the absence and presence of bioburden.

Thirty-nine products representing six categories of disinfectants (alcohols, chlorines, dilute glutaraldehydes, iodophors, phenolics, and quaternary ammonium compounds) were first tested in the absence of bioburden, using four test methods with five test organisms. Products that performed best were retested with the same methods and organisms in the presence of both serum and whole blood, using 3- and 10-minute contact times. Only products containing high ethyl alcohol had consistently high antimicrobial activity regardless of the test method, test organism, or contact time used both in the absence and presence of bioburden. Although these specific formulations demonstrated ability to penetrate and inactivate high concentrations of microorganisms within heavy bioburden, optimum disinfection of environmental surfaces is highly formulation dependent. Other products tested showed deficiencies that contraindicate their use as environmental surface disinfectants in clinical dental settings.

Alcohols↗