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[Effect of antimicrobial preparations on thermogenesis in yeast-like fungi and in staphylococcus].

The results of the investigation of the effect of various concentrations of levorin and decamethoxin on the curves of thermogenesis in cultures of Candida albicans 688 and Staph. aureus 209 are presented in the paper. It was found that the above drugs in the concentration ranges within 0.0001--1 gamma/ml had different inhibitory effect on thermoproduction in the microorganisms. In the presence of higher concentrations of the drugs, i.e. above 1 gamma/ml thermoproduction practically ceased. It is supposed that determination of the levels of thermoprocesses in the presence of antimicrobial drugs provided predistination of the state of the biochemical reactions in the microorganisms at various stages of their cultivation.

Anti-Bacterial Agents↗

Short communication on erythrocyte membrane stabilization by decamethonium and succinylcholine.

The effects of decamethonium and succinylcholine on hypotonic haemolysis of erythrocytes were studied. These drugs at concentrations of 5 x 10(-8) M to 10(-4) M caused a dose dependent inhibition of haemolysis of erythrocytes in 0.45 pc NaCl but lysis occurred when the drug concentrations were increased to 10(-3) M. These results indicate that decamethonium and succinylcholine may have a membrane stabilization-lysis effect on erythrocytes.

Decamethonium Compounds↗

[Action of decamethoxin on diphtherial exotoxin].

The results of the study of the detoxicating effect of decamethoxin on diphtheria toxin are presented. It was noted that decamethoxin in subbacteriostatic concentrations inhibited the process of the toxin production in Corynebacteria diphtheriae. The detoxicating effect of the drug was clearly evident when used in a concentration of 10gamma/ml at a 2-hour exposure. Decamethoxin in a dose of 0.1 gamma/ml neutralized the effect of the diphtheria toxin on contact for 24 hours.

Animals↗

Differential effects of "peripheral" site ligands on Torpedo and chicken acetylcholinesterase.

Comparison of the effect of three 'peripheral' site ligands, propidium, d-tubocurarine, and gallamine, on acetylcholinesterase (acetylcholine hydrolase; EC 3.1.1.7) of Torpedo and chicken shows that all three are substantially more effective inhibitors of the Torpedo enzyme than of the chicken enzyme. In contrast, edrophonium, which is directed to the "anionic" subsite of the active site, inhibits the chicken and Torpedo enzymes equally effectively. Two bisquaternary ligands, decamethonium and 1,5-bis(4-allydimethylammoniumphenyl)pentan-3-one dibromide, which are believed to bridge the anionic subsite of the active site and the "peripheral" anionic site, are much weaker inhibitors of the chicken enzyme than of Torpedo acetylcholinesterase, whereas the shorter bisquaternary ligand hexamethonium inhibits the two enzymes similarly. The concentration dependence of activity towards the natural substrate acetylcholine is almost identical for the two enzymes, whereas substrate inhibition of chicken acetylcholinesterase is somewhat weaker than that of the Torpedo enzyme. The experimental data can be rationalized on the basis of the three-dimensional structure of the Torpedo enzyme and alignment of the chicken and Torpedo sequences; it is suggested that the absence, in the chicken enzyme, of two aromatic residues, Tyr-70 and Trp-279, that contribute to the peripheral site of Torpedo acetylcholinesterase is responsible for the differential effects of peripheral site ligands on the two enzymes.

Acetylcholinesterase↗

[Microbiological characteristics and sensitivity to antibiotics of decamethoxin-resistant diphtheric bacilli].

Biological properties and sensitivity of 6 Corynebacteria strains to 9 antibiotics were studied in vitro. The rate of the development of resistance to neomycin, levomycetin, decamine and decamethoxin in the diphtheria causative agents was determined. Biological properties of the decamethoxin resistant variants of the diphtheria causative agents were investigated: 100 passages on media with increasing amounts of the drug. The rate of the development of resistance to decamethoxin was slower than that to neomycin, levomycetin and decamine. Changes in the biological properties and antibiotic sensitivity of the decamethoxin-adapted strains were revealed.

Anti-Bacterial Agents↗

[The effect of armin on neuromuscular transmission in the frog against a background of hexadecamethonium action].

Hexadecamethonium as well as its alkylating derivatives significantly decrease the effect of organophosphorous acetylcholinesterase inhibitor armine on the amplitude and duration of the EPPs. It seems possible that these substances prevent inhibition of acetylcholinesterase. This property of the substances seems to be due to a polymethelene chain with two nitrogens as the basic part of the molecule structure.

Alkylating Agents↗

In vivo reversal of depolarizing neuromuscular blockade.

The antagonism of depolarizing blockers, principally succinylcholine and decamethonium, by tetraethyl- and tetrabutylammonium ions in an in vivo neuromuscular preparation in anesthetized cats is described; possible mechanisms for these effects are discussed. Tetraethyl- (50-100 mg/kg, i.v.) and tetrabutylammonium (1-5 mg/kg, i.v.) produced sharp reversals of 95-99% succinylcholine and decamethonium blocks. These reversals were effective and sustained at any point during the course of the blockades. Tetraethyl- or tetrabutylammonium, administered 2-3 min before succinylcholine or decamethonium, prevented blockade, an effect compatible with an earlier reported in vitro investigation. The studies of others disclose the interaction of depolarizing blockers with acetylcholine receptors, leading to channel opening, channel entry and binding therein of these blockers. The present studies support this in showing the prevention of succinylcholine and decamethonium block by the prior administration of tetraethylammonium, which also interacts with acetylcholine receptors. It is proposed that a possible mechanism for tetraethylammonium reversals of succinylcholine and decamethonium blocks may be attributable to the tetraethylammonium reversal of a K+ current block by quaternary ammonium ions such as succinylcholine and decamethonium. Tetraethyl- and tetrabutylammonium ions proved to be effective antagonists of succinylcholine block following inactivation of plasma cholinesterases by hexafluorenium.

Action Potentials↗

Paralysis and long bone growth in the chick: growth shape trajectories of the pelvic limb.

Growth of chick embryonic femora, tibiotarsi and first phalanges of digit three were measured at one day intervals from day 6 through 16 of incubation. Normal controls were compared to embryos paralyzed at 5 days of incubation. Over the 10 day study period, length of the paralyzed femora, length and width of the paralyzed tibiotarsi and differences in length of the phalanges were observed. Growth in length of phalanx one of digit three was most affected by paralysis over this period. Changes in shape of these bones also occurred during growth. Normal long bones undergo changes in shape as differential growth in length and width occurs. Such changes in shape can be considered as the bone's normal growth "trajectory". Paralyzed bones displayed a different growth trajectory than normal bones. As expected, the long bones of paralyzed embryos were shorter than age-matched controls. Contrary to expectations, however, paralyzed long bones were relatively more stout than age-matched controls.

Animals↗

Muscle and tendon size relationships in a paralyzed chick embryo model of clubfoot.

Clubfoot is a birth defect that may be related to muscle weakness or imbalance. The purpose of this study was to examine the relationships among muscle and tendon size and embryonic motility in a paralyzed chick embryo model of clubfoot and arthrogryposis. Decamethonium bromide, a neuromuscular blocking agent, was administered to a series of embryos in five dosage groups, producing a cohort of embryos with various degrees of paralysis and atrophy of tendons and muscle. Embryonic movement frequency was monitored, and after death in late gestation, the cross-sectional areas of the calf musculature and the gastrocnemius tendon proximal to the ankle were measured histologically. Significant correlations were found between embryonic motility and both muscle (r2 = 0.52) and tendon (r2 = 0.77) areas. In addition, a significant correlation (r2 = 0.74) was found between muscle and tendon areas, suggesting that a measurement of one may be used to predict the other.

Animals↗

Inhibition of histamine-N-methyltransferase activity by neuromuscular blocking drugs.

On the basis of previous findings that histamine-N-methyltransferase (HMT) activity can be significantly enhanced or inhibited by a number of analogues of histamine and drugs containing dialkylaminoalkyl moieties, we investigated whether the neuromuscular blocking drugs alcuronium, d-tubocurarine, decamethonium, succinylcholine, gallamine and pancuronium each of which contain quaternary ammonium groups, influence the activity of HMT. Our findings showed that all six drugs significantly inhibited HMT activity in the concentration range 10(-7)-10(-3) M with alcuronium being the most potent inhibitor (I.D.50 = 2 X 10(-6) M). Activities at these concentrations reveals that alcuronium, pancuronium, d-tubocurarine and gallamine are more potent inhibitors than two of the most potent histamine analogue inhibitors, N tau-methylhistamine and 2-methylhistamine. Alcuronium proved to be of similar potency to the dimaprit analogue, SKF 91488 regarded as one of the most potent HMT inhibitors known. The structurally similar and chemically least complex straight chain neuromuscular blocking compounds, succinylcholine and decamethonium proved to be the least potent inhibitors.

Alcuronium↗