Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: T03G11 .9
 340,653 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

To test the effectiveness of local anesthetic aerosols in asthma, we compared the protection afforded by lidocaine and saline aerosols to bronchoconstriction provoked by inhalation of Ascaris antigen aerosols in five previously sensitized, anesthetized Basenji-Greyhound, crossbred dogs. Pulmonary resistance (RL) was determined by the method of Von Neergaard and Wirz, and blood lidocaine levels were determined by gas chromatography. Lidocaine, 4%, was administered as an aerosol for 10 minutes before challenge with Ascaris antigen and again during the 10-minute challenge with Ascaris antigen. Lidocaine aerosols frequently elicited a slight increase in RL before antigen challenge, whereas saline aerosols did not alter RL. Despite a large dose (approximately 10 mg/kg), which produced blood levels of 0.6 to 3.3 micrograms/ml, lidocaine afforded no protection against antigen challenge: RL increased from a control mean of 4.2 +/- 1.7 (SEM) cm H2O/liters/sec to 26.9 +/- 9.3 after challenge in lidocaine-treated dogs, and from 2.9 +/- 0.6 to 22.8 +/- 5.1 in saline-treated dogs. In contrast, lidocaine aerosols prevented the 7-fold increase in RL elicited by challenge with citric acid aerosols, demonstrating an adequate block of irritant reflexes. The failure of lidocaine aerosols to protect against antigen-induced bronchoconstriction indicates that the concentrations achieved in lung by this route are inadequate to relax smooth muscle directly.
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PMID:Lidocaine aerosols do not prevent allergic bronchoconstriction. 719 46

Procedures for determining a 7.5 S oxysterol-binding protein in the cytosol fraction of cultured mouse fibroblasts were developed. The methods involved precipitation of cytosolic proteins between 0.3 and 0.4 saturation with (NH4)2SO4, incubation of the proteins with 25-hydroxy[3H]cholesterol at 0 degrees C and analysis by velocity sedimentation of 7.5 S radioactivity or of specific binding using dextran-charcoal to adsorb free sterol. By these means it was shown that binding of the ligand to the protein in a citric acid-phosphate buffer was optimal at pH 5.5 and that the sedimentation rate of the complex was greater at pH 7.4 (7.5 S) than at pH 5.5 (6.9 S). The binding protein was essentially saturated at a diol concentration of about 20 X 10(-9) M. The apparent Kd of the sterol-protein complex was approximately 3.9 X 10(-9) M. Cholesterol did not bind to 25-hydroxycholesterol-binding sites on the 7.5 S protein, whereas several oxysterols that are potent suppressors of 3-hydroxy-3-methylglutaryl CoA reductase also inhibited the binding of 25-hydroxycholesterol. One of these sterols, 5 alpha-cholest-8(14)-en-3 beta-ol-15-one was shown to compete for sites occupied by 25-hydroxycholesterol.
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PMID:Assay of oxysterol-binding protein in a mouse fibroblast, cell-free system. Dissociation constant and other properties of the system. 730 51

A sensitive and reliable high-pressure liquid chromatography (HPLC) assay for miloxacin and its two principal metabolites, 5,8-dihydro-8-oxo-2H-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid (M-1) and 1,4-dihydro-1,6-dimethoxy-7-hydroxy-4-oxoquinoline-3-carboxylic acid (M-2), in human serum and urine was developed. A strong anion-exchange Zipax SAX column using a mobile phase of 0.01 M citric acid solution containing 0.03 M sodium nitrate with pH 5.0 was used to achieve separation of the three compounds. The retention times of miloxacin, M-1, and M-2 were 3.8, 9.3, and 5.9 min, respectively. Serum and urine concentrations of these compounds as low as 10 ng/ml were measured. When results from the HPLC assay were compared with those from the microbiological assay of serum and urine samples from human subjects receiving miloxacin orally, the correlation coefficients were 0.94 for the serum and 0.99 for the urine. The HPLC assay method presents an alternative to the microbiological assay and permits future pharmacokinetic investigations of miloxacin.
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PMID:Determination of miloxacin and metabolites in human serum and urine by high-pressure liquid chromatography. 741 51

Production of verotoxin 1 (VT1) by hemorrhagic Escherichia coli O157:H7 in food has received limited research attention. A study was therefore conducted to determine the effect of temperature and pH, as achieved using two different acidulants, on VT1 production in ground roasted beef slurry. Slurries (pH 5.9) containing 33% beef and 67% water were incubated at 21 degrees C or 37 degrees C. Transfers were made at 48-h intervals for up to 18 days to determine if repeated subculturing influenced VT1 production. Populations of E. coli O157:H7 ranged from 8.9 x 10(8) to 1.9 x 10(9) CFU/ml within 48 h of transfer, regardless of incubation temperature. Maximum VT1 concentrations ranged from 61 to 63 ng/ml and 63 to 85 ng/ml of slurries incubated at 21 degrees C and 37 degrees C, respectively. The amount produced within 48 h at 37 degrees C was 15-24% higher than the amount produced at 21 degrees C and did not change after ten successive 48-h transfers. Upon changing the incubation temperature of slurry cultures adapted to 21 degrees C to an incubation temperature of 37 degrees C, VT1 production increased within 48 h to the level of cultures which had been previously adapted to 37 degrees C. A shift in temperature from 37 degrees C to 21 degrees C resulted in an initial reduction of about 55% in the amount of VT1 produced within 48 h. For studies on the combined effect of incubation temperature, pH and acidulant, slurries were adjusted to pH 5.4 with acetic and citric acids. Growth and production of VT1 in slurry acidified with acetic acid was markedly reduced compared to that in the control slurry (pH 5.9). The amount of VT1 detected in slurries receiving the second and third 24-h transfer of culture incubated at 21 degrees C was essentially nil. Growth and VT1 production was reduced in slurry acidified with citric acid compared to that observed in the control slurry but not as drastically as that observed in slurry acidified with acetic acid. VT1 concentration in unacidified beef slurry (pH 5.9) and in beef slurry acidified at pH 5.4 with citric acid reached 21 and 16 ng/ml, respectively, within 24 h at 21 degrees C. Results emphasize the need for proper sanitation procedures in beef processing and preparation facilities to reduce the risk of cross contamination of roasted beef and subsequent growth of E. coli O157:H7 and VT1 production.
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PMID:Growth and verotoxin 1 production by Escherichia coli O157:H7 in ground roasted beef. 781 74

An LC method for the quantitation of carbenicillin in human serum has been developed and validated. After protein precipitation with acetonitrile and evaporation, the residue was taken up by citric acid at pH 1.9. Carbenicillin and the internal standard (I.S.), piperacillin, were extracted with ethyl acetate, evaporated to dryness and reconstituted with a buffer solution. The separation of carbenicillin,, the I.S., and matrix peaks was achieved on a Microsorb C18, 3 microns column with a mobile phase of acetonitrile-tetrabutylammonium-phosphate buffer (pH* 6.6). The detection was by UV at 208 nm. The run time was 8 min. The established linearity range was 0.25-20 microgram ml-1 (r2 > 0.99) with a limit of quantitation of 0.25 microgram ml-1. Interday precision (RSD) and bias over the entire range were 1.1-6.9% and -1.83 to +2.80%, respectively. The interday precision (RSD) and bias for the QC samples at 0.75, 3.0 and 12 micrograms ml-1 were 5.9-7.9% and -2.80 to +2.30%, respectively. Stabilities of on-system, bench top, freeze-thaw cycles and sample storage were established.
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PMID:Development and validation of an LC method for the quantitation of carbenicillin in human serum. 791 88

1. The antitussive effects of moguisteine have been compared with codeine in several experimental models of cough in guinea-pigs and dogs. 2. Moguisteine and codeine dose-dependently (respective ED50 values are given in parentheses) inhibited cough induced in guinea-pigs by 7.5% citric acid aerosol (25.2 and 29.2 mg kg-1, p.o.), by 30 microM capsaicin aerosol (19.3 and 15.2 mg kg-1, p.o.), by mechanical stimulation (22.9 and 26.4 mg kg-1, p.o.) and by tracheal electrical stimulation (12.5 and 13.9 mg kg-1, p.o.). 3. Moguisteine was effective against cough induced by tracheal electrical stimulation in dogs (ED50 17.2 mg kg-1, p.o.); codeine was not tested because of its emetic effect. 4. After repeated dosing (12-15 days), moguisteine did not induce tolerance in either guinea-pigs or dogs. 5. Moguisteine did not interact with opiate receptors, since it did not show affinity for [3H]-naloxone binding sites and furthermore naloxone (5 mg kg-1, s.c.) did not antagonize its antitussive effects. 6. Moguisteine had no antitussive effect after i.c.v. administration (20 micrograms), whilst codeine (2-10 micrograms) and dextromethorphan (2.5-20 micrograms) were highly effective. 7. Our findings demonstrate that moguisteine is a novel peripherally acting non-narcotic antitussive agent, the mode of action of which remains to be elucidated fully.
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PMID:Moguisteine: a novel peripheral non-narcotic antitussive drug. 792 5

21-Aminosteroids have been shown to attenuate neuronal damage and to improve neurological outcome after experimental ischemia. The aim of this study was to determine whether brain edema induced by a cryogenic injury can be influenced by the 21-aminosteroid U-74389F. A cortical freezing lesion was applied to the right parietal region of Sprague-Dawley rats under ketamine-xylazine anesthesia. Systemic blood pressure was monitored in the peritraumatic period. Four different doses of U-74389F (A-D) were studied for their effect on post-traumatic brain swelling and edema. Respective control groups received only the solvent, citric acid buffer. (A) 3 mg/kg b.w.i.p. (total dose) 30 min before, 1 and 12 h; post trauma (p.t.); (B) 9 mg/kg b.w.i.v. 30 min before, 1 and 12 h p.t.; (C) 25 mg/kg b.w.i.v. 30 min before, 1, 6, and 12 h p.t.; (D) 50 mg/kg b.w.i.v. 15 min before, 15 and 30 min as well as 1, 2, 6, and 12 h p.t. 24 h after trauma, brains were removed and hemispheric swelling and water content were determined from the difference between wet and dry weight. Application of the 21-aminosteroid U-74389F moderately reduced post-traumatic brain swelling in all treatment groups: (A) 5%, (B) 9%, (C) 12%, and (D) 14%. In parallel with this, the increase in water content of the traumatized hemisphere was marginally lowered by U-74389F in all groups; in (C) e.g. from 1.9 +/- 0.1% to 1.7 +/- 0.1%, p = 0.07. These two findings taken together indicate that the 21-aminosteroid U-74389F moderately reduces post-traumatic swelling and edema.
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PMID:21-Aminosteroid U-74389F reduces vasogenic brain edema. 797 35

This study evaluated the shear bond strengths of a phosphate ester bonding agent, Clearfil Photo Bond, using different phosphoric acid gels to etch dentin. The study also tested the shear bond strength of the Clearfil Liner Bond system. Sixty extracted human molars were ground to expose mid-coronal dentin and were randomly assigned to six treatment groups. The first group was left unetched as a control. In the next four groups, dentin was etched with phosphoric acid gels: K-etchant (40% with silica thickener); Uni-Etch (polymer-thickened 32%); All-Etch (10%, polymer thickener); or Ultra-Etch (10%, silica thickener). Specimens in the sixth group were etched with 10/20 Ca, a gel with 10% citric acid and 20% calcium chloride. All specimens were bonded with Clearfil Photo Bond and XRV Herculite resin composite. Specimens in the final group also received SA Primer and Protect Liner. After thermocycling, shear bond strengths were determined using an Instron universal testing machine. Mean shear bond strengths ranged from 1.3 MPa (control) to 15.9 MPa (Clearfil Liner Bond). The shear bond strengths of specimens that had been etched with phosphoric acid gels were in the range of 5-8 MPa, and were not significantly affected by either acid concentration or thickener type. SEM examination showed that phosphoric acid demineralized dentin to a depth of 5 microns, while 10/20 Ca demineralized dentin to a depth of only 1-1.5 microns.
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PMID:Adhesion of a total-etch phosphate ester bonding agent. 799 4

We examined the effects of the alpha 2-receptor agonist clonidine, administered orally and by inhalation, on citric acid- and capsaicin-induced reflexes in guinea pigs and healthy human subjects. In groups (n = 8-10) of conscious guinea pigs, oral clonidine (10 and 100 micrograms/kg) was without effects, whereas inhaled clonidine (10-1,000 microM) caused a concentration-dependent inhibition of citric acid-induced cough (coughs during 3 min: control, 6.5 +/- 0.9; 1,000 microM clonidine, 1.7 +/- 1.0; P < 0.05) and reflex bronchoconstriction (time to onset of bronchoconstriction: control, 191 +/- 24 s; 1,000 microM clonidine, 317 +/- 33 s; P < 0.05). The inhibitory effect of inhaled clonidine on both reflexes was completely reversed by pretreatment with yohimbine but not with prazosin. In 12 healthy human volunteers, oral clonidine (150 mg) caused a significant fall in supine and erect systolic blood pressure and a significant increase in drowsiness as measured on a visual analogue scale 1 and 2 h after administration. Despite these effects, oral clonidine had no effect on capsaicin-induced cough or reflex bronchoconstriction in humans. In contrast to the effects in guinea pigs, inhaled clonidine (281 microM) had no effect on capsaicin-induced cough or reflex bronchoconstriction in humans. These data suggest that peripheral alpha 2-receptors exert an inhibitory effect on sensory neurotransmission in the guinea pig but not in the healthy human airway, indicating an important difference between the two species.
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PMID:Effect of clonidine on induced cough and bronchoconstriction in guinea pigs and healthy humans. 800 49

The impact of two different modes of training on body fatness and skeletal muscle metabolism was investigated in young adults who were subjected to either a 20-week endurance-training (ET) program (eight men and nine women) or a 15-week high-intensity intermittent-training (HIIT) program (five men and five women). The mean estimated total energy cost of the ET program was 120.4 MJ, whereas the corresponding value for the HIIT program was 57.9 MJ. Despite its lower energy cost, the HIIT program induced a more pronounced reduction in subcutaneous adiposity compared with the ET program. When corrected for the energy cost of training, the decrease in the sum of six subcutaneous skinfolds induced by the HIIT program was ninefold greater than by the ET program. Muscle biopsies obtained in the vastus lateralis before and after training showed that both training programs increased similarly the level of the citric acid cycle enzymatic marker. On the other hand, the activity of muscle glycolytic enzymes was increased by the HIIT program, whereas a decrease was observed following the ET program. The enhancing effect of training on muscle 3-hydroxyacyl coenzyme A dehydrogenase (HADH) enzyme activity, a marker of the activity of beta-oxidation, was significantly greater after the HIIT program. In conclusion, these results reinforce the notion that for a given level of energy expenditure, vigorous exercise favors negative energy and lipid balance to a greater extent than exercise of low to moderate intensity. Moreover, the metabolic adaptations taking place in the skeletal muscle in response to the HIIT program appear to favor the process of lipid oxidation.
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PMID:Impact of exercise intensity on body fatness and skeletal muscle metabolism. 802 2


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