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Biomedical subjects

E Mussini

Publications and source records attributed to E Mussini.

At least 55 records · Page 3Linked to original sources
PubMed1980

The role of respiration in vinyl chloride monomer excretion in rats.

1, 5 and 10 mg/kg vinyl chloride monomer (VCM) in aqueous solution were injected i.v. into male rats with cannulated tracheas. Respiratory activity was regulated to permit investigation of the effect of modifying pulmonary ventilation on VCM excretion in blood and expired air assayed at different intervals for VCM. VCM excretion rate was found to be directly proportionate to pulmonary ventilation. When respiration was stopped for 1 min after VCM injection, there was no decrease in blood BCM, the main route of elimination of i.v. injected VCM thus being pulmonary.

Animals↗
PubMed1980

Effects of chronic treatment with di-(2-ethylhexyl) phthalate on rat liver microsomal activities.

The effects of chronic di-(2-ethylhexyl)phthalate (DEHP) on liver microsomal activity were studied in rats. Daily doses of 50 and 500 mg/kg for 4 weeks did not affect O-demethylation, aromatic hydroxylation, N-demethylation, C3-hydroxylation, styrene monooxygenase, glutamic-oxalacetic and glutamic-pyruvic transaminases (GOT, GPT). Inhibition of glutathione-S-transferase A and C and induction of epoxide hydrase, glutathione-S-transferase B and nitroreductase activity were instead observed. Protein, cytochrome P-450 and reduced glutathione levels in liver did not appear to be affected by DEHP pretreatment.

Animals↗
PubMed1980

Blood levels of ditazole and inhibition of platelet aggregation in man.

5 healthy volunteers (3 males, 2 females, aged 22-35 years) were given 600 mg ditazole (Ageroplas) every 12 h (9.00 a.m. and 9.00 p.m.) for 10 days. Venous blood was collected from all volunteers at 9.00 and 11.00 a.m. on days 0, 3, 5, 7 and 10. The threshold concentrations of adrenaline inducing two distinct waves of platelet aggregation (Born's method) within 3 min were determined each time. Blood levels of ditazole were measured by a gas-chromatographic technique using a nitrogen-phosphorus selective detector. The average blood levels of the drug ranged between 0.84 and 1.30 microgram/ml at 9.00 a.m., and between 1.93 and 2.85 microgram/ml at 11.00 a.m. Inhibition of platelet aggregation (expressed by a grading system in arbitrary units) ranged between 1.6 and 2.0 at 9.00 a.m. and between 2.0 and 2.4 at 11.00 a.m. The fluctuations of blood levels and platelet aggregation inhibitory activity of ditazole observed during the study period were virtually the same. It is suggested that the treatment schedule used in the present study results in blood levels of ditazole sufficient to reveal any consistent alteration of platelet function in normal subjects.

Adult↗
PubMed1979

Esterase activity of rat muscle.

The esterasic capacity of a series of skeletal muscles in response to three hemisuccinate ester drugs was investigated in rats and compared to that on alpha-naphthylacetate as a reference esterase substrate. Marked variations between different muscles and between given muscles of animals of different sex were observed, indicative of a complex heterogeneity in muscular expression of esterase activity.

Animals↗
PubMed1979

Isolation and structure determination of enzymatically formed styrene oxide glutathione conjugates.

When styrene oxide was incubated with glutathione in the presence of rat liver cytosolic fraction, two conjugates were formed. Structural investigation by mass spectrometry (MS), proton magnetic resonance (PMR) analysis and chemical fragmentation showed the presence of two positional isomers, namely S-(1-phenyl-2-hydroxyethyl)glutathione and S-(2-phenyl-2-hydroxyethyl)glutathione in a ratio of approx. 60 : 40.

Animals↗
PubMed1979

Head-space gas-chromatographic analysis of vinyl chloride monomer in rat blood and tissues.

1. A method for measuring vinyl chloride monomer (VCM) concn. in rat blood and tissues is described, using a head-space g.l.c. technique with flame ionization detector. The method is sensitive to 5 ng/ml VCM in blood and 30 ng/g in tissues. 2. VCM disposition was determined in rat blood, liver, kidney, brain and lung at different intervals after administration of 1--10 mg VCM/kg i.v. and 10 mg/kg orally. 3. VCM distributed rapidly in the organism after i.v. administration; it was eliminated rapidly and was no longer detectable at 15 min for the highest dose and at 4 min for the lowest. VCM was absorbed rapidly when given orally and tissue concn. were measurable for longer than after i.v. treatment. For both routes, VCM concn. in liver and lung decrease faster than in other organs, suggesting that these organs play a role in VCM elimination.

Animals↗
PubMed1978

Pharmacokinetic studies on ditazole, a novel inhibitor of platelet aggregation.

The distribution of ditazole in blood and tissues of rats was determined by a simple GLC technique. Ditazole, after intravenous injection in rats (20 mg/kg), entered preferentially into the brain, the liver, and the heart in decreasing order. In the epididymal adipose tissue, the drug was present only in small amounts. Ditazole disappeared from the rat organs 4 hr after the treatment. The apparent ditazole half-life in rat blood was 41 min, the volume of distribution was 2.068 liters/kg, and the body clearance was 0.0345 liter/kg/min.

Animals↗
PubMed1978

Distribution of camazepam in rats and mice.

Camazepam, 5 mg/kg iv, was injected in rats and mice to study its distribution in the blood and brain. Peak blood levels were about 0.9 microgram/ml in rats and 0.6 microgram/ml in mice. Peak brain levels were about 1.5 microgram/g in rats and 0.8 microgram/g in mice. The apparent blood half-life of camazepam was 9 min in mice and 20 min in rats.

Animals↗
PubMed1977

Hydroxylation of three benzodiazepines in vitro.

Three structurally related benzodiazepines were studied as substrates for hydroxylation by liver microsomal enzymes of rats and mice. The Vmax was comparable for dechlorodesmethyldiazepam, desmethyldiazepam, and 2'-chlorodesmethyldiazepam in the two animal species. The apparent Km decreased from dechlorodesmethyldiazepam to 2'-chlorodesmethyldiazepam for liver microsomal enzymes from both animal species. The hydroxylation of desmethyldiazepam and 2'-chlorodesmethyldiazepam yielded two pharmacologically active metabolites, oxazepam and lorazepam, respectively.

Animals↗
PubMed1976

A specific gas chromatographic method for the determination of microsomal styrene monooxygenase and styrene epoxide hydratase activities.

A gas chromatographic (GC) method for the determination of the metabolite resulting from the activities of microsomal styrene monooxygenase (epoxide synthetase) and epoxide hydratase using styrene or styrene epoxide as substrates has been developed. The determination of the activities of both enzymes is based on the GC determination of phenylethylene glycol after its esterification with n-butylboronic acid. Kinetic parameters for both enzymes are given.

Animals↗
PubMed1976

Microsomal styrene mono-oxygenase and styrene epoxide hydrase activities in rats.

1. Styrene epoxide formation and styrene epoxide hydration have been studied in liver, lung, kidney, heart, spleen and brain of female and male rats. 2. Styrene epoxide formation is NADPH-dependent although it is enhanced when NADH is added together with NADP. This enzymic activity is inhibited by metyrapone and SKF 525-A but not by the effective inhibitors of epoxide hydrase, 1,2-epoxy-3,3,3-trichloropropene and cyclohexene oxide. 3. Known inducers of liver microsomal mono-oxygenases show a different activity on the two enzymes. Phenobarbital increases both formation and hydration of styrene epoxide; and carbamazepine increase the hydration but not the formation of styrene epoxide; a steroid contraceptive combination (lynestrenol+ mestranol) increases styrene epoxide formation while it inhibits epoxide hydrase; 3-methylcholanthrene does not affect either of the activities.

Animals↗
PubMed1976

Activity of liver microsomal mono-oxygenases on some epoxide-forming cyclic tricyclic drugs. I. Kinetics in vitro.

1. The mono-oxygenase activity that forms epoxides has been studied in rat liver microsomes using as substrates carbamazepine and cyclobenzaprine, tricyclic drugs which form stable epoxides in vivo and in vitro. 2. A simple gas chromatographic method has been used to determine the amount of epoxide formed and the linearity of the enzymic reaction with time and protein concentration has been demonstrated. 3. Pre-treatment with carbamazepine increases the rate of formation of carbamazepine epoxide in rat liver microsomal preparations. 4. The effect of SKF 525-A on the formation of these epoxides has been studied.

Animals↗
PubMed1975

Gas chromatographic-mass spectrometric determination of intact C3-hydroxylated benzodiazepine glucoronides in urine.

A method is described for the determination C3-hydroxylated benzodiazepine glucuronides in biological samples. Oxazepam and lorazepam glucuronides are measured as methyl esters and trimethylsilyl derivates by a gas chromatographic procedure. The applicability of the method has been tested on the urine of rats, guinea pigs, rabbits and man, receiving oxazepam orally. Oxazepam glucuronide was not found in rat urine but it was present in the urine of rabbits (5.7% of the administered dose), guinea pigs (9.5%) and man (13.4-26.9%).

Administration, Oral↗