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Biomedical subjects

P Mazzone

Publications and source records attributed to P Mazzone.

14 recordsLinked to original sources

Correlation between monoamino oxidase inhibitor activity of some thiazol-2-ylhydrazines and their interaction with dipalmitoylphosphatidylcholine liposomes.

A calorimetric investigation has been carried out on the influence exerted by some 1-(alkoxybenzoyl)-2-(4-substituted thiazolyl-2-yl)hydrazines, possessing monoamine oxidase inhibitory (MAOI) activity, on the thermotropic behavior of model membranes constituted by dipalmitoylphosphatidylcholine (DPPC) vesicles. Attention was paid to evaluate how structural variations of drugs may influence drug-lipid interaction. The examined drugs were found to modify the gel to liquid-crystal phase transition of DPPC liposomes, by causing a shift of the transition temperature (Tm) toward lower values and a negligible variation in the enthalpy changes (delta H). The different effects on DPPC thermotropic behavior of these MAOI drugs could be considered in terms of different substituents on the molecule's backbone. The calorimetric results were related to drug's MAO inhibitory activity measured by fluorescence techniques and the apparent distribution coefficient of the compounds in water/n-octanol. A hypothesis on a correlation between a drug's structure, inhibitory activity, and membrane interaction has been suggested.

1,2-Dipalmitoylphosphatidylcholine

Monitoring of the discrimination threshold for interocclusal thicknesses in rehabilitated edentulous patients.

Thirty-seven white Caucasian subjects with unsatisfactory dentures were tested for interocclusal thickness discrimination threshold. New dentures were prepared and the test was repeated on days 1, 4 and 90 (from delivery). Eight patients whose situation was still unsatisfactory were given osseointegrated implant anchored dentures and the test repeated at the same intervals. Results were analysed statistically. Improved denture fit was found to increase interocclusal sensitivity. Decreased sensitivity during follow-up might indicate the need to check denture fit.

Aged

Cerebral blood flow and somatosensory evoked response changes induced by spinal cord stimulation: preliminary follow-up observations.

A group of 6 patients undergoing cervical spinal cord stimulation (SCS) because of different pathologies was studied. Multipolar leads (QUAD-Medtronic) were inserted percutaneously; following an SCS test period, leads were connected to a multiprogrammable, fully implantable generator (ITREL II). Neither surgical nor other side effects were found. Regional cerebral blood flow (rCBF) (xenon-133 inhalation) was determined in the basal condition and after 30 min of SCS. Somatosensory-evoked potential (SSERs) from the legs were recorded in basal conditions and after 45 min of SCS. In 2 patients SSERs could not be evaluated due to electrical noise from SCS. CBF increased mainly in anterior regions in 4/6 patients (P300 improved in 1 of them and in another case), and was unchanged in 2 patients. rCBF was retested after a mean of 9.5 months of continuous SCS with the same parameters. rCBF returned to basal values in the 4 patients showing an early flow increase; in contrast, rCBF increased in the other 2 cases without early flow changes. These preliminary data seem to support the view of an acute effect of SCS on rCBF as well as on SSER, at least in some patients. Differences in long-term rCBF modifications might depend on either the underlying pathology or on the different neuronal system involved by SCS.

Adolescent

MAOI activity of thiosemicarbazides and related 2-thiazolylhydrazines.

The preparation is described of hydrazides I, thiosemicarbazides II, III, IV and hydrazinothiazoles VIII, which can be considered as "precursors" or "open models" for the synthesized benzoyl-, benzilidene- and benzyl-hydrazinothiazoles V, VI and VII, analogous to 4-methyl and 4-phenyl substituted derivatives A, B and C, described and tested for their MAOI activity in a previous paper. Biochemical assay on the new prepared compounds allowed us to better clarify the structure-activity relationship also of compounds A, B and C of the precedent note. Moreover, on a group of derivatives, which showed a higher activity, a further test was performed to observe the possible correlation between MAOI activity and both their lipophilicity and ability in interacting with liposome bilayers, taken as a model of cell membrane.

Animals

Synthesis and local anesthetic activity of alkylaminoacyl derivatives of 2-amino-1,3,4-thiadiazole.

We prepared some series of 2-(alkylaminoacyl) derivatives of 2-amino-1,3,4-thiadiazoles. Most terms were subjected to a biological screening showing a local anesthetic activity both in infiltration and trunkular tests. For some of the assayed derivatives, the activity was comparable to that of lidocaine, taken as the reference molecule. From the obtained results an acceptable relationship between some structural features and activity was drawn.

Anesthetics, Local

MAOI activity of some novel series of substituted thiazol-2-yl-hydrazines.

Three series of 2-thiazolylhydrazines were synthetized and evaluated for their MAO inhibitory (MAOI) activity, both by in vivo tests, to assay their influence on several MAOI activity-related parameters (the variation on blood pressure induced by tyramine and clonidine and L-amfetamine-induced hypermotility) and in vitro tests, to assay their effect on rat brain mitochondria by a kinuramine fluorimetric assay. In vivo, all the tested compounds significatively influenced the evaluative parameters used. As regards in vitro test, all compounds displayed MAOI activity at a concentration of 1.10(-4) mol.l-1, which was significant in several cases. In the discussion of the results, the influence of the structure on the biological activity of the prepared compounds was delineated.

Amphetamine

Treatment of severe renovascular hypertension by percutaneous transluminal renal angioplasty in patients with solitary functioning kidney. Effects on blood pressure and renal function.

In this study the effects of percutaneous transluminal renal angioplasty on blood pressure and renal function were studied in 9 hypertensive patients with stenosis of the main artery of a solitary functioning kidney. The outcome of the percutaneous dilatation of the renal artery stenosis, and the effects on blood pressure and renal function were evaluated for a mean period of 16.4 +/- 2.13 (SE) months (ranging from 3 to 65 months). A successful dilatation of the renal artery stenosis was shown in all the patients by the aortography performed 1 h after the procedure. At the discharge (7.8 +/- 0.9 days after dilatation), blood pressure was 'cured' in 2 patients and 'improved' in the remaining patients; renal function was improved in all patients who had reduced renal function. At the last follow-up, no restenosis was found in patients who repeated the follow-up angiography; blood pressure was 'cured' in 3 patients and 'improved' in 6 patients, and renal function appeared steadly improved. In contrast with other reports, our results demonstrate that percutaneous renal angioplasty is a safe and effective procedure and should be attempted before considering surgical intervention in patients with artery stenosis of a solitary functioning kidney.

Adult