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Biomedical subjects

C Martini

Publications and source records attributed to C Martini.

At least 181 records · Page 10Linked to original sources

Endocrine pancreatic function in pheochromocytoma.

In six patients with pheochromocytoma oral glucose tolerance test (OGTT) and arginine test were carried out. Blood insulin and glucagon response were investigated. In subjects with adrenal tumor glycemic curve pattern was typical: a rapid and exaggerated increase of glycemia followed by an abrupt drop. Absolute insulinemic response to oral glucose was normal, but inappropriate to glycemic stimulus. Arginine infusion provoked a slightly above normal increase in blood glucose and a normal increase in blood glucagon. In three of the patients studied postoperatively, reduced glycemic response to glucose was observed, whereas there were no evident variations in blood insulin and glucagon response. These data suggest that in pheochromocytoma impaired glucose tolerance is partly due to the reduced insulin response to oral glucose load.

Adrenal Gland Neoplasms↗

Platelet peripheral benzodiazepine receptors are decreased in Parkinson's disease.

Peripheral benzodiazepine (BDZ) receptors are located in a variety of tissues, including platelets, in the nuclear and/or mitochondrial membranes. We studied the density of peripheral BDZ receptors in platelets of 10 de novo Parkinson's disease (PD) patients, 18 PD patients treated with a levodopa/carbidopa combination, and in 15 healthy subjects matched for sex and age. The binding assay was conducted using [3H]PK 11195, a specific ligand for peripheral BDZ receptors. A significant decrease in the density of [3H]PK 11195 binding sites has been observed in PD patients with respect to controls (p less than 0.01), but not between de novo and treated PD patients. No correlation has been found between the decrease in density of [3H]PK 11195 binding sites in platelets and either the duration or severity of PD. Peripheral BDZ receptors are implicated in the regulation of mitochondrial respiratory function. Thus, their decrease in PD might parallel the abnormalities in mitochondrial function recently found in this neurologic disease.

Aged↗

A clinical study on the use of codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine in cancer pain.

The authors report a prospective study on 944 cancer pain patients treated with one of the following opioids: codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine. Level of analgesia, duration of treatment, side effects, and drop out were evaluated for each drug. Twenty-four percent of the patients still benefitted from treatment at the fourth week of study, even if high drug dosages were not used. Pentazocine did not show an evident analgesic effect during the first 2 wk of treatment. The other opioids were found to be valid therapeutic instruments for chronic cancer pain control in a limited number of patients.

Adult↗

Renal handling of citrate in chronic renal insufficiency.

Citrate is a relevant component of the inhibitory potential of the urine environment. Its excretion and renal handling have been widely studied in subjects with normal renal function, but little is known about changes induced by chronic renal insufficiency. We have investigated renal handling of citrate in 50 patients with different degrees of renal insufficiency as compared to 30 healthy subjects with normal renal function. Among patients 34 were defined as having mild renal insufficiency based on a GFR of 80 through 40 ml/min/1.73 m2 BSA, while 16 had moderate-to-severe renal failure, defined by a GFR ranging from 40 to 20 ml/min/1.73 m2 BSA. Serum citrate increased in mild renal insufficiency, while it tended to be restored to normal values at more advanced renal failure. There was a stepwise decrease in the filtered load of citrate as GFR decreased, while its renal clearance was significantly reduced only at higher degrees of renal failure. This behavior was due to an increase in the fractional excretion of citrate which was inversely related to the decrease in GFR (p = 0.015). These data suggest that serum citrate levels and excretion are governed by renal mechanisms at mild degrees of renal insufficiency; in these conditions citrate is shown to behave conformly to other poorly reabsorbable anions such as sulfate. At more advanced renal failure the ensuing metabolic acidosis plays a crucial role as a regulatory factor of both serum concentration and renal handling of citrate, by increasing cellular uptake and metabolism as well as tubular reabsorption of this anion.(ABSTRACT TRUNCATED AT 250 WORDS)

Acid-Base Imbalance↗

Tricyclic heteroaromatic systems. Synthesis of 1,3 and 1,2 disubstituted [1]benzopyrano[4,3-b]pyrrol-4-ones and structure-activity relationships as benzodiazepine receptor ligands.

The synthesis of some 1,3- and 1,2- disubstituted [1]benzopyrano-pyrrol-4-ones is reported as well as their benzodiazepine receptor affinity, as measured by the ability to displace [3H]flunitrazepam from its specific central binding. The structure-activity relationships on the whole series of disubstituted [1]benzopyrano-pyrrol-4-ones show the importance of the presence of the 1-aryl substituent and the size limitation of the 3-substituent. The size of the latter seems also to be important for the "in vitro" efficacy.

Animals↗

[Giacomo Andrea Giacomini: a Padua clinician between metaphysics and science].

As Professor of Theoretical Medicine for Surgeons at Padua University between 1824 and 1849, Giacomini achieved a position of great academic professionalism and prestige, not only in Padua, but throughout Italy and Europe. His fundamental medical thesis became part of the established field of medical practice that existed into the first decades of the 19th century. This thesis, derived directly from a vitalistic concept of biological phenomena, was based on the existence of a 'life force' that is distinct from the forces of physical-chemistry, having its own specific laws, contrary to those of physical-chemistry. Using this concept Giacomini was able to distinguish two causes of death: mechanical illness and dynamic illness. The nosographic and therapeutic beliefs of Giacomini were based on his distinction between the 'mechanical' or 'dynamic' effects of drugs. Giacomini's medical philosophy is the result of an interweaving of scientific theories and metaphysical ideas. The merits and limits of this philosophy must be analysed in the light of modern epistemology to explain why Giacomini was unable to develop fully clinical anatomy.

Europe↗

Stress-related changes of benzodiazepine binding inhibitory activity (B.B.I.A.) in humans.

The presence of benzodiazepine binding inhibitory activity (B.B.I.A.) in sera from 44 psychiatric patients and from 14 healthy volunteers, prompted us to investigate whether or not this activity underwent changes in stressful situations. We measured the inhibitory units (IU) of deproteinized sera of 12 subjects, immediately before and 2 weeks after sitting for a difficult university exam. Our results showed significantly higher IU values (i.e., higher B.B.I.A. concentrations) in the samples taken just before the exam. This preliminary finding clearly suggests the involvement of B.B.I.A. in anxiety mechanisms.

Adult↗

Tricyclic heteroaromatic systems. [1]benzopyranopyrrol-4-ones and [1]benzopyrano-1,2,3-triazol-4-ones as benzodiazepine receptor ligands. Synthesis and structure-activity relationships.

The synthesis, ability to displace [3H]flunitrazepam binding from bovine brain membranes, and GABA ratio of some [1]benzopyranopyrroles 1a-i and [1]benzopyrano-1,2,3-triazoles 2a,b are reported. The GABA ratios of some previously synthesized pyrazoloquinolines A and [1]benzopyranopyrazoles C are also presented in order to draw some structure-activity relationships among our benzodiazepine receptor ligands. 1,3-Diarylpyrrole derivatives 1a-h show similar affinity and efficacy to that of diazepam, while the 1-aryltriazoles 2a,b have no receptor affinity. Comparison of the latter results with those on previously reported compounds suggests that there are several hydrophobic regions on the benzodiazepine recognition site whose occupation gives rise to different affinity and efficacy.

Animals↗

Specific inhibition of benzodiazepine receptor binding by some N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives.

Several N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives were synthesized and tested for their affinity for the benzodiazepine receptor in bovine cortical membranes. The 2-methyl derivatives showed a lower affinity than the unmethylated analogues, and the 1,2-dimethyl derivatives practically lacked any affinity for the benzodiazepine receptor. The importance of the indole N-H group is therefore evidenced for an optimal interaction of these ligands with receptor site.

Amino Acids↗

Tricyclic heteroaromatic systems: synthesis, [3H]flunitrazepam brain membrane binding inhibition, and structure-activity relationships of 2,3-dihydro-2-aryl-4-R-[1]benzopyrano[4,3-c]pyrazole-3-ones.

We report the synthesis and binding activity to the central benzodiazepine receptors of some 2,3-dihydro-2-aryl-4-R-[1]benzopyrano[4,3-c]pyrazole-3-ones, which are isosteres of the CGS series. Although the compounds of the CGS series are potent ligands of the benzodiazepine receptors, none of the isosteres tested showed any significant inhibiting potency. This may be due to the change in electronic properties brought about by the replacement of the NH of the CGS series with an oxygen atom.

Animals↗

Synthesis of 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines and studies of binding to specific peripheral benzodiazepine binding sites.

Some 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines were synthesized and tested for their ability to displace [3H]clonazepam or [3H]Ro 5-4864 from their specific binding on the central and peripheral benzodiazepine receptors. None of the tested compounds showed any activity as central binding inhibitors, while most of them were specific as peripheral binding inhibitors, although they were not very potent.

Animals↗

Binding of [3H] muscimol to the retina of rabbit and turtle.

1. We studied the binding of [3H]muscimol to membrane preparations of the retina of rabbit (Lepus cuniculus) and turtle (Pseudemys scripta elegans). 2. In both species, [3H]muscimol binding was maximal at 0 degrees C and decreased with increasing temperature, it was saturable, protein concentration dependent and specific. Muscimol, GABA and bicuculline were the most effective displacers, whereas baclofen and diaminobutyric acid were ineffective. 3. In the turtle retina, Scatchard analysis indicated the presence of a single site with a KD of 20.81 nM, and a Bmax of 3.620 pmol/mg prot. 4. In the rabbit, a single site could be identified in the nanomolar concentration range (KD of 12.8 nM, Bmax of 1.327). A study of the association rate of [3H]muscimol binding revealed a faster kinetics in turtle, as compared to rabbit.

Animals↗

Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives: stereoselective interactions.

Several optically active N-(indol-3-ylglyoxylyl)amino acid derivatives were synthesized and tested for [3H]flunitrazepam displacing activity in bovine brain membranes. IC50 values were measured and revealed that the D form of the amino acid moiety of the compounds was more potent than both the L form and racemic form, suggesting a key role of the amino acid stereochemistry on the affinity to the benzodiazepine receptors. GABA ratio and proconvulsant/convulsant data reported for the most active compounds reveal they behave as inverse agonists at the benzodiazepine receptor.

Amino Acids↗

Effect of animal and vegetable protein intake on oxalate excretion in idiopathic calcium stone disease.

Oxalate excretion was measured in healthy subjects and idiopathic calcium stone-formers on dietary regimens which differed in the type and amount of protein allowed; 24-h urine collections were obtained from 41 practising vegetarians and 40 normal persons on a free, mixed, "mediterranean" diet. Twenty idiopathic calcium stone-formers were also studied while on two low calcium, low oxalate diets which differed in that animal protein was high in one and restricted in the other. Vegetarians had higher urinary oxalate levels than controls and although the calcium levels were markedly lower, urinary saturation with calcium/oxalate was significantly higher. This mild hypercalciuria was interpreted as being secondary to both a higher intake and increased fractional intestinal absorption of oxalate. Changing calcium stone-formers from a high to a low animal protein intake produced a significant decrease in calcium excretion but there was no variation in urinary oxalate. As a result, the decrease in calcium oxalate saturation was only marginal and not significant. It was concluded that dietary animal protein has a minimal effect on oxalate excretion. Mild hyperoxaluria of idiopathic calcium stone disease is likely to be intestinal in origin. Calcium stone-formers should be advised to avoid an excess of animal protein but the risks of a vegetable-rich diet should also be borne in mind.

Adult↗