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Biomedical subjects

M Font

Publications and source records attributed to M Font.

At least 37 records · Page 2Linked to original sources
PubMed1993

Pharmacological characterization of the vasodilator effect of DF-100, a new pyridazino[4,5-b]indole, in vascular smooth muscle.

DF-100, i.e., 1-hydrazino-4-(3,5-dimethyl-1-pyrazolyl)-5H-pyridazino[4,5-b ]indole is a new pyridazino[4,5-b]indole derivative related to dihydralazine. The inhibitory effects of DF-100 were investigated on the contractions in isolated aorta and portal vein. In rat aorta, DF-100 inhibited both K(+)-induced as well as norepinephrine-induced contractions. DF-100 also caused dose-dependent relaxation of contractions produced by 80 mM K+. Moreover, DF-100 significantly inhibited the CaCl2 dose response in high-K+ depolarizing medium. DF-100 inhibited the phasic contractile response to norepinephrine and the caffeine-induced response, suggesting that this molecule affects the mobilization of Ca2+ from a membrane-bound pool. In rat portal vein, DF-100 inhibited the spontaneous rhythmic contractions. The results obtained in this study in isolated rat aorta and portal vein suggest that DF-100 has a direct vasodilating effect that could be attributed to inhibition of cellular Ca2+ influx and release from intracellular stores.

Animals↗
PubMed1993

Comparative analysis of Brucella serotype A and M and Yersinia enterocolitica O:9 polysaccharides for serological diagnosis of brucellosis in cattle, sheep, and goats.

Hapten polysaccharides of Brucella smooth M and A serotypes were prepared from Brucella sp. and Yersinia enterocolitica O:9 by previously described hydrolytic (O chain) or nonhydrolytic (native hapten [NH]) procedures. The purified polysaccharides differed only in the presence (O chain) or absence (NH) of lipopolysaccharide core sugars. The polysaccharides were compared by reverse radial immunodiffusion for the diagnosis of brucellosis in cattle (Brucella abortus biotype 1 [A serotype] and Brucella melitensis biotype 3 [AM serotype]), sheep (B. melitensis biotypes 1 [M serotype] and 3), and goats (B. melitensis biotype 1). The reverse radial immunodiffusion test with the NH from B. melitensis 16 M (serotype M) showed the highest sensitivity (89.6 to 97.3%), regardless of the host species and the serotype of the infecting Brucella sp. Y. enterocolitica O:9 NH (A serotype) was useful for diagnosing disease in cattle infected with B. abortus biotype 1, but not in cattle infected with B. melitensis biotype 3, sheep, or goats. The different results obtained with the serotype M and A polysaccharides and the sera from animals infected with M, A, and AM serotypes of Brucella spp. showed that in naturally infected animals, a large proportion of the antibodies are directed to or react with a previously defined common epitope(s) (J. T. Douglas and D. A. Palmer, J. Clin. Microbiol. 26:1353-1356, 1988) different from the A or M epitopes. By using the radial immunodiffusion test with B. melitensis 16M NH, it was possible to differentiate infected from vaccinated cattle, sheep, and goats with a sensitivity and specificity similar to that of the complement fixation test.

Animals↗
PubMed1993

New pyridazino[4,5-b]indole derivatives with inodilator and antiaggregatory activities.

Some 4-(3,5-dimethylpyrazol) 5H-pyridazino [4,5-b]indoles (7), 1,2,4-triazolo [4,3-b]pyridazino [4,5-b]indoles (9) and 1,2,4-tetrazolo [4,5-b]pyridazino [4,5-b] indoles (11) substituted in position 1 by amino groups have been synthesized and tested as inotropic agents and inhibitors of platelet aggregation. 6-Imidazolyl-11H-1,2,4-triazolo [4,3-b]pyridazino [4,5-b]indole (9) shows an activity superior to that of amrinone, with a notable selectivity towards phosphodiesterase (PDE) IV and PDEV, vasodilator activity and a good effect on blood platelet aggregation.

Animals↗
PubMed1993

Anthelmintic activity of pyrazinothiadiazine dioxide derivatives.

In a search for new anthelmintic compounds, some pyrazinothiadiazine dioxide derivatives were synthesized. Their anthelmintic activity was tested against larva and preadult stages of Trichinella spiralis. The mode of action and acute toxicity of these compounds were investigated. Structure-activity relationships are discussed.

Animals↗
PubMed1992

Antihypertensive and vasodilator effect of A-80b, a new pyridazino indole derivative.

The hypotensive and antihypertensive activities of a A-80b, a newly synthesized pyridazino[4,5-b]indole derivate were investigated in anaesthetized rats. In vitro studies were also done to examine the possible mechanism of its vasodilator action. A 80b (3-15 mg/kg i.p.) showed potent and long-lasting antihypertensive activity in spontaneous hypertensive rats. In normotensive rats, A-80b (7.5-30 mg/kg i.p.) also lowered blood pressure but less than in hypertensive rats. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. Contractile responses induced in isolated rat thoracic aorta by K+ and noradrenaline were inhibited by A-80b. In K(+)-depolarized rat aorta, A-80b showed dose-dependent inhibition of the Ca(2+)-induced contraction. Also, A-80b inhibited spontaneous contractions of rat portal vein. The vasodilator action seemed to be endothelium-independent. These results suggest that A-80b is a new chemical entity which exerts a hypotensive and antihypertensive effect, possibly attributable to vasodilator activity via interference with Ca2+ influx and probably Ca2+ mobilization from intracellular stores.

Animals↗
PubMed1992

New indole and triazino[5,4-b]indol-4-one derivatives: synthesis and studies as inotropics and inhibitors of blood platelet aggregation.

New triazino[5,4-b]indol-4-one derivatives carrying amino groups in position 3 were synthetized and tested as inotropic agents and inhibitors of platelet aggregation. 2h, 2p, 5p, and 6g are the most active as inotropic agents. Compounds were tested as inhibitors of platelet aggregation induced by adenosine 5'-diphosphate (ADP) and arachidonic acid (AA) (guinea pig whole blood). 2k, 2p, 5o, 6d, 6m, and 6o are the most active as inhibitors of the platelet aggregation induced by AA. 6d, 6h, and 6o are most active compounds also in the aggregation induced by ADP. Radioimmunoassay studies, following AA induced aggregation, measuring thromboxane B2 (TXB2) and prostaglandin E2 (PGE2) were carried out on compounds 2b, 2d, 2f, 2g, 2h, 2i, 2k, 2m, 2o, 2p, 2r, 5i, 5j, 5k, 5r, and 5f, which inhibit platelet aggregation induced by AA. None of the compounds tested turned out to be selective inhibitors. Compounds 2h and 2p showed both inotropic and platelet aggregation inhibiting activity.

Animals↗
PubMed1991

[Improving drug prescription in primary care: a controlled and randomized study of an educational method].

BACKGROUND: The aim of the present study was to assess whether educational intervention on the primary care physician may be an effective method to improve drug prescription. METHODS: An experimental randomized controlled study was carried out in 244 physicians of the management area No. 5 of the Institut Català de la Salut. Intervention consisted in 3 individualized interviews with the 123 physicians of the study group (IG), during which written informative material was also presented. The issues were: cerebral and peripheral vasodilators (CPVD) and antibiotics. The changes in the prescription of CPVD, combination of anti-infective agents with expectorants, mucolytics and/or balsamics (R05C1) and cephalosporins were specially evaluated in both groups. Subsequently, a stratified analysis was carried out depending on the volume of prescription of the physicians. RESULTS: The IG showed a greater reduction in the prescription of CPVD (9.78 bottles per physicians and months versus 6.43, p less than 0.01). The relative reduction in R05C1 prescription was also higher in the IG (12.3% versus 6.7%, p less than 0.01). The expenditure showed similar results. The use of oral cephalosporins increased in the IG and was reduced in the CG (p less than 0.01). CONCLUSIONS: The results show a favorable impact of personalized information in the groups with high prescription volume, which is particularly remarkable in the highest prescribers.

Drug Prescriptions↗
PubMed1991

New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.

Some fused 5H-pyridazino[4,5-b]indoles (7-10), substituted in positions 1 and 4 by hydrazine and/or amino groups, have been synthesized. These new compounds present a planar topography, a dipole with an adjacent acidic proton, and a basic hydrogen-acceptor site opposite the dipole. These compounds have some resemblance to carbazeram and other pyridazino agents with cardiotonic activity. Some of the new compounds here described possess inotropic activity (Table I and II), with a complementary effect as inhibitors of platelet aggregation (Table III and IV). 1-Hydrazino-4-(3,5-dimethyl)-1-pyrazolyl-5H-pyridazino[4,5-b ]indole hydrochloride (7a.HCl) is the first compound described in the literature with activities as inhibitor of PDE-IV and as selective inhibitor of TXA2 synthetase (Table V).

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1989

[Ki-1 non-Hodgkin's lymphoma. A multihospital study of 21 cases].

The Ki-1 monoclonal antibody recognizes a specific membrane antigen of activated lymphoid cells and stains large-cell non Hodgkin's lymphomas and Hodgkin's disease. Thus, it is widely used in the diagnosis of anaplastic lymphomas. Morphologically, the Ki-1 monoclonal non Hodgkin's lymphoma are diffuse of multifocal either classical or cell anaplastic type. The clinical behaviour is similar to the rest of the high grade lymphomas, disseminated at diagnosis but may reach remission after aggressive chemotherapy. The immunophenotype showed T, B or null nature of the latter. The clinical and pathological results of our study carried out in a group of 21 cases ki-1 positive lymphomas is herewith reported.

Adolescent↗
PubMed1989

[A quantitative study of the consumption of antihypertensives in Management Area 5 of the ICS (Costa de Ponent). Institut Català de la Salut].

The use of antihypertensive drugs (AHD) in the area n degrees 5 of the Institut Català de la Salut was evaluated for the period October 1986-December 1987. The unit of measure was the DDD (daily defined dose) per 1,000 population individuals per day. The overall use of AHD in 1987 was 49.31 DDDs/1,000 individuals/day; it was distributed among diuretics (53.5% of all AHD), beta-blockers (11.3%), and other AHD (35.2%). The most commonly prescribed drugs, by decreasing frequency order, were combinations of low ceiling diuretics with potassium sparing drugs, and of rauwolfia alkaloids with diuretics, followed by nifedipine, chlortalidone and furosemide. The interannual evaluation disclosed an increase of 18.6% in 1987 as compared with the preceding year, mostly at the expense of beta-blockers. On the other hand, there was a tendency to refrain from the use of fixed dose drug associations. This is a criterion of better use of antihypertensive therapy.

Adrenergic beta-Antagonists↗
PubMed1987

Selective thromboxane synthetase inhibitors and antihypertensive agents. New derivatives of 4-hydrazino-5H-pyridazino[4,5-b]indole, 4-hydrazinopyridazino[4,5-a]indole, and related compounds.

A series of new derivatives of 4-hydrazino-5H-pyridazino[4,5-b]indole (5) and 4-hydrazinopyridazino[4,5-a]indole (12) have been synthesized to investigate their activities as selective thromboxane synthetase inhibitors as well as antihypertensive agents. Several of the prepared compounds were found to be selective thromboxane synthetase inhibitors, in concordance with the Gorman model. The most potent were 8-(benzyloxy)-3,4-dihydro-4-oxo-5H-pyridazino[4,5-b]indole (3c) and 8-methoxy-4-hydrazino-5H-pyridazino[4,5-b]indole (5). This last compound did not inhibit prostacyclin formation and showed an antihypertensive activity similar to that of hydralazine. The acute toxicity in mice for 5a . HCl is about 2.2 times less than that for hydralazine.

Animals↗
PubMed1986

Effects of 2-indolecarbohydrazides on thromboxane synthetase activity and on in vitro and ex vivo blood platelet aggregation. New selective inhibitors.

Platelet antiaggregatory action of 42 synthetic 2-indolecarbohydrazides was studied observing their actions on arachidonic acid (AA) and adenosine-5-diphosphate (ADP) induced platelet aggregation. Radioimmunoassay studies, following AA induced aggregation, measuring thromboxane B2 (TXB2) and prostaglandin E2 (PGE2) were carried out on those compounds whose previous activities included inhibition of AA induced platelet aggregation and inhibition of the second wave of aggregation using ADP as the aggregating agent. Those compounds which demonstrated inhibition of TXB2 with increased PGE2 were subsequently tested with PGH2 as the aggregating agent. Results of this work demonstrate that 3 of the 42 compounds have specific inhibitory activity for thromboxane synthetase. The most active compounds were 1-methyl-5-hydroxyindole derivatives.

Arachidonic Acid↗
PubMedDate not supplied

[Exactness of the birth registry of Barcelona regarding birth weight and weeks of gestation].

OBJECTIVE: The aim of the study is to know the accuracy of the variables birth weight and gestational age in the Barcelona Birth Registry. Hospital medical records are used as gold standard. METHODS: A representative sample (n = 1,932) was selected from all the residents born in the city of Barcelona between 1st of May and 31st of December of 1996. The variables birth weight and gestational age were evaluated. Exhaustivity, sensitivity, specificity and predictive value for these variables were calculated. RESULTS: The Registry shows a high exhaustivity for the study variables. The lowest value of sensitivity corresponds to premature births (65.1%) and the lowest value of specificity to term births (63.9%). The predictive value positive was 77.5% for preterm births and 76.7% for term births. CONCLUSIONS: In general, exhaustivity and accuracy of the Barcelona Birth Registry are high, but sensitivity for preterm births in the Registry is lower. However, the corresponding maternal and child health indicators do not vary in an important manner.

Birth Certificates↗
PubMedDate not supplied

[Striatal dopamine transporter density decrease in first episode schizophrenic patients treated with risperidone].

UNLABELLED: Extrapyramidal symptoms and Parkinsonism (PS) are side effects commonly observed with antipsychotic treatment. However, about 24% of never-treated schizophrenic patients may suffer from PS, which contrast with that 1% observed from the general population. 123I-FP-CIT SPECT has probe useful to differentiate degenerative from non-degenerative PS, so it could be interesting using it for establishing the functional state of presynaptic dopamine neurons of these patients. AIM: To determine the dopamine transporter binding (DAT) in a homogeneous group of first-episode schizophrenic patients. METHODS: An open, transversal study. Thirty schizophrenic in-patients and 15 healthy subjects were recruited. Patients were treated with similar doses of risperidone and all subjects were scanned with 123I-FP-CIT. Extrapyramidal symptoms and psychopathological status was assessed by Simpson-Angus, CGI and PANSS. Semi-quantitative analyses of SPECT images were performed using ROIs placed in caudate nucleus, anterior, medium and posterior putamen and occipital cortex. RESULTS: Whole striatum 123I-FP-CIT binding ratio was significantly lower in patients than healthy subjects (t = 2.56, p < 0.014). This was observed in whole putamen (t = 2.66, p < 0.011), anterior (t = 2.35, p < 0.023), medium (t = 2.38, p < 0.022) and posterior putamen (t = 2.09, p < 0.042). No differences were observed in caudate nucleus (t = 1.81, p = 0.076). Females obtained higher binding ratios than males (t = -3.13, p < 0.003). No correlation was observed between 123I-FP-CIT binding ratios and clinical scales. CONCLUSION: In our series, first episode schizophrenic patients treated with risperidone have a decrease striatal DAT binding assessed with 123I-FP-CIT SPECT. This alteration could be related to their own schizophrenia disease or be secondary to the antipsychotic treatment.

Adult↗
PubMedDate not supplied

[Functional neuroimaging of auditory hallucinations in schizophrenia].

The neurobiological bases underlying the generation of auditory hallucinations, a distressing and paradigmatic symptom of schizophrenia, are still unknown in spite of in-depth phenomenological descriptions. This work aims to make a critical review of the latest published literature in recent years, focusing on functional neuroimaging studies (PET, SPECT, fMRI) of auditory hallucinations. Thus, the studies are classified according to whether they are sensory activation, trait and state. The two main hypotheses proposed to explain the phenomenon, external speech vs. subvocal or inner speech, are also explained. Finally, the latest unitary theory as well as the limitations the studies published are commented on. The need to continue investigating in this field, that is still underdeveloped, is posed in order to understand better the etiopathogenesis of auditory hallucinations in schizophrenia.

Brain↗
PubMedDate not supplied

[Intrinsic PEEP as a ventilation complication after pneumonectomy].

We report the case of a female patient who developed a clinical picture characterized by hemodynamic deterioration, bradycardia and asystole due to pulmonary hyperinsufflation (documented by X-ray examination) during the immediate postoperative phase of a right pneumonectomy. Occlusion of the respiratory limb of the respirator was followed by a positive pressure at the end of the respiration (PEEP) suggesting the presence of an intrinsic PEEP independent of the respirator. Application of a PEEP to the respirator induced a radiologic improvement. The mechanisms by which an intrinsic PEEP may develop are discussed.

Adenocarcinoma↗
PubMedDate not supplied

Action of metadoxine on isolated human and rat alcohol and aldehyde dehydrogenases. Effect on enzymes in chronic ethanol-fed rats.

Metadoxine (pyridoxine-pyrrolidone carboxylate) has been reported to accelerate ethanol metabolism. In the present work we have investigated the effect of metadoxine on the activities of isolated alcohol and aldehyde dehydrogenases from rat and man, and on the activity of these enzymes in chronic ethanol-fed rats. Our results indicate that in vitro metadoxine does not activate any of the enzymatic forms of alcohol dehydrogenase (classes I and II) or aldehyde dehydrogenase (low-Km and high-Km, cytosolic and mitochondrial). At concentrations higher than 0.1 mM, metadoxine inhibits rat class II alcohol dehydrogenase, although this would probably not affect the physiological ethanol metabolism. Chronic ethanol intake for 5 weeks results in a 25% decrease of rat hepatic alcohol dehydrogenase (class I) activity as compared with the pair-fed controls. The simultaneous treatment with metadoxine prevents activity loss, suggesting that the positive effect of metadoxine on ethanol metabolism can be explained by the maintenance of normal levels of alcohol dehydrogenase during chronic ethanol intake. No specific effect of chronic exposure to ethanol or to metadoxine was detected on rat aldehyde dehydrogenase activity.

Alcohol Dehydrogenase↗