[SENSITIVITY CHANGES OF THE ISOLATED GUINEA PIG INTESTINE BY PREMEDICATION, ANESTHESIA AND SPASMOLYTICS].
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For certain metal arc-welding and other metal processing operations, compounds of barium are used as flux components. Airborne fumes generated by welding with electrodes using barium fluoride or carbonate fluxes may contain 15-30% of barium in readily water-soluble form (Dare et al. 1984). Urine of welders inhaling such fumes was shown to contain elevated levels of barium ions (up to 234 micrograms/l). To assess the possible hazards of such exposure, the toxic potencies of fume samples, expressed in terms of their water-soluble barium ion contents, were compared with effects of solutions of barium salts in anaesthetised guinea-pigs. Dose-effect relationships were established and it was verified that acute toxic effects of inhaled aerosols or of intravenous bolus administration correlated with the barium contents of various forms of welding fumes. Bronchopulmonary reactivity to the barium was observed as marked increases in resistance to ventilatory air-flow, indicating bronchoconstriction. Simultaneously, marked pressor effects on blood pressure occurred. ECG abnormalities indicated myocardial hyperexcitability. Effects were modified by nifedipine and propranolol pretreatments.
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This paper reports the synthesis of 2- and 4- [benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and the evaluation of their inhibitory properties against histamine (H1), acetylcholine and barium chloride, on guinea pig isolated ileum. 4-[p.Methoxybenzyl-(2-dimethylaminoethyl)amino]-2-methoxy-pyrimidine (VIII) is shown to possess H1 receptor antagonist activity, with a potency similar to that observed for Tonzylamine. By contrast, a specific, although weak, antimuscarinic effect is displayed by 4-[benzyl-(2-dimethylaminoethyl)amino]-2-methoxy-5-methylthio-pyrimidine (XII).
Carbon dioxide absorbents, such as soda lime and Baralyme brand absorbent, convert sevoflurane to CF2 = C(CF3)OCH2F, a vinyl ether called "Compound A," whose toxicity raises concerns regarding the safety of sevoflurane in rebreathing circuits. Because an increased inflow rate to an anesthetic circuit decreases rebreathing, we assumed that an increased rate would proportionately decrease the concentration of Compound A. In the present report, we measured the Compound A concentration resulting from the action of wet (standard) soda lime and wet (standard) Baralyme on 2% sevoflurane in a model anesthetic circuit, using inflow rates (0.5, 1.0, 2.0, 4.0, and 6.0 L/min), ventilations (5 and 10 L/min), and carbon dioxide production/removal (200 and 400 mL/min) found in clinical practice. An increase in inflow rate decreased Compound A concentration to lower levels as inflow rate approached minute ventilation. At lower inflow rates, increasing duration of sevoflurane inflow increased the concentration of Compound A, a finding consistent with a progressive increase in absorbent temperature from absorption of carbon dioxide and consequently greater sevoflurane degradation. There was no material difference between Baralyme and soda lime in the concentrations of Compound A produced at a particular inflow rate. An increase in ventilation increased the concentration of Compound A, having a much greater effect at high rather than low inflow rates. An increase in amount of carbon dioxide absorbed also increased the concentration of Compound A. We conclude that inflow rate, ventilation, and carbon dioxide production are major determinants of the concentration of Compound A.
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In this study, the synthesis of some new 5-acetyl-3,4-dihydro-6-methyl-4-(substituted phenyl)-2(1H)-pyrimidinones has been reported. The compounds were prepared by the Biginelli reaction of acetylacetone with aromatic aldehydes and urea. The structures of the compounds were characterized by UV, IR, 1H NMR, 13C NRM, mass spectra and elementary analysis. The calcium antagonistic activity of these compounds was tested in vitro on rat ileum precontracted with 4 x 10(-3) M barium chloride.
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