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B Pavan

Publications and source records attributed to B Pavan.

24 records · Page 2Linked to original sources

Effect of different classes of antibiotics on amniotic prostaglandin E release.

Our purpose was to investigate the effects of different classes of antibiotics, namely beta-lactamines, aminoglicosides, tetracyclines, macrolides, on amniotic prostaglandin E release to clarify their role in the treatment of premature labor. The effects of these antibiotics were tested also in combination with ampicillin, whose antiprostaglandinergic action had been demonstrated previously. Ceftriaxone and gentamicin significantly and reversibly inhibit both basal and arachidonic acid- or oxytocin-stimulated prostaglandin E release from amnion, although to a different extent. On the contrary, tetracycline and erythromycin do not influence prostaglandin E output. The inhibitory effect of ampicillin is potentiated, in an additive manner, by ceftriaxone, reduced by gentamycin, and eliminated by tetracycline and erythromycin. The finding that diverse classes of antibiotics and their combinations affect amniotic prostaglandin E release should be taken into account in the management of premature labor.

Aminoglycosides↗

Thermodynamic in vitro studies as a method to investigate the pharmacodynamic behavior of adenosine A1 receptor ligands.

PURPOSE: A thermodynamic analysis of the binding to rat cortex adenosine A1 receptor of N6-substituted (full agonists) and N6-substituted-deoxyribose (partial agonists) adenosine derivatives was performed. The intrinsic activity of the compounds was evaluated by measurements of the inhibition of forskolin stimulated 3', 5'-cyclic adenosine monophosphate (c-AMP) levels in isolated epididymal rat adipocytes. METHODS: The thermodynamic parameters deltaG(o) (standard free energy), deltaH(o) (standard enthalpy), and deltaS(o) (standard entropy) of the binding equilibrium were determined by means of affinity measurements carried out at different temperatures (0, 10, 20, 25, 30 degrees C). Levels of c-AMP were evaluated performing competitive protein binding assays. RESULTS: The binding of the ligands increases with temperature enhancement and, as a consequence, is totally entropy driven. Standard entropy values correlate significantly with intrinsic activity ones. CONCLUSIONS: It is proposed the data obtained by these in vitro experiments can be used to investigate the in vivo pharmacodynamic of A, full and partial agonists.

Adenosine↗

Processing of adenosine receptor agonists in rat and human whole blood.

A stability study of adenosine receptor agonists in rat and human whole blood was performed. The compounds were incubated at 37 degrees in fresh blood, and aliquots of the incubation mixture were hemolyzed at regular time intervals and analyzed with HPLC. N6-cyclopentyladenosine (CPA) and N6-cyclobutyladenosine (CBA) were degraded, whereas N6-cyclohexyladenosine, N6-cycloheptyladenosine and N6-sulfophenyladenosine were not. 2-Chloroadenosine had a half-life very similar to that of CPA. However, the 2'-, 3'-, and 5'-deoxyribose derivatives of CPA remained intact. The nucleoside transport inhibitor nitrobenzylthioinosine attenuated CBA and CPA metabolism in rat blood as did the inhibitor of adenosine deaminase erythro-9-(2-hydroxy-3-nonyl)adenine, albeit at relatively high concentrations. Complete blockade of CBA and CPA degradation was achieved by a preincubation of rat and human blood with the adenosine kinase (AK) inhibitor 5'-amino-5'-deoxyadenosine. We conclude that the two adenosine analogues are metabolized by AK both in rat and in human whole blood.

Adenine↗

Inhibition of amniotic prostaglandin E release by ampicillin.

OBJECTIVE: The effect of antibiotics in the prevention of preterm labor needs to be further investigated. The aim of this study was to determine the effect of ampicillin on prostaglandin E release from amnion as a possible explanation for its ability to retard preterm labor. STUDY DESIGN: The effect of the beta-lactam antibiotic ampicillin on prostaglandin E release from human amnion was tested under basal and stimulated conditions. RESULTS: Ampicillin dose dependently inhibits basal prostaglandin E release from amnion in both static and dynamic conditions. In our experiments, 10(-7) mol/L ampicillin (a concentration able to significantly inhibit prostaglandin E output) leaves the microbiologic features of the medium substantially unmodified up to 5 hours of incubation. Moreover, the drug reversibly counteracts the prostaglandin E elevation induced by arachidonic acid or oxytocin. CONCLUSION: This finding (i.e., that ampicillin inhibits prostaglandin E release from amnion) may offer an explanation for a beneficial response to ampicillin therapy in the case of preterm labor even in the absence of bacterial infection.

Amnion↗

Adenosine analogs inhibit acetylcholine release and cyclic AMP synthesis in the guinea-pig superior cervical ganglion.

The ability of adenosine agonists to modulate the electrically evoked release of acetylcholine (ACh) from [3H]choline preloaded guinea-pig superior cervical ganglia (SCG) was investigated. The adenosine A1-receptor selective agonist N6-cyclohexyladenosine (CHA) and 2-chloroadenosine (2-CADO) inhibited the evoked transmitter release, the effect being reversed by the A1-receptor selective antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), and by sulmazole (SUL), which blocks both the A1-receptor and the adenylate cyclase inhibitory regulator Gi. In whole ganglia, CHA decreased both the basal and the forskolin (FSK)-stimulated cyclic AMP synthesis. The latter effect was again prevented by the A1 antagonist DPCPX. These results are compatible with the existence, in the guinea-pig SCG, of adenosine A1-receptors, part of which are located on the presynaptic nerve terminals mediating an inhibition of ACh release.

Acetylcholine↗

The use of immobilized enzyme reactors in continuous-flow analyzers for the determination of glucose, urea, and uric acid.

We describe the use of immobilized enzymes in assay methods for the determination of glucose with glucose oxidase, uric acid with uricase, and urea with urease in serum samples. The enzyme reactor tubes were adapted to continuous-flow analyzers (Technicon AA II, SMA 12/60, and SMAC) used in routine laboratory determinations, and results with their use were compared to those from assays involving soluble enzymes. We substituted the reactors for the free enzyme reagents in the respective channels of the SMA 12/60 and SMAC, without modifying the parameters of the remaining channels. We compared assay sensitivity, precision, and carryover for immobilized and conventional liquid enzymes. Immobilized enzyme reactors provide accurate, reliable, convenient, and economical alternatives to the use of free enzyme reagents in these systems.

Autoanalysis↗