Measurement of gastric contraction activity in dogs by means of AC biosusceptometry

The mechanical nature of gastric contraction activity (GCA) plays an important role in gastrointestinal motility. The aim of this study was to detect GCA in anaesthetized dogs, using simultaneously the techniques of AC biosusceptometry (ACB) and manometry, analysing the characteristics of frequency and amplitude (motility index) of GCA, modified by drugs such as prostigmine and N-butyl-scopolamine. The ACB method is based on a differential transformer of magnetic flux and the magnetic tracer works as a changeable external nucleus. This magnetic tracer causes a modification in the magnetic flux, which is detected by the coils. The results obtained from the ACB showed a performance comparable to the manometry in measuring the modifications in the frequency and amplitude of the GCA. We concluded that this ACB technique, non-invasive and free of ionizing radiation, is an option for evaluating GCA and can be employed in future clinical studies.

The ACB technique: a biomagentic tool for monitoring gastrointestinal contraction directly from smooth muscle in dogs

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

CNS-selective noncompetitive cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline

LASSBio-767 [(-)-3-O-acetyl-spectaline] and LASSBio-822 [(-)-3-O-tert-Boc-spectaline] were recently described as cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline, obtained from the flowers of Senna spectabilis (Fabaccae). We investigated their mechanism of inhibition of acetylcholinesterase and their efficacy in reversing scopolamine-induced amnesia. Competition assays with the substrate acetylthiocholine showed a concentration-dependent reduction in rat brain cholinesterase V-max without changes in apparent K-m. The kinetic data for LASSBio-767 and LASSBio-822 were best fit by a model of simple linear noncompetitive inhibition with K-i of 6.1 mu M and 7.5 mu M, respectively. A dilution assay showed a fast and complete reversal of inhibition, independent of incubation time. Simulated docking of the compounds into the catalytic gorge of Torpedo acetylcholinesterase showed interactions with the peripheral anionic site, but not with the catalytic triad. Anti-amnestic effects in mice were assessed in a step-down passive avoidance test and in the Morris water maze 30 min after injection of scopolamine (1 mg/kg i.p.). Saline, LASSBio-767, or LASSBio-822 was administered 15 min before scopolamine. Both compounds reversed the scopolamine-induced reduction in step-down latency at 0.1 mg/kg i.p. LASSBio-767 reversed scopolamine-induced changes in water maze escape latency at 1 mg/kg i.p. or p.o., while its cholinergic side effects were absent or mild up to 30 mg/kg i.p. (LD50 above 100 mg/kg i.p.). Thus, the (-)-spectaline derivatives are potent cholinergic agents in vivo, with a unique profile combining noncompetitive cholinesterase inhibition and CNS selectivity, with few peripheral side effects. (C) 2007 Elsevier B.V. All rights reserved.

New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

Five new piperidine alkaloids were designed from natural (-)-3-O-acetyl-spectaline and (-)-spectaline that were obtained from the flowers of Senna spectabilis (sin. Cassia spectabilis, Leguminosae). Two semi-synthetic analogues (7 and 9) inhibited rat brain acetylcholinesterase, showing IC50 of 7.32 and 15.1 mu M, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1 mg/kg, ip) was fully efficacious in reverting scopolamine-induced amnesia in mice. The two active compounds (7 and 9) did not show overt toxic effects at the doses tested in vivo. (c) 2005 Elsevier Ltd. All rights reserved.

Análise das vantagens de duas técnicas anestésicas - Venosa e inalatória - Para colecistectomia por videolaparoscopia

Background and Objectives - It is essential to reduce health care costs without impairing the quality of care. Propofol is associated to faster recovery and it is known that post-anesthesia care unit (PACU) costs are high. The aim of this study was to evaluate the advantages of two anesthesia regimens - propofol continuous infusion or isoflurane - taking into account the cost of both techniques on PACU stay. Methods - Forty seven patients, physical status ASA I, II and III, undergoing laparoscopic cholecystectomy were divided into 2 groups according to the anesthetic agent: G1, conventional propofol continuous infusion (100-150 μg.kg-1.min-1) and G2, isoflurane. All patients were induced with sufentanil (1 μg.kg-1) and propofol (2 mg.kg-1) and were kept in a re-inhalation circuit (2 L.min-1 of fresh gas flow) with 50% N2O in O2, sufentanil (0.01 μg.kg-1.min-1) and atracurium (0.5 mg.kg-1), or pancuronium (0.1 mg.kg-1) for asthma patients. All patients received atropine and neostigmine at the end of the surgery. Prophylactic ondansetron, dipyrone and tenoxican were administered and, when necessary, tramadol and N-butylscopolamine. Costs of anesthetic drugs (COST), total PACU stay (t-PACU), and PACU stay after extubation (t-EXT) were computed for both groups. Results - Costs were significantly lower in the isoflurane group but t-PACU was 26 minutes longer and t-EXT G1

Farmacomagnetografia colônia: estudo in vitro da desintegração de comprimidos magnéticos revestidos

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Avaliação da atividade eletromecânica uterina em ratas por biosusceptometria AC e eletromiografia

Pós-graduação em Biologia Geral e Aplicada - IBB