Ketamine structure activity relationship for quinolones

ketamine structure activity relationship for quinolones

Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors .. Synthesis, Antimalarial Activity, and Structure–Activity Relationship of. Ketamine is an NMDA receptor antagonist with a potent anesthetic effect. metabolism of Ketamine can be decreased when combined with Levofloxacin. inducers, inhibitors and structure-activity relationships of human Cytochrome P Keywords: Anti-ischemic agents; Quinolone analog; Structure–activity relationship; MCAO; MI structure–activity relationship of CPFX and the mech- anism of the Charles River, USA) were anesthetized with ketamine. (10 mg/ kg) and.

It is questionable whether such experiments help in predicting the convulsant risk associated with FQ administration in the usual clinical situation, that is without concomitant use of NSAIDs.

ketamine structure activity relationship for quinolones

The answer is probably no, for at least two main reasons. One is that in vitro experiments do not take into account the CNS diffusion characteristics of FQs, which vary considerably between compounds. We have recently developed a modelling approach to characterize the proconvulsant effect of BPAA on norfloxacin based upon determination of drug concentrations in CSF, shown previously to be part of the biophase, at the onset of activity.

Materials and methods Animals This work was carried out in accordance with Principles of Laboratory Animal Care NIH Publicationrevisedand the study protocol was approved by the local ethics committee.

ketamine structure activity relationship for quinolones

Animals were placed in wire cages in a 12 h light—dark cycle for 5 days before the beginning of the experiment. A polyethylene cannula [0.

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Following surgery, the rats were kept under a heating lamp, and after the first signs of movement, the animals were placed into individual plastic cages. Food was withdrawn 12 h before the experiment, but the animals had free access to water until drug infusion. Drug administration The day after surgery, a BPAA suspension was given orally by gastric tube 1 h before the beginning of the FQ infusion.

A solution of sodium carboxymethyl cellulose 0. Enoxacin, fleroxacin and sparfloxacin were dissolved in a minimal volume of 1 M NaOH to which an equal volume of phosphate buffer pH 7. Drug administrations were conducted between 2: In any case, CSF and blood were collected within 3 min, as described previously. Plasma was transferred into two separate tubes.

Intravenous Anesthesia - Ketamine - Chemistry

The other fraction was ultrafiltered with a Centrifree system CF50A model; Amicon, Molshein, France for determination of unbound concentrations. The chromatographic system consisted of a Shimadzu LC-6A pump connected to a Waters plus autosampler and to a Waters fluorimetric detector. Excitation and emission wavelengths were, respectively, and nm for pefloxacin, and nm for fleroxacin, and and nm for enoxacin.

Intro to Bacteria & Antibiotics: Quinolones

Data were recorded and processed using a Waters integrator. Plasma samples were diluted appropriately by addition of 1. Plasma protein binding modelling. FQ unbound versus plasma total concentrations were linearly related and fitted according to the following equation.

Doulchard, France were used in this study. Animals were housed in the animal breeding facilities of our laboratory authorization no.

  • Structure-activity relationships for ketamine esters as short-acting anaesthetics.

The animals were housed in wire cages in a h light—h dark cycle for 1 week to allow them adjust to the new environment and to overcome possible stress incurred during transit. Colombe, France and water. One day before the experiment, rats had a cannula implanted in the left jugular vein under anesthesia with 60 mg of sodium pentotal Sanofi Laboratories per kg of body weight.

Structure-activity relationships for ketamine esters as short-acting anaesthetics.

After this surgery animals were housed individually in plastic cages and food was withdrawn 12 h before the experiment, but the animals had free access to water until drug infusion. Pefloxacin solution was adjusted to pH The actual concentration was then determined by high-performance liquid chromatography HPLC and was used for dose calculations.

Drug administration was conducted between 2: The day after surgery, the jugular vein cannula was connected to a motor-driven syringe pump model SEB; Vial Inc. Animals were kept under a heat lamp to maintain their body temperature. The infusion was stopped when the animals exhibited maximal seizures. Immediately thereafter, rats were anesthetized with an intramuscular injection of CSF and blood samples were collected in this order and within 3 to 5 min, as previously described 9.

Pipemidic acid was used as an internal standard IS for pefloxacin, fleroxacin, and norfloxacin assay, and pefloxacin was used for enoxacin analysis. No IS was used for sparfloxacin determinations.

CSF and ultrafiltrate samples were injected directly after dilution into a mixture of 0. Plasma samples were diluted by addition of a 1. The mobile phase consisted of 0. The chromatographic system consisted of a model L pump Merck and a model autosampler Waters connected to a model fluorimetric detector Waters.

Excitation and emission wavelengths were, respectively, and nm for pefloxacin and norfloxacin, and nm for fleroxacin, and and nm for enoxacin. A Waters model spectrophotometric detector was used for UV detection at nm of sparfloxacin. Chromatographic data were recorded and processed with a Waters model integrator.

The limits of quantification in plasma were 1. They were equal to 0. Synaptic plasma membranes were prepared from the brains of Sprague-Dawley rats as previously described 1 with minor modifications. Brain cortices were homogenized with a potter mixer Eurostar digital IKA; Labotechnik in 10 volumes of ice-cold 0.

The resultant crude membrane pellet was suspended in 50 volumes of 50 mM Tris hydrochloride buffer pH 7.