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ARD-353 [4-((2R,5S)-4-(R)-(4-diethylcarbamoylphenyl)(3-hydroxyphenyl)methyl)-2,5-dimethylpiperazin-1-ylmethyl)benzoic acid], a novel nonpeptide delta receptor agonist, reduces myocardial infarct size without central effects.
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A novel delta-receptor selective compound, ARD-353 [4-((2R,5S)-4-(R)-(4-diethylcarbamoylphenyl)(3-hydroxyphenyl)methyl)-2, 5-dimethylpiperazin-1-ylmethyl)benzoic acid], was evaluated for activity on infarct size in a rat model of acute myocardial infarction. ARD-353 was characterized as having delta
Stability, bactericidal activity, vitamin B6 activity and gastrointestinal absorption of benzoic acid esters of pyridoxine.
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alpha 4-O-Benzoyl-pyridoxine (PN-4'MB) and alpha 5-O-benzoyl-pyridoxine (PN-5'MB) were hydrolyzed in 10% aqueous solution of acetone at pH 1-4. They were hydrolyzed obeying apparent first-order kinetics. In the pH range of 1-7, PN-4'MB was hydrolyzed 10 times faster than PN-5'-MB. At pH 7-12, an
Design, synthesis and computational evaluation of a novel intermediate salt of N-cyclohexyl-N-(cyclohexylcarbamoyl)-4-(trifluoromethyl) benzamide as potential potassium channel blocker in epileptic paroxysmal seizures.
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The narrow therapeutic range and limited pharmacokinetics of available Antiepileptic drugs (AEDs) have raised serious concerns in the proper management of epilepsy. To overcome this, the present study attempts to identify a candidate molecule targeting voltage gated potassium channels anticipated to
Comparative in vivo and in vitro studies with the potent GABAB receptor antagonist, CGP 56999A.
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CGP 56999A ([3-[1-(R)-[(3-cyclohexylmethyl)hydroxyphosphinyl]-2-(S)- hydroxy-propyl] amino]ethyl]-benzoic acid) is a potent GABAB receptor antagonist showing much more pronounced convulsant features in mice than do other previously studied GABAB receptor antagonists. The goal of this study was to
Preclinical and clinical studies on safety and tolerability of repaglinide.
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Repaglinide, an insulinotropic benzoic acid derivative, has been tested extensively in the preclinical and clinical setting for safety and tolerability. In preclinical safety trials, no clinically relevant laboratory or histopathological changes were found and repaglinide was not found to be
Effects of GABAB receptor antagonism on the development of pentylenetetrazol-induced kindling in mice.
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Pentylenetetrazol (PTZ) administered chronically in rodents induces kindling which is considered to be a model of chronic epilepsy mediated through a specific interaction with the GABA-gated chloride ionophore. PTZ kindling also impairs shuttle-box learning indicating a possible modulation of memory
[Convulsive properties of various organoselenium compounds].
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Three organo-selenium compounds have been synthetized : methyl seleno-2 benzoic acid, acetylseleno-2 benzoic acid and diselenosalicylic acid. These compounds induce convulsive seizures in the rat, the most active of them being methyl seleno 2 benzoic acid. Convulsions are stopped after anaesthesia
Fluorination of an antiepileptic drug: A self supporting transporter by oxygen enrichment mechanism.
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Drug therapy of seizures involves producing high levels of antiepileptic drugs in the blood. Drug must enter the brain by crossing from the blood into the brain tissue, called a transvascular route (TVR). Even before the drug can reach the brain tissue, factors such as systemic toxicity, macrophage
Product selection criteria for intravascular ionic contrast media.
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The chemistry, clinical use, pharmacokinetics, adverse reactions, dosages, and formulary recommendations for intravascular ionic contrast media routinely used in radiologic procedures are reviewed. The meglumine, sodium, or combined meglumine-sodium salts of triiodinated benzoic acid derivatives,
Synthesis of some new thioxoquinazolinone derivatives and a study on their anticonvulsant and antimicrobial activities.
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OBJECTIVE
A series of ten novel derivatives of 3-substituted-2-thioxoquinazolin-4(3H)-ones have been synthesized from anthranilic acid via Mannich reaction with various secondary amines in presence of formaldehyde in ice cold condition.
METHODS
The structure of these compounds have been elucidated
Probenecid pretreatment enhances anticonvulsant action of NBQX in mice.
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NBQX (2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline) was studied following intravenous administration to mice. Maximal electroshock seizures were suppressed by low doses of NBQX (ED50 = 13 mg/kg) but effects had dissipated by 10 min after a dose of 25 mg/kg. Coadministration of the transport
Prenyloxyphenylpropanoids as a novel class of anticonvulsive agents.
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In this study, we synthesized some natural and semi-synthetic prenyloxyphenylpropanoids (e.g., acetophenones, benzoic and cinnamic acids, chalcones, and coumarins), and we assessed their in vivo neuroprotective activity, using the mouse maximal electroshock-induced seizure model (MES test).
Unidentified anion gap metabolic acidosis.
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A 35-month-old female with nonketotic hyperglycinemia (NKH) presented to the Emergency department with severe hypoglycemia, fever, and several episodes of seizures. Due to worsening respiratory status, additional seizures and anion gap worsening metabolic acidosis the patient was transferred to the
Identification of different forms of cocaine and substances used in adulteration using near-infrared Raman spectroscopy and infrared absorption spectroscopy.
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Identification of cocaine and subsequent quantification immediately after seizure are problems for the police in developing countries such as Brazil. This work proposes a comparison between the Raman and FT-IR techniques as methods to identify cocaine, the adulterants used to increase volume, and
Expression and function of recombinant S1179D endothelial NO synthase in human pial arteries.
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OBJECTIVE
Mutation of serine 1179 to aspartate on the endothelial NO synthase (eNOS) increases NO production in the absence of stimulation by agonists. The present study was designed to determine the effect of recombinant S1179DeNOS gene expression on the vasomotor function of human pial
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