This work concerns the investigation of porous polybenzoxazines based on the non-toxic renewable diphenolic acid. The approach described relies on the in situ generation of foaming agent (CO2) during the thermal curing. For this purpose, the previously synthesized benzoxazine monomer from diphen...
The effect of the non-opioid antitussive caramiphen was studied in the rat maximal electroshock test. Caramiphen produced a dose- and time-dependent blockade of tonic hindlimb extension and was nearly twice as potent as the prototypical anticovulsant drug diphenylhydantoin. Pretreatment with a s...
Therapy of seizure activity following exposure to the nerve agent soman (GD) includes treatment with the anticonvulsant diazepam (DZP), an allosteric modulator of γ-aminobutyric acid A (GABAA) receptors. However, seizure activity itself causes the endocytosis of GABAA receptors and diminishes t...
The progression of epileptiform activity following soman (GD) exposure is characterized by a period of excessive cholinergic activity followed by excessive glutamatergic activity resulting in status epilepticus, which may lead to neuropathological damage and behavioral deficits. Caramiphen edisy...
Potent cholinesterase inhibitors such as sarin, induce an array of harmful effects including hypersecretion, convulsions and ultimately death. Surviving subjects demonstrate damage in specific brain regions that lead to cognitive and neurological dysfunctions. An early accumulation of acetylchol...
Antagonists of steroid receptors may interfere with seizure phenomena. The present study deals with effects of aminoglutethimide and spironolactone on the action of carbamazepine and diphenylhydantoin in amygdala-kindled rats of both genders. Co-administration of the antimineralocorticoid with c...
Gas chromatography–mass spectrometry (GC–MS) and high performance liquid chromatography (HPLC) offer highly efficient and potentially sensitive separation and detection techniques. This work describes the quantification of aminoglutethimide (AG) in nanocapsules suspension with both techniques....
Straightforward crushing and sieving bulk polymeric R-aminoglutethimide-imprinted materials were prepared by classical free radical polymerization, whereas nano thin walled grafted imprinted materials were prepared using RAFT mediated control polymerization technique. A stoichiometric non-covale...
In this study, the cellular effects resulting from the metabolism of aminoglutethimide by myeloperoxidase were investigated. Human promyelocytic leukemia (HL-60) cells were treated with aminoglutethimide (AG), an arylamine drug that has a risk of adverse drug reactions, including drug-induced ag...
The multifunctional alkoxysilane precursor, 2,6-bis(propyl-trimethoxysilylurelene)pyridine (DPS) was designed and synthesized, envisaging a multiple hydrogen-bond interaction in the molecular imprinting of the drug aminoglutethimide (AGT). Imprinted xerogels were obtained in bulk and spherical f...
Aminoglutethimide is an inhibitor of steroid synthesis in the adrenal cortex, where it inhibits a number of cytochrome P450-mediated steps, including the synthesis of pregnenolone from cholesterol. It also inhibits the cytochrome P450 aromatase enzyme responsible for the conversion of androgens ...
The separation of aminoglutethimide enantiomers by the continuous multicolumn chromatographic processes were investigated experimentally and theoretically, where the columns were packed with cellulose tris 3,5-dimethylphenyl-carbamate stationary phase (brand name Chiralcel OD) and mobile phase w...
Aminoglutethimide is a steroidogenesis inhibitor and inhibits a cholesterol side-chain cleavage enzyme (CYP11A1) that converts cholesterol to pregnenolone in mitochondria. We investigated histopathological changes induced by 5-day administration of AG in mice. Cytoplasmic vacuoles of various siz...
Aminoglutethimide is an inhibitor of steroid synthesis in the adrenal cortex, where it inhibits several cytochrome P450-mediated steps, including the synthesis of pregnenolone from cholesterol. It also inhibits the cytochrome P450 aromatase enzyme responsible for the conversion of androgens to e...
Thienopyrimidine scaffold is a fused heterocyclic ring system that structurally can be considered as adenine, the purine base that is found in both DNA and RNA-bioisosteres. Thienopyrimidines exist in three distinct isomeric forms. The current review discusses thieno[2,3-d]pyrimidine as a one of...
Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small molecule modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to th...
Two novel Michael adducts 9α-cyano-15,16-epoxy-7β-hydroxylabda-13(16),14-dien-6-one (2) and 9α-cyano-15,16-epoxy-7-hydroxylabda-7,13(16),14-trien-6-one (3) and the reduction product of 2, 9α-cyano-15,16-epoxy-6β,7β-dihydroxylabda-13(16),14-diene (4), were synthesized from the naturally occ...
Hispanolone (1), employed recently in our partial synthesis of the specific platelet activating factor antagonist prehispanolone (2), was prepared from (±)-Wieland-Miescher ketone (4).
Macrophages are highly plastic cells that adopt different functional phenotypes in response to environmental signals. Classically activated macrophages (M1) exhibit a pro-inflammatory role, mediating host defense against microorganisms or tumor cells; whereas alternatively activated macrophages ...
Pyrethroids are three membered ring compounds similar to the natural pyrethrins produced by the flowers of Chrysanthemum cinerariaefolium and C. coccineum. Pyrethroids are insecticides and may also have insect repellent properties and are generally harmless to humans. Due to our interest in comp...
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