In the present study, we analyzed the effects of a systemic treatment with the competitive 3β-hydroxysteroid dehydrogenase (3β-HSD) inhibitor trilostane on: (i) neurosteroid and monoamine levels in the brain, and (ii) the antidepressant activity of steroids and antidepressants in the forced sw...
Pituitary-dependent hyperadrenocorticism is a common endocrine disorder in dogs in the United States. Once a diagnosis is established, a decision must be made whether or not to pursue treatment, and if so, which medication to use. Historically, mitotane (Lysodren, o,p'-DDD, Bristol-Myers Sq...
Trilostane, a competitive inhibitor of 3β-hydroxysteroid dehydrogenase, is often used to treat canine hyperadrenocorticism. In some species, trilostane has been shown to have additional effects on steroid biosynthesis, and it has been postulated that trilostane might have effects on 11β-hydrox...
BackgroundTrilostane was identified in an in vivo screen of compounds in a lipopolysaccharide model of inflammation to support a repurposing effort. There is no previous documentation of any anti-inflammatory effects of trilostane.
Trilostane is a reversible, competitive inhibitor of 3 beta-hydroxysteroid dehydrogenase, a key enzyme involved in the synthesis of steroids. It inhibits the conversion of pregnenolone to progesterone, therefore inhibiting the synthesis of progesterone and, therefore, of the adrenal, gonadal, an...
Trilostane is a synthetic steroid analog used to treat canine hyperadrenocorticism. For small dogs, the dose found in commercially available dosage forms of trilostane is sometimes too high. Compounding trilostane in a liquid diluent provides an option for more precise dosing and adjustments, an...
The aim of this study was to describe the incidence and permanence of hypoadrenocorticism associated with trilostane treatment and to assess potential risk factors for hypoadrenocorticism. A retrospective cohort study was conducted using case records for 156 dogs treated with trilostane after a ...
5-Iodo- and 4,5-dibromo-2-methylpyridazin-3(2H)-ones were aminocarbonylated in the presence of various amines including amino acid methyl esters in a palladium-catalysed reaction. The iodo derivative afforded the corresponding amides with complete conversion and high isolated yields. The dibromo...
High-throughput screening of a small-molecule library identified a 5-triazolo-2-arylpyridazinone as a novel inhibitor of the important glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Such inhibitors are of interest due to PFKFB3’s control of the important glycolytic pa...
Six novel photochromic bisarylpyridazinones containing 2,5-dimethylthiophene or 5-methyl-2-phenylthiazole unit were synthesized, and their photochromic and fluorescence properties were investigated. The bisarylpyridazinones underwent reversible color change upon irradiation with UV or visible li...
Ninety 9,10-anthraquinone (AQ) derivatives and related anthracene derivatives were screened for mutagenicity with five Salmonella typhimurium tester strains with and without mammalian microsomal activation. About 35% of the compounds tested are considered to be mutagenic. Three patterns of mutag...
Leucoquinizarin reacted with butylamine to give 1-butylamino-4-hydroxyanthraquinone and 1,4-bis(butylamino)anthraquinone. Their structures were elucidated and the reaction mechanism was discussed from the kinetic studies. Quinizarin reacted with butylamine to give 2-butylaminoquinizarin selectiv...
Anthraquinones form the basis of several anticancer drugs. Anthraquinones anticancer drugs carry out their cytotoxic activities through their interaction with DNA, and inhibition of topoisomerase II activity. Anthraquinones (AQ4 and AQ4H) were synthesized and studied along with 1,4-DAAQ by compu...
Anthraquinones are well-known anticancer drugs. Anthraquinones anticancer drugs carry out their cytotoxic activities through their interaction with DNA, and inhibition of topoisomerase II activity. Anthraquinones (AQ5 and AQ5H) were synthesized and studied with 1,5-DAAQ by computational and expe...
The position of equilibrium between 7-substituted and 7,8-disubstituted 1,3,5-cyclooctatrienes (1) and the corresponding valence isomeric bicyclo[4.2.0]-2,4-octadienes (2) is highly sensitive to the nature of substituents. In particular, the difference between trans and cis-7,8 isomers in this r...
In the course of the Lewis acid-mediated cycloaddition of 1,8-bis(trimethylsilyl)-2,6-octadiene to bis-ketals, we have observed an unprecedented retro-Claisen condensation from the ketalisation of a 3-hydroxy-2,4-pentadione giving rise to a substituted 2,2,3-trimethoxybutane and an anti-Markovni...
The transformation of benzothiophene (BT) with 2-methyl-1-pentene was investigated over HBEA, HMCM-22 and HY zeolites having similar Brønsted acidities, at 85 °C under atmospheric pressure in a fixed bed reactor. Over these zeolites, BT underwent only alkylation, whereas 2-methyl-1-pentene unde...
The alkylation of 3-methylthiophene with 2-methyl-1-pentene was investigated over acidic zeolites at 85 °C under atmospheric pressure in a fixed bed reactor. Three zeolites were tested, HY, HBEA and HMCM-22, which presented different pore systems but the same Brønsted acidity. Over these zeolit...
13C NMR analysis of poly(4-methyl-1,3-pentadiene) (poly(4-MPD)) obtained by using the C2 symmetric zirconocene based catalytic system: rac-[CH2(3-tert-butyl-1-indenyl)2]ZrCl2 (1)/13C enriched methylaluminoxane (MAO) shows strong differences between the microstructure of the first inserted monome...
Pentafluorophenyl acrylate and -methacrylate were polymerized using AIBN as a thermal initiator. The obtained polymers were soluble polymeric active esters that could be used for the preparation of multifunctional polymers. The reactivity of poly(pentafluorophenylacrylate) and poly(pentafluoroph...
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