Disease relevance of Carbostyril

• Highly purified tetanus toxin at 2.5 x 10(5) 50% lethal doses per ml lost all toxicity in 40 mM PTL or 150 mM DPD but was not detectably affected by 100 mM HQL (the highest concentration possible) [1].
• In two calves suffering from Adema disease, the bovine parallel to Acrodermatitis enteropathica, hydroxyquinoline supplementation resulted in an increase in intestinal 65Zn absorption, while picolinic acid had no such effect [2].
• 2-Oxoquinoline 8-monooxygenase is a Rieske non-heme iron oxygenase that catalyzes the NADH-dependent oxidation of the N-heterocyclic aromatic compound 2-oxoquinoline to 8-hydroxy-2-oxoquinoline in the soil bacterium Pseudomonas putida 86 [3].
• Rebamipide, a gastroprotective drug, is a compound selected from over 500 amino acid analogs of 2(1H)-quinolinone tested for gastroprotective action and for efficacy to heal experimental gastric ulcers [4].
• In the case of patients with impetigo, hydrocortisone/potassium hydroxyquinoline sulphate proved significantly more effective than the other combination, the success rates being 92% and 74%, respectively [5].

Psychiatry related information on Carbostyril

• The reaction time for synthesis of carbostyril analogues was drastically reduced from a reported 18-58 h to only 80 min [6].

High impact information on Carbostyril

• Cells of the yeast Saccharomyces cerevisiae rapidly accumulated in the G1 phase of the cell cycle when exposed to the chelating agents o-phenanthroline (OP) or 8-hydroxyquinoline (HQ) [7].
• The electronic effect of the oxidized heterocyclic nitrogen atom makes the excited state both less basic and more acidic than the parent and adds hydroxyquinoline N-oxides to the class of high-acidity excited-state proton donors in photochemistry and photobiology [8].
• Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists [9].
• Effects of 2 quinolone antibacterials, temafloxacin and enoxacin, on theophylline pharmacokinetics [10].
• The synthesis of 5-(dipropylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij] quinolin-2(1H)-one (5), a potent dopamine D2 agonist showing high dopamine/serotonin (5HT1A) selectivity, is described [11].

Chemical compound and disease context of Carbostyril

• Effect of OPC-8212 (2(1H)-quinolinone), a new inotropic agent, on myocardial energy metabolism in patients with coronary heart disease [12].

Biological context of Carbostyril

• All of the target compounds were prepared by alkylation of the appropriate 2-oxoquinoline intermediates with a halo ester, followed by hydrolysis of the intermediate esters [13].
• Several iron chelators with hydroxyquinoline backbone were synthesized and their ability to inhibit basal as well as iron-induced mitochondrial lipid peroxidation was examined [14].
• On the inhibition of the b-c1 segment on the mitochondrial respiratory chain by quinone analogues and hydroxyquinoline derivatives [15].
• 2-Oxoquinoline 8-monooxygenase oxygenase component: active site modulation by Rieske-[2Fe-2S] center oxidation/reduction [3].
• Effect of 7-(3-[4-(2,3-dimethylphenyl)piperazinyl]propoxy)- 2(1H)-quinolinone (OPC-4392), a newly synthesized agonist for presynaptic dopamine D2 receptor, on tyrosine hydroxylation in rat striatal slices [16].

Anatomical context of Carbostyril

• In the iron-loaded hepatocyte cultures, the three hydroxyquinoline chelators, although showing diversity in terms of lipophilicity, appeared to be very similar in their capacity to chelate iron [17].
• Preincubation of membranes with either of the carbostyril congeners followed by washing reduced specific [125I]CYP binding capacity without changing the KD value for the remaining receptors [18].
• The interaction of the carbostyril derivatives 5-[2-[[1-(4-aminophenyl)-2-methyl-prop-2-yl]amino]-1-hydroxyethyl]- 8-hydroxycarbostyril (carbo-amine) and 5-[2-[[3-[4-(bromoacetamido)phenyl]-2-methylprop-2-yl]amino]-1- hydroxyethyl]-8-hydroxycarbostyril (carbo-Br) with the rat reticulocyte beta-adrenoreceptor system has been partially characterized [18].
• Studies on 2-oxoquinoline derivatives as blood platelet aggregation inhibitors. I. Alkyl 4-(2-oxo-1,2,3,4-tetrahydro-6-quinolyloxy)butyrates and related compounds [19].
• A microiontophoretic study was performed to investigate the effects of a newly synthesized quinolinone derivative, 7-[3-(4-(2,3-dimethylphenyl) piperazinyl) propoxy] 2-(1H)-quinolinone (OPC-4392), on neuronal activities of the ventral tegmental area (VTA) of rats anesthetized with chloral hydrate [20].

Associations of Carbostyril with other chemical compounds

• Derivatives carrying a substituent in the para position of the phenyl group of 8-hydroxy-5-[2-[(1-phenyl-2-methylprop-2-yl)amino]-1-hydroxyethyl] carbostyril (10) were prepared and their effects on beta-adrenoceptors evaluated in vitro [21].
• Plasma was acidified to the optimal pH (6.0) of angiotensin l generation with the least possible dilution, by using a single addition of hydrochloric acid and the enzyme inhibitor hydroxyquinoline [22].
• Four new hexadendate chelators, three hydroxyquinoline-based, Csox, O-Trensox, Cox750, and one catecholate-based CacCam-which have comparable skeletal structures and pFe, but widely different partition coefficients, (Kpart), 0.01, 0.02, 1 and 3.2 respectively, have been tested for their iron chelating efficacy in vitro by two methods [17].
• Characteristics of antitumor activity of 3,4-dihydro-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]- 2(1H)-quinolinone (vesnarinone) against a human adenoid squamous carcinoma-forming cell line grown in athymic nude mice [23].
• An in vitro system was used for growing this fruit, showing that the presence in the incubation medium of sucrose or hydroxyquinoline hemisulfate has no effect on the bioformation of these compounds [24].

Gene context of Carbostyril

• The novel hydroxyquinoline-containing tetrapodal ligand forms water soluble and stable chelates and is a good sensitizer of the NIR luminescence of its Nd(III) and Yb(III) complexes; its easy synthesis opens the way for potential biomedical applications [25].
• Several carbostyril-based beta-agonists have been shown to bind tightly to and slowly dissociate from the beta2-adrenoceptor (beta2AR) [26].
• The medium is supplemented with a recently described chromogenic substrate, hydroxyquinoline-beta-D-glucuronide, for beta-glucuronidase enzyme [27].
• Synthesis of 3-ureido derivatives of coumarin and 2-quinolone as potent acyl-CoA: cholesterol acyltransferase inhibitors [28].
• Hydroxyquinoline causes a marked increase in renal weight, the development of wedge-shaped foci with severely dilated tubule segments, and a simultaneous reduction in dehydrogenases, alkaline phosphatase, and alpha-naphthyl esterase [29].

Analytical, diagnostic and therapeutic context of Carbostyril

• Hydroxyquinoline overcomes PCR inhibition by UV-damaged mineral oil [30].
• The resistant hepatocyte model was chosen for a rat model of carcinogenesis and Sprague-Dawley rats were divided into the following groups: the control groups of normal diet and iron-rich diet with or without hydroxyquinoline and the groups of carcinogen alone and carcinogen plus iron-rich diet with or without administration of hydroxyquinoline [31].

References