In vitro enantioselective glucuronidation of fenoprofen.

abstract：BACKGROUND/AIMS:The in vivo metabolic profile of a benzopyridooxathiazepine (BPT) derivative, a potent tubulin polymerization inhibitor with a promising in vitro activity, was investigated. METHODS:The quantification of the BPT derivative and the identification of metabolites in the plasma of Wistar rats after i.p. an...

journal_title：Pharmacology

authors： Bourdon F,Lecoeur M,Lebègue N,Gressier B,Luyckx M,Odou P,Dine T,Goossens JF,Kambia N

更新日期：2014-01-01 00:00:00

abstract：:We investigated the effects of S-777469 (1-[[6-Ethyl-1-[4-fluorobenzyl]-5-methyl-2-oxo-1, 2-dihydropyridine-3-carbonyl]amino]-cyclohexanecarboxylic acid), a novel cannabinoid type 2 receptor (CB2) agonist, on 1-fluoro-2,4-dinitrobenzene (DNFB)-induced ear inflammation and mite antigen-induced dermatitis in mice. The o...

journal_title：Pharmacology

authors： Haruna T,Soga M,Morioka Y,Imura K,Furue Y,Yamamoto M,Hayakawa J,Deguchi M,Arimura A,Yasui K

更新日期：2017-01-01 00:00:00

abstract：:The effects of a 1- or 24-hour pretreatment regimen with monophosphoryl lipid A (MLA, 35 micrograms/kg i.v.) on myocardial stunning produced by repetitive coronary occlusions were studied in barbital-anesthetized dogs. Regional segment function (%SS) and myocardial blood flow were measured by sonomicrometry and the ra...

journal_title：Pharmacology

authors： Yao Z,Elliott GT,Gross GJ

更新日期：1995-09-01 00:00:00

abstract：:The effect of beta-adrenoceptor antagonists on the receptor-mediated low density lipoprotein (LDL) binding and internalization was studied in vitro in human skin fibroblasts. The cellular uptake of 125I-labeled human LDL was dose dependently elevated by some, but not all, of the drugs used. This effect of beta-adrenoc...

journal_title：Pharmacology

authors： Bernini F,Corsini A,Allorio M,Musanti R,Fumagalli R

更新日期：1987-01-01 00:00:00

abstract：:The temporal effects of vitamin A deficiency on hepatic cytochrome P-450-dependent and conjugation reactions were studied in the rat. Cytochrome P-450 levels and N-methyl-p-chloroaniline N-demethylase activity were significantly reduced in the deficient animals. No other changes in parameters dependent on cytochrome P...

journal_title：Pharmacology

authors： Siddik ZH,Drew R,Litterst CL,Mimnaugh EG,Sikic BI,Gram TE

更新日期：1980-01-01 00:00:00

abstract：:Glutathione S-transferases (GSTs) detoxify diverse electrophilic chemicals, including anticancer drugs. Containing at least 100 microM total GST, the adult rat liver has abundant alpha and mu class GST isoenzymes. We utilized primary cultured rat hepatocytes, maintained in chemically defined medium, to examine direct ...

journal_title：Pharmacology

authors： Grgurevich S,Greene FE

更新日期：1995-06-01 00:00:00

abstract：:Two diazepam derivatives, the N-desmethyl and the 2'-chlor-N-desmethyldiazepam, were compared in rats using behavioral and EEG techniques. Both drugs had depressant effects upon locomotor activity, facilitated behavior suppressed by punishment, increased the number of shocks received by rats in a Sidman avoidance proc...

journal_title：Pharmacology

authors： Babbini M,Gaiardi M,Bartoletti M

更新日期：1978-01-01 00:00:00

abstract：:This study was designed to evaluate the antidepressant activity of various antidepressants using the learned helplessness test (LH) or the forced swimming test (FS) in rats. Repeated treatment of the tricyclic antidepressants imipramine (10 mg/kg, p.o.), clomipramine (0.625 mg/kg, p.o.), amitriptyline (10 mg/kg, p.o.)...

journal_title：Pharmacology

authors： Takamori K,Yoshida S,Okuyama S

更新日期：2001-01-01 00:00:00

abstract：:The vasodepressor responses to intravenous injections of arachidonic acid, and the formation of its metabolites, were studied in rats made diabetic 1 or 2 weeks after a 1-dose alloxan treatment. Arachidonic acid dose-dependently decreased the diastolic blood pressure in normal animals, but this hypotensive effect was ...

journal_title：Pharmacology

authors： Hui SC,Ogle CW,Wang Z,An Y,Hu YH

更新日期：1989-01-01 00:00:00

abstract：:The frequent resistance of malignant tumors to chemotherapy documents the fact that numerous patients are uselessly traumatized by highly toxic drugs. Investigations into this resistance have shown that many different mechanisms exist which can abolish the antitumor action of chemotherapeutics. So far, no safe method ...

journal_title：Pharmacology

authors： Lippert TH,Ruoff HJ,Volm M

更新日期：2008-01-01 00:00:00

abstract：BACKGROUND/AIMS:Stent thrombosis is a serious complication after percutaneous coronary intervention and femoropopliteal endovascular intervention. The aim of this study was to determine the antithrombotic effects of a direct factor Xa inhibitor edoxaban alone or in combination with antiplatelet agents in a rat model of...

journal_title：Pharmacology

authors： Morishima Y,Honda Y,Kamisato C

更新日期：2019-01-01 00:00:00

abstract：:Neurochemical and neuropharmacological investigations with four ergot derivatives reveal differential pharmacodynamic effects of these compounds. Bromocriptine and CM 29-712 showed actions typical of postsynaptic dopamine receptor stimulants, in particular in the extrapyramidal system. CM 29-712 proved to be more pote...

journal_title：Pharmacology

authors： Vigouret JM,Bürki HR,Jaton AL,Züger PE,Loew DM

更新日期：1978-01-01 00:00:00

abstract：:Chronic administration of epinephrine to adult male rats resulted in a significant increase in the rate of ethanol elimination, when given alone or together with the beta-adrenergic blocker alprenolol. This effect was observed concomitantly with an increased hepatic oxygen utilization and no changes in mitochondrial r...

journal_title：Pharmacology

authors： Petermann M,Bravo M,Videla L,Ugarte G

更新日期：1979-01-01 00:00:00

abstract：:Acute ethanol administration to rats fasted overnight resulted in a significant decrease in the content of glutathione (GSH) of the liver concomitantly with a partial increase in oxidized glutathione levels, representing a net 38% decrease in total GSH equivalents. In these conditions, liver lipoperoxidation is signif...

journal_title：Pharmacology

authors： Videla LA,Fernández V,Valenzuela A,Ugarte G

更新日期：1981-01-01 00:00:00

abstract：:Honokiol and magnolol have been identified as modulators of the GABAA receptors in vitro. Our previous study suggested a possible selectivity of honokiol and magnolol on GABAA receptor subtypes. This possibility was examined in the current study by 3H-muscimol and 3H-flunitrazepam binding assays on various rat brain m...

journal_title：Pharmacology

authors： Ai J,Wang X,Nielsen M

更新日期：2001-07-01 00:00:00

abstract：BACKGROUND/AIMS:We studied the effect of the combined treatment with an angiotensin-converting enzyme (ACE) inhibitor (ramipril) and eplerenone compared with ramipril alone in streptozocin-induced diabetic rats. METHODS:Wistar rats were divided into 4 groups: nondiabetic controls, streptozocin-treated diabetic rats (5...

journal_title：Pharmacology

authors： Mavrakanas TA,Cheva A,Kallaras K,Karkavelas G,Mironidou-Tzouveleki M

更新日期：2010-01-01 00:00:00

abstract：:This study examined effects of intracerebroventricularly (i.c.v.) administered somatostatin (SRIH-14 and SRIH-28) on growth and function of pituitary somatotropes (GH cells) and lactotropes (PRL cells). Male rats received three i.c.v. injections (1 microgram/5 microliters) of SRIH-14 or SRIH-28 every second day. Blood...

journal_title：Pharmacology

authors： Milosević V,Brkić B,Velkovski SD,Sekulić M,Lovren M,Starcević V,Severs WB

更新日期：1998-07-01 00:00:00

abstract：:The oral bioavailability of two investigational formulations of bicalutamide was compared with the current clinical formulation. The first formulation was amorphous R-/S-bicalutamide in solid dispersion with a polymeric matrix of hydroxypropyl methylcellulose phthalate (HP55S) (R-/S-bicalutamide/HP55S); the second was...

journal_title：Pharmacology

authors： Cantarini M,Fuhr R,Morris T

更新日期：2006-01-01 00:00:00

abstract：:We investigated the antihypertensive effect of 5-HT1A agonist (buspirone) and 5-HT2B antagonists (SB204741 and SB200646) in deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats. Experiments were divided into two sets: in the first set, sham-operated control and DOCA-treated hypertensive rats received busp...

journal_title：Pharmacology

authors： Shingala JR,Balaraman R

更新日期：2005-03-01 00:00:00

abstract：BACKGROUND/AIMS:Vaginismus is characterized by recurrent or persistent involuntary contraction of the perineal muscles surrounding the outer third of the vagina when penile, finger, tampon, or speculum penetration is attempted. Recent results have suggested the use of botulinum toxin for the treatment of vaginismus. He...

journal_title：Pharmacology

authors： Ferreira JR,Souza RP

更新日期：2012-01-01 00:00:00

abstract：:The aims of the present study were to investigate the pharmacological effects induced by Tityus serrulatus venom (TsV) and its fractions and to compare with the effects induced by pure alpha (TsTX-V) and beta (TsTX-I) toxins isolated from TsV on rat retractor penis muscle (RPM). TsV, fractions X, XI, XIIa, XIIb (0.01-...

journal_title：Pharmacology

authors： Bomfim JH,de Godoy MA,Giglio JR,de Oliveira AM,Arantes EC

更新日期：2005-03-01 00:00:00

abstract：:43 patients with osteoarthritis of the knee and/or hip(s) were treated with suprofen 800 mg/day or ibuprofen 1,600 mg/day for 14 days. Both drugs produced an improvement in subjective symptoms by day 7, although the most rapid analgesic effect was obtained with suprofen. Patients receiving suprofen experienced a signi...

journal_title：Pharmacology

authors： Schuermans Y

更新日期：1983-01-01 00:00:00

abstract：:Congestive heart failure (CHF) is associated with exercise intolerance that cannot be entirely explained by hypoperfusion of the skeletal muscles. We studied the contractile properties of fast-twitch (extensor digitorum longus; EDL) and slow-twitch (soleus; SOL) skeletal muscles in doxorubicin-induced CHF in rats, and...

journal_title：Pharmacology

authors： Ertunc M,Sara Y,Korkusuz P,Onur R

更新日期：2009-01-01 00:00:00

abstract：:The use of angiotensin converting enzyme (ACE) inhibitors in combination with diuretics is a common strategy used for the treatment of patients affected by heart failure. An infant affected by initial congestive cardiac failure, after starting the treatment with enalapril in association with furosemide, developed acut...

journal_title：Pharmacology

authors： Fabiano V,Carnovale C,Gentili M,Radice S,Zuccotti GV,Clementi E,Perrotta C,Mameli C

更新日期：2016-01-01 00:00:00

abstract：AIMS:To compare the bioavailability of a new oromucosal formulation of flurbiprofen 8.75-mg lozenges, developed by Alfa Wassermann S.p.A. (test drug) to that of marketed flurbiprofen 8.75-mg lozenges (Benactiv Gola®, reference drug). METHODS:This was an open, randomised, two-period, crossover, pharmacokinetic (PK) stu...

journal_title：Pharmacology

authors： Matzneller P,Burian A,Martin W,Annoni O,Lauro V,Tacchi R,Brunner M,Zeitlinger M

更新日期：2012-01-01 00:00:00

abstract：:We determined the susceptibility of two ages of rat pups to become tolerant to and dependent on morphine infusions from osmotic minipumps. Neonatal rats (postnatal day 6; P6) were infused for 72 h with morphine at 0.175 or 0.7 mg/kg/h. On P9, morphine's antinociceptive efficacy was reduced in both groups. P14 infant r...

journal_title：Pharmacology

authors： Stoller DC,Thornton SR,Smith FL

更新日期：2002-09-01 00:00:00

abstract：:The relationship between alpha(1)-adrenoceptor binding in rat tissues and pharmacodynamic effects of continuous infusion of KMD-3213 was examined. In vivo specific binding of [(3)H]KMD-3213 after continuous intravenous infusion of the ligand (100 pmol/kg/min for 10 min, followed by 30 pmol/kg/min for 60 or 90 min) dif...

journal_title：Pharmacology

authors： Akiyama K,Tatemichi S,Katayama S,Nakajima M,Oki T,Okura T,Yamada S,Kimura R

更新日期：2002-01-01 00:00:00

abstract：:Previously published data from this laboratory on the urinary excretion of 3-hydroxymethyl antipyrine (one of the major metabolites of antipyrine in man) have to be reconsidered, because of use of an impure reference substance in the high-pressure liquid chromatographic assay method. Comparison with newly synthesized,...

journal_title：Pharmacology

authors： Danhof M,Teunissen MW,Breimer DD

更新日期：1982-01-01 00:00:00

abstract：:Previous investigations demonstrated that CYP2D16 was expressed at high levels in guinea pig adrenal microsomes. The studies presented here were done to determine whether adrenal metabolism of bufuralol (BUF), a model CYP2D substrate, was similar to that in the liver. Guinea pig adrenal microsomes converted BUF to 1'-...

journal_title：Pharmacology

authors： Colby HD,Nowak DM,Longhurst PA,Zhang X,Hayes JR,Voigt JM

更新日期：2001-05-01 00:00:00

abstract：:Various new butyridenyl-2-hydroxybenzylidenyl-1,3-thiazolidinones were synthesized and characterized by elemental analyses, IR and PMR spectral data. The compounds were evaluated for their ability to afford protection against inflammation by carrageenin-induced oedema and cotton pellet implantation in albino rats of e...

journal_title：Pharmacology

authors： Tandon M,Kumar P,Pande K,Bhalla TN,Barthwal JP

更新日期：1985-01-01 00:00:00