Effects of staurosporine on the pressor responses to alpha-adrenoceptor agonists in pithed rats: a comparison with nifedipine.

abstract：BACKGROUND/AIMS:Putative in vitro-in vivo correlations of pharmacokinetic (PK) parameters are regarded as a prerequisite to filter hits derived from high-throughput screening (HTS) approaches for subsequent murine in vivo PK studies. METHODS:In this study, we assessed stabilities in rat and human microsomes of 121 com...

journal_title：Pharmacology

authors： Schrezenmeier E,Zollmann FS,Seidel K,Böhm C,Schmerbach K,Kroh M,Kirsch S,Klare S,Bernhard S,Kappert K,Goldin-Lang P,Skuballa W,Unger T,Funke-Kaiser H

更新日期：2012-01-01 00:00:00

abstract：:Wood creosote, a mixture of phenolic compounds, suppresses in vitro contractions of rat intestine. To identify a compound in wood creosote able to inhibit intestinal motility, we screened its constituent phenolic compounds and found 4-ethylguaiacol (4-EG) as an active compound. It suppressed the spontaneous phasic (IC...

journal_title：Pharmacology

authors： Toyoda M,Ogata N,Shibata T

更新日期：1993-11-01 00:00:00

abstract：:Metabotropic G protein-coupled receptors have recently been recognized as targets for anesthetics and analgesics. In particular, G(q)-coupled receptors such as muscarinic M(1) receptors (M(1)R) and 5-hydroxytryptamine (5-HT) type 2A receptors have been reported to be targets for anesthetics. Much less is known, howeve...

journal_title：Pharmacology

authors： Minami K,Uezono Y,Shiraishi M,Okamoto T,Ogata J,Horishita T,Taniyama K,Shigematsu A

更新日期：2004-11-01 00:00:00

abstract：:In anesthetized rats the glucose release of the kidneys was estimated from the glucose concentrations in the arterial and renal venous plasma, urinary glucose excretion and the total renal plasma flow. Net renal glucose release was found in control experiments. The glucose release of the kidneys decreased with rising ...

journal_title：Pharmacology

authors： Greven J,van Eys B,Jacobs W

更新日期：1975-01-01 00:00:00

abstract：:Zopiclone (ZPC; RP 27,267), which is chemically unrelated to benzodiazepines (BZD), was found to have a similar pharmacological profile and to possess in man hypnotic activity similar to that of some BZD such as nitrazepam. It was, therefore, interesting to study the interaction of ZPC with rat brain receptors and spe...

journal_title：Pharmacology

authors： Blanchard JC,Boireau A,Julou L

更新日期：1983-01-01 00:00:00

abstract：:Previous studies have demonstrated that calcium storage and release from IP3-dependent sites in the sarcoplasmic reticulum play an important role in the contractile response of the rabbit urinary bladder to both field stimulation (mediated via neurotransmitter release) and bethanechol (direct muscarinic stimulation). ...

journal_title：Pharmacology

authors： Levin RM,Nicholas TJ,Snitkoff GG,Mandell J,Russell D,Wilbur HJ,Mogavero LJ

更新日期：1997-12-01 00:00:00

abstract：:The effect of promethazine on the metabolic responsiveness of human polymorphonuclear leukocytes to opsonized zymosan was evaluated by chemiluminescence (CL) assay under the following situations: (1) preincubation of granulocytes with promethazine; (2) simultaneous addition of zymosan and promethazine, and (3) additio...

journal_title：Pharmacology

authors： Trush MA,Van Dyke K

更新日期：1978-01-01 00:00:00

abstract：:This study was designed to document possible changes in the binding of bupivacaine (BV), lidocaine (LC) and their main metabolites desbutylbupivacaine (PPX) and monoethylglycinexylydide (MEGX), respectively, to plasma proteins and erythrocytes in mice after acute treatment with the calcium antagonists diltiazem (DZ), ...

journal_title：Pharmacology

authors： Jacob D,Grignon S,Attolini L,Gantenbein M,Bruguerolle B

更新日期：1996-10-01 00:00:00

abstract：:In anesthetized rats intravenously infused, norepinephrine (NE) was accumulated by the heart, the spleen and the lung in a dose-related manner. With the lower dose of NE (2.5 mg/kg) the organ/blood ratios were more than unity and were generally greater than with higher doses (5 and 10 mg/kg), indicating that accumulat...

journal_title：Pharmacology

authors： Sivaramakrishna N,Gulati OD

更新日期：1975-01-01 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：:Stimulants (histamine, acetylcholine and substance P) and relaxants (isoprenaline and bradykinin) of the guinea pig trachea were tested in the absence and presence of mepacrine, eicosatetraynoic acid, BW 755C and indomethacin in order to evaluate the involvement of prostaglandins and congeners in the effects of amines...

journal_title：Pharmacology

authors： Mizrahi J,D'Orléans-Juste P,Caranikas S,Regoli D

更新日期：1982-01-01 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：:The signaling of seven transmembrane receptors/G-protein- coupled receptors (GPCRs) is regulated by a number of receptor interacting proteins, including βarrestins (βarrs) and GPCR kinases (GRKs). In the present report, we have analyzed the interaction pattern between the glucagon-like peptide-1 (GLP-1) receptor (GLP-...

journal_title：Pharmacology

authors： Jorgensen R,Norklit Roed S,Heding A,Elling CE

更新日期：2011-01-01 00:00:00

abstract：:The effects of aspirin and suprofen on gastrointestinal blood loss were compared in a double-blind, crossover study of 20 healthy male subjects. Fecal blood loss was measured by 51Cr-labeled red cells. Subjects treated with aspirin (2,600 mg/day) experienced a mean fecal blood loss of 4.2 ml/day, compared with subject...

journal_title：Pharmacology

authors： Arnold JD,Berger AE

更新日期：1983-01-01 00:00:00

abstract：:The regulatory action exerted on receptors by acebutolol, a cardioselective beta-blocker containing intrinsic sympathomimetic activity, has been investigated. beta-Adrenoceptor affinity and density of human mononuclear leukocytes were assayed in hypertensive patients before and after treatment with 400 mg/day acebutol...

journal_title：Pharmacology

authors： Basso A,Piantanelli L,Cognini G,Giunta S,Andreoni A,Paciaroni E

更新日期：1985-01-01 00:00:00

abstract：:The hypoxia-inducible factor 1alpha (HIF-1alpha), a member of the PAS superfamily, is a global regulator of cellular and systemic O(2) homeostasis as well as embryonic development. As the activity of HIF-1alpha is increased by a lowered oxygen tension in vivo and in vitro, we established a cell line producing high amo...

journal_title：Pharmacology

authors： Meissner U,Allabauer I,Repp R,Rascher W,Dötsch J

更新日期：2003-10-01 00:00:00

abstract：:The effects of the novel antihypertensive agent, carvedilol, on renal hemodynamics and excretory function have been investigated and compared with the effects of labetalol in conscious, spontaneously hypertensive rats. Sustained intravenous infusion of carvedilol or labetalol at a rate of 10 micrograms/kg/min resulted...

journal_title：Pharmacology

authors： Gellai M,DeWolf R,Ruffolo RR Jr

更新日期：1990-01-01 00:00:00

abstract：:The marijuana plant Cannabis sp. and its derivatives and analogues, known as cannabinoids (CBs), induce many effects throughout the whole body. Herein we briefly review the gastrointestinal (GI) pharmacology of CBs, with special focus on motor function. Some drugs are available to treat nausea and emesis, and evidence...

journal_title：Pharmacology

authors： Abalo R,Vera G,López-Pérez AE,Martínez-Villaluenga M,Martín-Fontelles MI

更新日期：2012-01-01 00:00:00

abstract：:The diastereomeric glucuronic acid conjugates are major metabolites of the nonsteroidal anti-inflammatory drug fenoprofen (FEN). Glucuronidation of FEN enantiomers was investigated with liver microsomal preparations from different species (sheep, rabbit, rat and human). The formed R- and S-FEN conjugates can be separa...

journal_title：Pharmacology

authors： Volland C,Benet LZ

更新日期：1991-01-01 00:00:00

abstract：:TRK-530 is a novel synthetic bisphosphonate compound which exhibits inhibitory activity in the rat adjuvant arthritis (AA) model. We found that, during AA development, the concentrations of cytokine-induced neutrophil chemoattractant-1 (CINC-1) and tumor necrosis factor alpha (TNF-alpha) in the bone marrow increased, ...

journal_title：Pharmacology

authors： Tanahashi M,Koike J,Kawabe N,Nakadate-Matsushita T

更新日期：1998-05-01 00:00:00

abstract：:The cardioprotective effects of (2S,3R,4S)-N'-benzyl- N"-cyano-N-(3,4-dihydro-2-dimethoxymethyl-3-hydro- xy-2-methyl-6-nitro-2H-benzopyran-4-yl)-guanidine (KR-31372) were evaluated against ischemic/reperfusion injury in isolated rat hearts in vitro and in anesthetized rats and dogs in vivo. In isolated perfused rat he...

journal_title：Pharmacology

authors： Lee BH,Seo HW,Yoo SE

更新日期：2004-02-01 00:00:00

abstract：:Tetraethylammonium chloride (TEA) at concentrations over 10(-3) mol/l produced a concentration-dependent contraction in the isolated canine coronary artery. We investigated mechanisms of the contractile response and the effects of various vasodilators on the contraction. While phentolamine, propranolol, guanethidine, ...

journal_title：Pharmacology

authors： Nishio M,Kigoshi S,Muramatsu I

更新日期：1986-01-01 00:00:00

abstract：:In the isolated guinea pig vas deferens, 10(-4) M cocaine shifts to the left (13.5-fold at the EC50 level) the concentration-effect curve and increases the maximum response to noradrenaline, whilst supersensitivity to phenylephrine, an amine with a low affinity for the neuronal uptake, was smaller (4.1-fold) and the m...

journal_title：Pharmacology

authors： DeMoraes S,Capaz FR

更新日期：1977-01-01 00:00:00

abstract：:Clofibrate treatment decreased drastically the activity of serum postheparin lipoprotein lipase of rats fed with fat-free test diet but had no effect on hepatic lipase. 3 weeks' treatment was followed by a significant fall in serum cholesterol caused by a marked decrease in HDL-cholesterol. Clofibrate decreased in vit...

journal_title：Pharmacology

authors： Strandberg TE,Kuusi T,Tilvis RS,Miettinen TA

更新日期：1983-01-01 00:00:00

abstract：:Sensitive radiometric assays were adapted to study the development and kinetics of meperidine and methadone N-demethylation and morphine glucuronidation by microsomes isolated from livers of fetal stump-tailed macaques (Macaca arctoides). Times in development selected for study were midterm, three-quarter term, near t...

journal_title：Pharmacology

authors： Dvorchik BH,Stenger VG,Hartman RD

更新日期：1979-01-01 00:00:00

abstract：:Several compounds with the backbone of 1,4-naphthoquinone chemical structure have been reported to display antiplatelet and antithrombotic activities, indicating that this congener compound may be a new source in the antithrombotic drug development. In the present study, the possible antiplatelet activity and antithro...

journal_title：Pharmacology

authors： Jin YR,Ryu CK,Moon CK,Cho MR,Yun YP

更新日期：2004-04-01 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：:A multicenter, placebo-controlled, double-dummy, randomized, parallel-group, double-blind study was conducted to verify the hypothesis of noninferiority for single-dose administration of zaltoprofen 160 mg, a nonsteroidal anti-inflammatory drug, compared with loxoprofen sodium 60 mg (loxoprofen), in terms of antipyret...

journal_title：Pharmacology

authors： Azuma A,Kudoh S,Nakashima M,Nagatake T

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND/AIMS:Since beta-adrenoceptors have been shown to affect cardiac gap junction channels, we wanted to elucidate the possible effect of metoprolol on the gap junction protein connexin-43, using racemic RS-metoprolol or the isomer R-metoprolol (no beta-adrenoceptor blockade) or S-metoprolol (beta(1)-adrenoceptor...

journal_title：Pharmacology

authors： Salameh A,Blanke K,Dhein S,Janousek J

更新日期：2010-01-01 00:00:00

abstract：OBJECTIVE:To study the myocardial benefit effect and mechanism of paeoniflorin on myocardial ischemia reperfusion injury (MIRI) in rats. METHODS:Hundred SD rats were randomly divided into 5 groups: sham group, model group, Paeoniflorin (15 mg/kg) group, Paeoniflorin (30 mg/kg) group, and Paeoniflorin (60 mg/kg) group....

journal_title：Pharmacology

authors： Wu F,Ye B,Wu X,Lin X,Li Y,Wu Y,Tong L

更新日期：2020-01-01 00:00:00