Pharmacological characterization of M-II, the major human metabolite of ramelteon.

abstract：INTRODUCTION:Homeostasis of cholesterol is crucial for cellular function, and dysregulated cholesterol biosynthesis is a metabolic event that can lead to hepatic and cardiovascular abnormalities. OBJECTIVE:The aim of this study was to investigate the effects and mechanisms of domain-associated protein (Daxx) and andro...

journal_title：Pharmacology

authors： Li TP,Sun SW,Xiong GZ,Qiu F,Yang DM,Sun SY,Xie XJ,Liao DF,Chen JX,Tuo QH

更新日期：2020-07-21 00:00:00

abstract：:The function of melatonin (MLT) in promoting fracture healing has been demonstrated in previous studies. However, the molecular mechanism underlying therapeutic effects of MLT is not entirely clear. In this study, mesenchymal stem cells (MSCs) were isolated from rat bone marrow and identified by flow cytometry. We fou...

journal_title：Pharmacology

authors： Dong P,Gu X,Zhu G,Li M,Ma B,Zi Y

更新日期：2018-01-01 00:00:00

abstract：:Gene knockout mice have proven to be very useful in understanding the role of xenobiotic-metabolizing enzymes in chemical toxicity and carcinogenesis. The combination of gene knockout technology with transgenic mouse technology should provide more versatile and suitable animal models to study the risks of chemical exp...

journal_title：Pharmacology

authors： Kimura S,Gonzalez FJ

更新日期：2000-09-01 00:00:00

abstract：:Danthron infused intravenously in rats shows a complex dose-dependent pattern of metabolism and excretion. The metabolites, particularly the more polar ones, are in general excreted predominantly in bile, to a lesser extent in urine. They can be separated as metabolite groups according to polarity and molecular size o...

journal_title：Pharmacology

authors： Sund RB,Junker T,Malterud KE

更新日期：1993-10-01 00:00:00

abstract：:Three synthetic peptides, urotensin I, sauvagine and ovine CRF, have less than 50% sequence homology. In the dog, all three produce selective mesenteric dilation, which appears to be solely responsible for a decrease in peripheral resistance and systemic arterial blood pressure. Urotensin I and sauvagine were found to...

journal_title：Pharmacology

authors： MacCannell KL,Lederis K,Hamilton PL,Rivier J

更新日期：1982-01-01 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：:Self-administration of either nicotine (NIC) or ethanol (ETH) has been extensively studied. This study addressed for the first time the self-administration of both substances when offered together. Male and female rats of different ages were offered NIC and ETH using the two- or three-bottle free-choice method. When N...

journal_title：Pharmacology

authors： Marshall CE,Dadmarz M,Hofford JM,Gottheil E,Vogel WH

更新日期：2003-03-01 00:00:00

abstract：:Three doses (0.31, 3.1 and 31 mg/kg) of methotrexate (MTX) were given intravenously to rats. The resulting concentration-time curves in plasma (normalized by dividing the plasma concentration by a multiple of the dose) were not superimposable, indicating nonlinear plasma pharmacokinetics. In liver, kidney, bone marrow...

journal_title：Pharmacology

authors： Scheufler E

更新日期：1982-01-01 00:00:00

abstract：:The purpose of this investigation on human umbilical arteries was: (1) to analyze the effects of magnesium (Mg2+) in the prevention of contractions induced by 5-hydroxytryptamine (5-HT), KCl, Bay K 8644 and BaCl2; (2) to determine whether the presence of Mg2+ could modulate the response to caffeine in Ca2+-free medium...

journal_title：Pharmacology

authors： Tiritilli A

更新日期：1998-12-01 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 gross behavioral observation the minimum effective dose of zopiclone was intravenously 0.06-0.25 mg/kg and intragastrically 1-4 mg/kg in rhesus monkeys. Zopiclone suppressed barbital withdrawal signs of rhesus monkeys at a single dose of 16 mg/kg or more. The suppressing effect of zopiclone 32 mg/kg i.g. was compar...

journal_title：Pharmacology

authors： Yanagita T

更新日期：1983-01-01 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：AIM:To evaluate the efficacy and safety of 2 analogs of L-carnitine on rats made insulin resistant by a high-fructose diet. METHODS:Using rats made insulin resistant by a high-fructose diet, we investigated the impact of 2 analogs of L-carnitine (25 mg/kg) and L-carnitine (250 mg/kg) on glucose, triglycerides and chol...

journal_title：Pharmacology

authors： Gómez-Solís A,De la Cruz-Cordero R,Avalos-Soriano A,Duarte-Vázquez MA,Reyes-Esparza J,Rodríguez-Fragoso L

更新日期：2011-01-01 00:00:00

abstract：:Papers published over 100 years since the beginning of the scientific study of drug metabolism in birds were reviewed. Birds were found to be able to accomplish more than 20 general biotransformation reactions in both functionalization and conjugation. Chickens were the primary subject of study but over 30 species of ...

journal_title：Pharmacology

authors： Pan HP,Fouts JR

更新日期：1979-01-01 00:00:00

abstract：:The systemic and coronary hemodynamic effects of the nitrovasodilator, pirsidomine, were compared with SIN-1, nitroprusside, and nitroglycerin. Four groups consisting of 32 experiments were performed in 17 conscious dogs chronically instrumented for measurement of aortic and left ventricular pressure, left ventricular...

journal_title：Pharmacology

authors： Arkonac BM,Kersten JR,Wynsen JC,Nijhawan N,Warltier DC

更新日期：1996-02-01 00:00:00

abstract：:The present study examined the interaction of opioidergic systems in the hypotensive action of atenolol. Anesthetized, adult spontaneously hypertensive (SHR) and Wistar Kyoto (WKY) rats were instrumented to monitor blood pressure and heart rate. Atenolol (100 micrograms/kg, i.v.) produced a decrease in blood pressure ...

journal_title：Pharmacology

authors： Laskey RE,Jones LF,Tackett RL

更新日期：1989-01-01 00:00:00

abstract：BACKGROUND/AIMS:Isoniazid (ISO) has been reported to inhibit the hepatic aldehyde dehydrogenase (ALDH) and to cause a disulfiram (DIS)-like reaction, albeit there are no reports demonstrating increased blood acetaldehyde levels after co-administration of ISO with alcohol. The aim of our study was to clarify whether the...

journal_title：Pharmacology

authors： Karamanakos PN,Pappas P,Boumba V,Vougiouklakis T,Marselos M

更新日期：2016-01-01 00:00:00

abstract：:A potential cytokine-drug interaction between interleukin 6 (IL-6) and itraconazole (ITZ) was studied using human hepatocytes in primary culture. Cultures from 5 adult males (mean age 42 +/- 15 years) who had not received any medicines known to interact with CYP3A4 were studied. Cultures were exposed to ITZ 500 ng/ml,...

journal_title：Pharmacology

authors： Gubbins PO,Melchert RB,McConnell SA,Franks AM,Penzak SR,Gurley BJ

更新日期：2003-04-01 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：:The haemodynamic changes during epidural anaesthesia and following the administration of dihydroergotamine (DHE; 10 micrograms/kg i.v.) were studied in 7 dogs (epidural group). Epidural anaesthesia was associated with reductions in mean arterial, mean pulmonary arterial and mean right atrial pressures. Femoral flow wa...

journal_title：Pharmacology

authors： Zimpfer M,Schwarz M,Stanek B,Raberger G

更新日期：1981-01-01 00:00:00

abstract：AIMS:The aim of the present study was to investigate the effects of rutin on potassium oxonate-induced hyperuricemia and renal dysfunction in mice. METHODS:Rutin was administered orally 1 h after oxonate at doses of 25, 50 and 100 mg·kg(-1). Serum uric acid levels and kidney function parameters were assayed. Mouse uro...

journal_title：Pharmacology

authors： Chen YS,Hu QH,Zhang X,Zhu Q,Kong LD

更新日期：2013-01-01 00:00:00

abstract：PURPOSE:The purpose of this study is to examine the effectiveness of introducing both rituximab (RTX) and 131I for active Graves' ophthalmopathy (GO) with hyperthyroidism. METHODS:In total, 217 patients suffering from active GO with hyperthyroidism were included in this research. All subjects were randomly assigned to...

journal_title：Pharmacology

authors： Li J,Xiao Z,Hu X,Li Y,Zhang X,Zhang S,Gong W,Zhao J,Ye X

更新日期：2017-01-01 00:00:00

abstract：:Various attempts to developing antagonists for substance P (SP) and related peptides, based on our past experience with angiotensin, kinins, and neurotensin, were unsuccessful. The particular features of SP, namely the high activity of C-terminal partial sequences in some pharmacological tests were used to develop one...

journal_title：Pharmacology

authors： Regoli D,Escher E,Mizrahi J

更新日期：1984-01-01 00:00:00

abstract：:delta9-Tetrahydrocannabinol (THC) inhibited ulcer formation in the pylorus-ligated rat (Shay rat test). However, this antiulcer activity of THC was substantially less than for the anticholinergic substance tridihexethyl chloride both in terms of degree of activity and potency. In addition, the results of the present s...

journal_title：Pharmacology

authors： Sofia RD,Diamantis W,Harrison JE,Melton J

更新日期：1978-01-01 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：: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：:The present study was designed to investigate the effects of fluid administration on survival in endotoxemic or septicemic male Sprague-Dawley rats. Endotoxemia was induced by intravenous injection of Escherichia coli lipopolysaccharide (LPS), and septicemia produced by cecal ligation and puncture (CLP). In endotoxemi...

journal_title：Pharmacology

authors： Smith EF 3rd,Slivjak MJ,Egan JW,Gagnon R,Arleth AJ,Esser KM

更新日期：1993-05-01 00:00:00

abstract：:Previously it was demonstrated that intravenously administered morphine produced greater analgesic but lower hyperthermic responses to morphine in 24-week-old rats in comparison to 8-week-old rats. The differential pharmacological responses to morphine could not solely be attributed to the pharmacokinetic parameters, ...

journal_title：Pharmacology

authors： Bhargava HN,Villar VM,Rahmani NH,Larsen AK

更新日期：1993-07-01 00:00:00

abstract：:Feeding a thiamin-deficient diet to male and female rats for 3 weeks alters the mixed function oxidases responsible for metabolizing benzo(a)pyrene and enhances the response of these enzymes to induction by phenobarbital or 3-methylcholanthrene. The caloric restriction observed in thiamin deprivation may be partially ...

journal_title：Pharmacology

authors： Wade AE,Bunce OR,Harley W,Baker MT,Holmes D

更新日期：1984-01-01 00:00:00

abstract：:Various stressful stimuli cause mast cell degranulation. Hemorrhagic shock is one such stressful stimulus which may cause mast cell degranulation and histamine release. Histamine may be involved in the pathophysiology of hemorrhage. It was reported that there are large amounts of histamine in the anterior and posterio...

journal_title：Pharmacology

authors： Tikiz H,Tunçel N,Gürer F,Baycu C

更新日期：1991-01-01 00:00:00