Formation of the thiol adducts of 4'-(9-acridinylamino)methanesulfon-m-anisidide and their binding to deoxyribonucleic acid.

abstract：:There is evidence to suggest that the oxidative metabolism of hydralazine (HP), an antihypertensive drug, may represent a toxic pathway which could account for some of the adverse effects of the drug. Experiments were done to determine whether the hepatic oxidative metabolism of HP is associated with the formation of ...

journal_title：Biochemical pharmacology

authors： LaCagnin LB,Colby HD,Dalal NS,O'Donnell JP

更新日期：1987-08-15 00:00:00

abstract：:Glucuronidation, catalyzed by UDP-glucuronosyltransferases (UGTs), is a crucial substance metabolism and elimination process that mostly occurs in the liver to protect the body from toxic substances and maintain homeostasis. The reaction functions well in a uridine diphosphate glucuronic acid (UDPGA) -dependent manner...

journal_title：Biochemical pharmacology

authors： Zhang L,Zhu L,Qu W,Wu F,Hu M,Xie W,Liu Z,Wang C

更新日期：2020-02-01 00:00:00

abstract：:During receptor-mediated endocytosis (RME), extracellular molecules are internalized after being recognized and bound to specific cell surface receptors. In previous studies of the asialoglycoprotein receptor (ASGPR) in rats, we showed that ethanol impairs RME at multiple ASGPR sites. Ethanol administration has been s...

journal_title：Biochemical pharmacology

authors： Dalton SR,Wiegert RL,Baldwin CR,Kassel KM,Casey CA

更新日期：2003-02-15 00:00:00

abstract：:Coenzyme CoQ10 (CoQ10), a ubiquinone compound, has been reported to inhibit tyrosinase activity and melanin production in melanoma B16F10 cells. However, the molecular mechanism underlying this inhibitory effect is poorly understood. In this paper we aimed to investigate the molecular mechanisms involved in the anti-m...

journal_title：Biochemical pharmacology

authors： Hseu YC,Ho YG,Mathew DC,Yen HR,Chen XZ,Yang HL

更新日期：2019-06-01 00:00:00

abstract：:gamma-Carbolines are tricyclic aromatic compounds which intercalate into DNA base pairs and exhibit significant cytotoxic and antitumor activities. These compounds which are structurally related to ellipticine by deletion of an aromatic ring, induce DNA breaks in cultured L1210 cells. Since the mechanism of cytotoxic ...

journal_title：Biochemical pharmacology

authors： Fossé P,René B,Saucier JM,Nguyen CH,Bisagni E,Paoletti C

更新日期：1990-02-15 00:00:00

abstract：:The aim of the present study was to investigate the effects of myricitrin, a flavonoid with anti-inflammatory and antinociceptive action, upon persistent neuropathic and inflammatory pain. The neuropathic pain was caused by a partial ligation (2/3) of the sciatic nerve and the inflammatory pain was induced by an intra...

journal_title：Biochemical pharmacology

authors： Meotti FC,Missau FC,Ferreira J,Pizzolatti MG,Mizuzaki C,Nogueira CW,Santos AR

更新日期：2006-12-15 00:00:00

abstract：:Oligodendrocytes and activated macrophages are involved in the immunopathology of demyelinating disease. In this study, we investigated the in vitro effect of dietary compounds, in particular flavonoids, on oxidative damage in OLN-93 oligodendrocytes and on nitric oxide (NO) production by NR8383 macrophages. Using a c...

journal_title：Biochemical pharmacology

authors： van Meeteren ME,Hendriks JJ,Dijkstra CD,van Tol EA

更新日期：2004-03-01 00:00:00

abstract：:In activation of 12-lipoxygenase (12-LO) in mouse epidermal homogenate by the antipsoriatic drug anthralin has been studied in detail. In view of the chemical instability of anthralin in a physiological buffer, the biological effects ascribed to the molecule itself may be related to some of its breakdown products. How...

journal_title：Biochemical pharmacology

authors： Müller K,Gawlik I

更新日期：1996-05-03 00:00:00

abstract：BACKGROUND AND PURPOSE:Beraprost is a prostacyclin analogue and IP receptor agonist which is approved to treat pulmonary arterial hypertension (PAH) in Asia. The beraprost-314d isomer (esuberaprost) is one of four stereoisomers contained within the racemic mixture of beraprost. The pharmacological profile of esuberapro...

journal_title：Biochemical pharmacology

authors： Shen L,Patel JA,Norel X,Moledina S,Whittle BJ,von Kessler K,Sista P,Clapp LH

更新日期：2019-08-01 00:00:00

abstract：:Stimulated mast cells produce and release adenosine, and the release of mast cell mediators is potentiated by adenosine, yet very little is known regarding mast cell purine metabolism. Because 5-amino-4-imidazolecarboxamide riboside (AICA riboside) has been shown to alter adenosine metabolism and accelerate the replet...

journal_title：Biochemical pharmacology

authors： Marquardt DL,Gruber HE

更新日期：1986-12-15 00:00:00

abstract：:The tissue distributions of debrisoquine 4-monooxygenase and bufuralol 1'-monooxygenase activities in microsomes from bovine and rabbit tissues were analysed. Debrisoquine 4-monooxygenase and bufuralol 1'-monooxygenase activities were found in liver, and at low levels in cerebral cortex, kidney cortex, lung, small int...

journal_title：Biochemical pharmacology

authors： Matsuo Y,Iwahashi K,Ichikawa Y

更新日期：1992-05-08 00:00:00

abstract：:Administration to hamsters of a highly purified human leukocyte interferon subtype, IFN-alpha A, obtained by recombinant DNA methods, abolished the efficacy of high doses of cyclophosphamide (2.5 mg/hamster) against the TBD 932 lymphosarcoma. The effect was more pronounced with concomitant than with sequential treatme...

journal_title：Biochemical pharmacology

authors： Lee SH,Chiu H,Renton KW,Stebbing N

更新日期：1984-11-01 00:00:00

abstract：:Treatment of immature 21-day-old female Sprague-Dawley rats with 17 beta-estradiol (E2) (0.5 microgram/rat) caused a significant increase in uterine wet weight, DNA synthesis, progesterone receptor (PR) binding, and peroxidase activity. At doses as high as 40 mg/rat, the bioflavonoid naringenin did not cause a signifi...

journal_title：Biochemical pharmacology

authors： Ruh MF,Zacharewski T,Connor K,Howell J,Chen I,Safe S

更新日期：1995-10-26 00:00:00

abstract：:The peripheral benzodiazepine receptor (PBR), an integral protein of the mitochondrial membrane, is involved in the formation of mitochondrial permeability transition (MPT) pores. The opening of the MPT-leading to the dissipation of the inner-mitochondrial transmembrane potential (deltapsi(m))-is considered to be an e...

journal_title：Biochemical pharmacology

authors： Strohmeier R,Roller M,Sänger N,Knecht R,Kuhl H

更新日期：2002-07-01 00:00:00

abstract：:In the present study, a novel synthetic compound 4-(2-(cyclohex-2-enylidene)hydrazinyl)quinolin-2(1H)-one (CYL-4d) was found to inhibit lipopolysaccharide (LPS)-induced nitric oxide (NO) production without affecting cell viability or enzyme activity of expressed inducible NO synthase (iNOS) in RAW 264.7 macrophages. C...

journal_title：Biochemical pharmacology

authors： Lin MW,Tsao LT,Chang LC,Chen YL,Huang LJ,Kuo SC,Tzeng CC,Lee MR,Wang JP

更新日期：2007-06-01 00:00:00

abstract：:Intracellular cyclic AMP accumulation following exposure to dopamine (DA) agonists and and antagonists was measured in striatal slices from rats with a unilateral 6-hydroxydopamine (6-OHDA) lesion of the nigrostriatal pathway and which showed contralateral circling to apomorphine. Both DA (10-320 microM) and the D-1 a...

journal_title：Biochemical pharmacology

authors： Thomas KL,Rose S,Jenner P,Marsden CD

更新日期：1992-07-07 00:00:00

abstract：:Bromodomains are epigenetic readers of histone acetylation involved in chromatin remodeling and transcriptional regulation. The human proteome comprises 46 bromodomain-containing proteins with a total of 61 bromodomains, which, despite highly conserved structural features, recognize a wide array of natural peptide lig...

journal_title：Biochemical pharmacology

authors： Ferri E,Petosa C,McKenna CE

更新日期：2016-04-15 00:00:00

abstract：:Adenosine (Ado, 10 microM) did not inhibit ADP-induced human platelet aggregation in whole blood. However, if the blood was preincubated with dipyridamole (10 microM), a potent inhibitor of the erythrocytic nucleoside transport system (NTS), Ado acted as a strong inhibitor of platelet aggregation. Similarly, Ado inhib...

journal_title：Biochemical pharmacology

authors： Dawicki DD,Agarwal KC,Parks RE Jr

更新日期：1985-11-15 00:00:00

abstract：:Thromboxane A2 is a potent mediator of inflammation and platelet aggregation exerting its effects through the activation of a G protein-coupled receptor (GPCR), termed TP. Although the existence of dimers/oligomers in Class A GPCRs is widely accepted, their functional significance still remains controversial. Recently...

journal_title：Biochemical pharmacology

authors： Capra V,Mauri M,Guzzi F,Busnelli M,Accomazzo MR,Gaussem P,Nisar SP,Mundell SJ,Parenti M,Rovati GE

更新日期：2017-01-15 00:00:00

abstract：:The possibility of NQ12 (2-chloro-3-[4-(ethylcarboxy)-phenyl]-amino-1,4-naphthoquinone) as a novel antithrombotic agent and its mode of action were investigated. The effects of NQ12 on platelet aggregation in human platelet-rich plasma in vitro, in rats ex vivo, and on murine pulmonary thrombosis in vivo, as well as t...

journal_title：Biochemical pharmacology

authors： Yuk DY,Ryu CK,Hong JT,Chung KH,Kang WS,Kim Y,Yoo HS,Lee MK,Lee CK,Yun YP

更新日期：2000-10-01 00:00:00

abstract：:It has been reported that endothelins (ETs) stimulate catecholamine release from chromaffin cells. However, it is not known whether ETs also affect catecholamine biosynthesis. Thus, using a rat pheochromocytoma cell line, PC12, we examined the effects of ETs on catecholamine biosynthesis. The mRNA level and activity o...

journal_title：Biochemical pharmacology

authors： Takekoshi K,Ishii K,Shibuya S,Kawakami Y,Isobe K,Nakai T

更新日期：2002-03-01 00:00:00

abstract：:Chondrosarcoma is a common primary malignant tumor of the bone that can metastasize through the vascular system to other organs. A key step in the metastatic process, lymphangiogenesis, involves vascular endothelial growth factor-C (VEGF-C). However, the effects of lymphangiogenesis in chondrosarcoma metastasis remain...

journal_title：Biochemical pharmacology

authors： Su CM,Tang CH,Chi MJ,Lin CY,Fong YC,Liu YC,Chen WC,Wang SW

更新日期：2018-08-01 00:00:00

abstract：:Ethyl 2[5(4-chlorophenyl)pentyl]oxirane-2-carboxylate (POCA) is strongly hypoglycaemic in fasted normal and diabetic rats [H. P. O. Wolf, K. Eistetter and G. Ludwig, Diabetologia 22, 456 (1982)]. POCA was fed for 12 weeks to rats on a standard low-fat (3%) diet at levels of 0.05% and 0.2% to give daily intakes of abou...

journal_title：Biochemical pharmacology

authors： Koundakjian PP,Turnbull DM,Bone AJ,Rogers MP,Younan SI,Sherratt HS

更新日期：1984-02-01 00:00:00

abstract：:Thrombospondin (TSP)-2, a matricellular glycoprotein of the TSP family, regulates multiple biological functions, including proliferation, angiogenesis, cell adhesion, and extracellular matrix (ECM) modeling. The clinical relevance of TSP-2 has been explored in many different cancers. TSP-2 expression levels vary betwe...

journal_title：Biochemical pharmacology

authors： Liu JF,Lee CW,Tsai MH,Tang CH,Chen PC,Lin LW,Lin CY,Lu CH,Lin YF,Yang SH,Chao CC

更新日期：2018-09-01 00:00:00

abstract：:The increasing incidence of severe liver diseases worldwide has resulted in a high demand for curative liver transplantation. Unfortunately, the need for transplants by far eclipses the availability of suitable grafts leaving many waitlisted patients to face liver failure and often death. Routine use of smaller grafts...

journal_title：Biochemical pharmacology

authors： Greenbaum LE,Ukomadu C,Tchorz JS

更新日期：2020-05-01 00:00:00

abstract：:A strain of hyperlipidaemic Sprague-Dawley (HSD) rat was compared with normal Sprague-Dawley (SD) rats for expression of cholesterol 7alpha-hydroxylase activity (CYP7A1) and other cytochrome P450 (P450) enzymes in liver. Hepatic microsomal CYP7A1 activity in male HSD rats was 2-3-fold lower than in male SD rats with C...

journal_title：Biochemical pharmacology

authors： Brassil PJ,Debri K,Nakura H,Kobayashi S,Davies DS,Edwards RJ

更新日期：1998-07-15 00:00:00

abstract：:Oridonin is a diterpene compound that regulates the activity of PPAR-γ (peroxisome proliferator-activated receptor gamma) transcription factor. Cumulative evidence indicates that AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid)-type glutamate receptors (AMPARs) play an important role in the treatment of de...

journal_title：Biochemical pharmacology

authors： Liu P,Du J

更新日期：2020-10-01 00:00:00

abstract：:Previously we reported that liposomal cisplatin (CDDP) overcomes CDDP resistance of ovarian A2780cis cancer cells (Krieger et al., Int. J. Pharm. 389, 2010, 10-17). Here we find that the cytotoxic activity of liposomal CDDP is not associated with detectable DNA platination in resistant ovarian cancer cells. This sugge...

journal_title：Biochemical pharmacology

authors： Koch M,Krieger ML,Stölting D,Brenner N,Beier M,Jaehde U,Wiese M,Royer HD,Bendas G

更新日期：2013-04-15 00:00:00

abstract：:Ca2+/calmodulin-dependent protein kinase II (CaMKII) plays an important role in the cardiovascular system. However, the potential protective role of inhibitor 1 of protein phosphatase 1 (I1PP1), which is able to regulate CaMKII, in high glucose-induced cardiomyocytes injury remains unknown. In the present study, cardi...

journal_title：Biochemical pharmacology

authors： Sun L,Chen Y,Luo H,Xu M,Meng G,Zhang W

更新日期：2019-05-01 00:00:00

abstract：:Dinucleotides of adenosine and thymidine in the ApnT series (n = 3,4,5 and 6) and their corresponding phosphonate analogues, where a methylene group replaces the oxygen between the alpha and beta phosphorus atoms adjacent to thymidine, have been evaluated as inhibitors of human leukaemic thymidylate kinase (dTMP kinas...

journal_title：Biochemical pharmacology

authors： Orr RM,Davies LC,Stock JA,Taylor GA,Powles RL,Harrap KR

更新日期：1988-02-15 00:00:00