The GABAA receptor-gated ion channel: biochemical and pharmacological studies of structure and function.

abstract：:Cyclic nucleotide phosphodiesterases (PDEs) are the only enzymes that inactivate intracellular cyclic AMP (cAMP). Because the functions of T-lymphocytes are modulated by cAMP levels, the isozymes of PDE in these cells are potential targets for new drugs designed to modify the body's immunity through selective alterati...

journal_title：Biochemical pharmacology

authors： Robicsek SA,Blanchard DK,Djeu JY,Krzanowski JJ,Szentivanyi A,Polson JB

更新日期：1991-07-25 00:00:00

abstract：:In order to study the metabolism of benzo[a]pyrene (BP), it must be dissolved in an organic solvent vehicle for delivery to the tissue. We studied the effects of five organic solvent vehicles, i.e. dimethyl sulfoxide (DMSO), acetone, methanol, ethanol, and ethyl acetate, on benzo[a]pyrene hydroxylase activity and the ...

journal_title：Biochemical pharmacology

authors： Kontir DM,Glance CA,Colby HD,Miles PR

更新日期：1986-08-01 00:00:00

abstract：:Pyrroloquinoline quinone (PQQ) is a novel redox cofactor recently found in human milk. It has been reported to function as an essential nutrient, antioxidant and redox modulator in cell culture experiments and in animal models of human diseases. As mitochondria are particularly susceptible to oxidative damage we studi...

journal_title：Biochemical pharmacology

authors： He K,Nukada H,Urakami T,Murphy MP

更新日期：2003-01-01 00:00:00

abstract：:Mitochondrial biogenesis is a key feature of energy expenditure and organismal energy balance. Genetic deletion of PARP1 or PARP2 was shown to induce mitochondrial biogenesis and energy expenditure. In line with that, PARP inhibitors were shown to induce energy expenditure in skeletal muscle. We aimed to investigate w...

journal_title：Biochemical pharmacology

authors： Nagy L,Rauch B,Balla N,Ujlaki G,Kis G,Abdul-Rahman O,Kristóf E,Sipos A,Antal M,Tóth A,Debreceni T,Horváth A,Maros T,Csizmadia P,Szerafin T,Bai P

更新日期：2019-09-01 00:00:00

abstract：:The beta 2-adrenoceptor agonist, clenbuterol (initially 5 mg/kg), was found to significantly reduce plasma tyrosine and raise brain tryptophan levels (P less than 0.01). By comparison, decreases in plasma tryptophan and increases in brain tyrosine were small and often nonsignificant. Amino acid levels measured in diff...

journal_title：Biochemical pharmacology

authors： Edwards DJ,Sorisio DA,Knopf S

更新日期：1989-09-15 00:00:00

abstract：:Oxidative damage of creatine kinase (CK) induced by Adriamycin((R)) (ADM) with peroxidase was investigated using horseradish peroxidase (HRP). ADM oxidatively inactivated CK during its interaction with HRP in the presence of H(2)O(2) (HRP-H(2)O(2)). The red color of ADM was lost during oxidation by HRP-H(2)O(2). Addin...

journal_title：Biochemical pharmacology

authors： Miura T,Muraoka S,Fujimoto Y

更新日期：2000-07-01 00:00:00

abstract：:Nitric oxide sensitive guanylyl cyclase (NOsGC) is a heterodimeric enzyme consisting of an α and a β subunit. Two heterodimeric enzymes are known to be important for NO-signalling in humans: α(1)/β(1) and α(2)/β(1). No difference had so far been detected with respect to their pharmacological properties, but as we show...

journal_title：Biochemical pharmacology

authors： Haase N,Haase T,Kraehling JR,Behrends S

更新日期：2010-12-01 00:00:00

abstract：:3H-(+/-) propranolol and 125I-(+/-) cyanopindolol have been used to characterize beta adrenoceptors of liver, lung, kidney and heart of rat. Two main binding parameters, KD and Bmax were measured using either cells, homogenates or plasma membranes of each organ (except heart). Results show that the most accurate deter...

journal_title：Biochemical pharmacology

authors： Zini R,Gault I,Ledewyn S,D'Athis P,Tillement JP

更新日期：1983-11-15 00:00:00

abstract：:Administration of pentylenetetrazol (PTZ) (60 mg/kg, s.c.) to normal or carbaryl (200 mg/kg, p.o.) treated adult male albino rats produced characteristic changes in the steady-state levels of striatal dopamine (DA), noradrenaline (NA) and homovanillic acid (HVA) at different time intervals (0.5, 1.0 and 2.0 hr). The e...

journal_title：Biochemical pharmacology

authors： Ray SK,Poddar MK

更新日期：1985-02-15 00:00:00

abstract：:The multidrug resistance (MDR) phenotype is the major cause of failure of cancer chemotherapy. This phenotype is mainly due to the overexpression of the human MDR1 (hMDR1) gene. Several studies have shown that transcriptional regulation of this gene is unexpectedly complex and is far from being completely understood. ...

journal_title：Biochemical pharmacology

authors： Labialle S,Gayet L,Marthinet E,Rigal D,Baggetto LG

更新日期：2002-09-01 00:00:00

abstract：:Reactive oxygen species (ROS) attack guanine bases in DNA and form 8-hydroxydeoxyguanosine (8-OHdG), which has been regarded simply as an oxidative mutagenic by-product. On the other hand, our previous report showed paradoxically ROS attenuating action of generated 8-OHdG. In the current study, both in vitro and in vi...

journal_title：Biochemical pharmacology

authors： Ock CY,Hong KS,Choi KS,Chung MH,Kim Ys,Kim JH,Hahm KB

更新日期：2011-01-01 00:00:00

abstract：:Oxidant damage from reactive oxygen species (ROS) and reactive nitrogen species (RNS) is a major contributor to the cellular damage seen in numerous types of renal injury. Resveratrol (trans-3,4',5-trihydroxystilbene) is a phytoalexin found naturally in many common food sources. The anti-oxidant properties of resverat...

journal_title：Biochemical pharmacology

authors： Holthoff JH,Woodling KA,Doerge DR,Burns ST,Hinson JA,Mayeux PR

更新日期：2010-10-15 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：:The development of the plasma cell tumor (PCT) model was the first widely accepted in vivo model of multiple myeloma (MM). Potter and colleagues used this chemically induced PCT model to study the pathophysiology of malignant plasma cells and also used it to screen anti-MM agents. Two decades later the C57BL/KaLwRij m...

journal_title：Biochemical pharmacology

authors： Sanchez E,Chen H,Berenson JR

更新日期：2014-06-01 00:00:00

abstract：:The structure and membrane interactions of lipophilic glucosyl phosphotriester derivatives of thymidine and 5-fluoro-deoxy thymidine are investigated by NMR spectroscopy. The self-association of these molecules, found in different solvents, presents a diastereoisomeric effect which is also observed in the transmembran...

journal_title：Biochemical pharmacology

authors： Debouzy JC,Hervé M,Neumann JM,Gouyette C,Dupraz B,Huynh-Dinh T

更新日期：1990-06-01 00:00:00

abstract：:Cocaine has been shown to be hepatotoxic in mice, rats and humans. N-Oxidative metabolism of cocaine is required for this effect, and it has been proposed that binding of cocaine reactive metabolites formed via this pathway might be responsible for cytotoxicity. To explore this hypothesis, cocaine-protein adducts in l...

journal_title：Biochemical pharmacology

authors： Ndikum-Moffor FM,Roberts SM

更新日期：2003-07-01 00:00:00

abstract：:We have previously shown [8] that rat liver adenosine kinase can produce [14C]AMP from [14C]adenosine (Ado) and unlabelled adenosine monophosphate (AMP), in the absence of ATP, by an exchange reaction. In this study, we investigated whether Ado or AMP could be replaced in this exchange reaction by other nucleosides or...

journal_title：Biochemical pharmacology

authors： Mimouni M,Bontemps F,Van den Berghe G

更新日期：1995-11-09 00:00:00

abstract：:The metabolism of tienilic acid, a drug containing a thiophene ring, was reinvestigated in man, rat and dog. The major urinary metabolite in man and rat was isolated and completely characterized by comparison with a synthetic compound. This metabolite derives from the hydroxylation of the thiophene ring of tienilic ac...

journal_title：Biochemical pharmacology

authors： Mansuy D,Dansette PM,Foures C,Jaouen M,Moinet G,Bayer N

更新日期：1984-05-01 00:00:00

abstract：:The role of nitric oxide (NO)/guanosine 3',5'-cyclic monophosphate (cGMP) signaling pathway in the regulation of fatty acid metabolism was investigated in rat hepatocytes. Treatment with NO donors, which are known to activate soluble guanylyl cyclase, inhibited in parallel fatty acid synthesis de novo and acetyl-CoA c...

journal_title：Biochemical pharmacology

authors： García-Villafranca J,Guillén A,Castro J

更新日期：2003-03-01 00:00:00

abstract：:The capacity of cultured bovine adrenal medullary cells to metabolize and export cyclic AMP has been studied. Basal cellular cyclic AMP levels were increased 50% by 100 microM 3-isobutyl-1-methylxanthine (IBMX) and rolipram, a class IV (cyclic AMP-specific) phosphodiesterase (PDE) inhibitor. They were not affected by ...

journal_title：Biochemical pharmacology

authors： Marley PD,Thomson KA

更新日期：1992-12-01 00:00:00

abstract：:Aldrin epoxidase, a cytochrome P-450-dependent monooxygenase, was studied in the lung and kidney of male rats. The sensitivity of the liver enzyme activity to different chemicals in vitro was influenced by the treatment of the animals with phenobarbital or methylcholanthrene. These results confirm that more than one f...

journal_title：Biochemical pharmacology

authors： Van Cantfort J,Léonard-Poma M,Sèle-Doyen J,Gielen JE

更新日期：1983-09-15 00:00:00

abstract：:Neuronal nicotinic acetylcholine receptors (nAChR), recognized targets for drug development in cognitive and neuro-degenerative disorders, are allosteric proteins with dynamic interconversions between multiple functional states. Activation of the nAChR ion channel is primarily controlled by the binding of ligands (ago...

journal_title：Biochemical pharmacology

authors： Williams DK,Wang J,Papke RL

更新日期：2011-10-15 00:00:00

abstract：:Dopamine can exist in both charged and uncharged forms at physiological pH. At present it is unclear which of these forms is responsible for dopaminergic agonist activity. The purpose of this study was to determine whether permanently charged structural analogs of dopamine containing either a nitrogen, sulfur, or sele...

journal_title：Biochemical pharmacology

authors： Wallace RA,Farooqui T,Wallace L,Ares J,Chang YA,Miller D,Uretsky N

更新日期：1987-11-15 00:00:00

abstract：:Antibiotic resistance issues necessitate the continued discovery and development of new antibacterial agents. Efforts are ongoing in two approaches to find new compounds that are effective against antibiotic-resistant pathogens. These efforts involve modification of existing classes including fluoroquinolones, tetracy...

journal_title：Biochemical pharmacology

authors： Bush K,Pucci MJ

更新日期：2011-12-01 00:00:00

abstract：:The tissue distribution of captopril, an antihypertensive drug possessing a free sulfhydryl group, and its sulfur-conjugated metabolites was studied in rats by gas chromatography-mass spectrometry at 15, 30 and 60 min following a single 10 mg/kg oral dose of captopril. It was found that tissue accumulation of captopri...

journal_title：Biochemical pharmacology

authors： Drummer OH,Worland PJ,Jarrott B

更新日期：1983-05-15 00:00:00

abstract：:4'-Deoxydoxorubicin (4'-deoxy) is a new adriamycin analogue with a similar spectrum of antitumour activity but is significantly more lipophilic than the parent compound. We report the kinetics and uptake of the two drugs by human non-small cell lung tumour cells in monolayer culture and the relationship between intrac...

journal_title：Biochemical pharmacology

authors： Kerr DJ,Kerr AM,Freshney RI,Kaye SB

更新日期：1986-08-15 00:00:00

abstract：:The ex vivo sensitivity of murine pluripotent hematopoietic stem cells (CFU-S) and myeloid progenitor cells (CFU-GM) to 4-hydroperoxycyclophosphamide, ASTA Z 7557, phosphoramide mustard, acrolein, melphalan, and cis-platinum was determined in the absence and presence of known (disulfiram, diethyldithiocarbamate, cyana...

journal_title：Biochemical pharmacology

authors： Kohn FR,Sladek NE

更新日期：1985-10-01 00:00:00

abstract：:Stress, be it from environmental factors or intrinsic to the cell as result of growth and metabolism, can be harmful to cells. Mammalian cells have developed numerous mechanisms to respond to diverse forms of stress. These mechanisms combine signaling cascades and activation of gene expression programs to orchestrate ...

journal_title：Biochemical pharmacology

authors： Aramburu J,Drews-Elger K,Estrada-Gelonch A,Minguillón J,Morancho B,Santiago V,López-Rodríguez C

更新日期：2006-11-30 00:00:00

abstract：:MRP1 overexpression in multidrug-resistant cancer cells has been shown to be responsible for collateral sensitivity to some flavonoids that stimulate a huge MRP1-mediated GSH efflux. This massive GSH depletion triggers the death of these cancer cells. We describe here that bivalent flavonoid dimers strikingly stimulat...

journal_title：Biochemical pharmacology

authors： Dury L,Nasr R,Lorendeau D,Comsa E,Wong I,Zhu X,Chan KF,Chan TH,Chow L,Falson P,Di Pietro A,Baubichon-Cortay H

更新日期：2017-01-15 00:00:00

abstract：:It has been suggested that vasoactive intestinal polypeptide (VIP) has a role as a neurotransmitter and that it participates in the control of hormone release from thyroid follicles. Many hormones and neurotransmitters alter the ionic permeability properties of the plasma membrane of their target cells when they bind ...

journal_title：Biochemical pharmacology

authors： Green ST

更新日期：1987-12-15 00:00:00