Inhibition of pyruvate oxidation in rat islets by alpha-cyano-4-hydroxycinnamate. Differential effects on insulin secretion and inositol lipid metabolism.

abstract：:Metastatic migration of murine L1210 leukemia cells, sensitive and resistant to the antitumor agent L-phenylalanine mustard, from the peritoneal cavity of mice to the liver resulted in a 2-fold elevation in their GSH content. This increase in GSH was accompanied by a corresponding increase in their resistance to the d...

journal_title：Biochemical pharmacology

authors： Ahmad S,Mulberg A,Aljian J,Vistica DT

更新日期：1986-05-15 00:00:00

abstract：:It has been reported that nonsteroidal anti-inflammatory drugs (NSAIDs) suppress bone repair and bone remodeling but only mildly inhibit bone mineralization at the earlier stage of the repair process. We proposed that the proliferation and/or the earlier stage of differentiation of osteoblasts may be affected by NSAID...

journal_title：Biochemical pharmacology

authors： Ho ML,Chang JK,Chuang LY,Hsu HK,Wang GJ

更新日期：1999-09-15 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：:Studies were carried out using a tetraphenylphosphonium (TPP+)-selective electrode to monitor the effect of selected calcium (Ca2+) antagonists and the dihydropyridine Ca2+ agonist Bay K8644 on membrane potential (psi) associated with isolated rat heart mitochondria. Verapamil and diltiazem (10-500 microM), standard C...

journal_title：Biochemical pharmacology

authors： Fox RM,Morgan RM,Markham A

更新日期：1993-05-25 00:00:00

abstract：:The N-type voltage-gated calcium channel (Ca(v)2.2) functions in neurons to regulate neurotransmitter release. It comprises a clinically relevant target for chronic pain. We have validated a calcium mobilization approach to assessing Ca(v)2.2 pharmacology in two stable Ca(v)2.2 cell lines: alpha1(B), alpha2delta, beta...

journal_title：Biochemical pharmacology

authors： Benjamin ER,Pruthi F,Olanrewaju S,Shan S,Hanway D,Liu X,Cerne R,Lavery D,Valenzano KJ,Woodward RM,Ilyin VI

更新日期：2006-09-14 00:00:00

abstract：:In the present work we set out to apply pharmacodynamic concepts derived from dose-response curves (Potency and Efficacy) to characterize the gene transfer efficiency of a vector:DNA complex. We employed two widely used vectors, the cationic lipid DOTAP (N,N, N-trimethyl 1-2-3-bis (1-oxo-9-octa-decenyl)oxy-(Z, Z)-1-pr...

journal_title：Biochemical pharmacology

authors： Aliño SF,Escrig E,Revert F,Guillem VM,Crespo A

更新日期：2000-12-15 00:00:00

abstract：:The formation of triacylglycerols containing fenoprofen was studied in rat isolated adipocytes and hepatocytes incubated with [3H]glycerol and R or S fenoprofen. In both hepatocytes and adipocytes there was a high-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen which was stereospe...

journal_title：Biochemical pharmacology

authors： Sallustio BC,Meffin PJ,Knights KM

更新日期：1988-05-15 00:00:00

abstract：:To determine if both the Ca2+-calmodulin system and the cyclic AMP system may regulate tyrosine hydroxylase (TH) activity in situ, rat striatal tissue slices that contain all of the components of the TH, cyclic AMP and Ca2+-calmodulin systems were subjected to experimental manipulations. Incubation of striatal tissue ...

journal_title：Biochemical pharmacology

authors： Hirata Y,Nagatsu T

更新日期：1985-08-01 00:00:00

abstract：:The oxidative metabolism of more than 20 drugs (e.g. sparteine, debrisoquine, dextromethorphan) is mediated by cytochrome P450IID6. Codeine O-demethylation to morphine was recently demonstrated to co-segregate with the polymorphic metabolism of debrisoquine and dextromethorphan. The female Dark-Agouti rat (DA) is an a...

journal_title：Biochemical pharmacology

authors： Mikus G,Somogyi AA,Bochner F,Eichelbaum M

更新日期：1991-03-01 00:00:00

abstract：:α6β2-Containing nicotinic acetylcholine receptors (α6β2* nAChRs) are predominantly expressed in midbrain dopaminergic neurons, including substantia nigra pars compacta (SNc) neurons and their projections to striatal regions, where they regulate dopamine release and nigrostriatal activity. It is well established that n...

journal_title：Biochemical pharmacology

authors： van Hout M,Klein J,Ahring PK,Brown DT,Thaneshwaran S,Dos Santos AB,Jensen AA,Kohlmeier KA,Christophersen P,Dyhring T

更新日期：2020-04-01 00:00:00

abstract：:Diethyl esters of the glutathione S-conjugate S-p-bromobenzylglutathione, an inhibitor of glyoxalase I, and S-p-nitrobenzoxycarbonylglutathione, an inhibitor of glyoxalase II, induced growth arrest and toxicity in human leukaemia 60 cells in culture. The median growth inhibitory concentration IC50 values were 8.3 micr...

journal_title：Biochemical pharmacology

authors： Lo TW,Thornalley PJ

更新日期：1992-12-15 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are now understood to fall into one of two agent classes in clinical use. Traditional NSAIDs inhibit both cyclooxygenases-1 and 2 (COX-1, 2), which act as key enzymes catalyzing the same reaction in the production of prostaglandins (PGs), while the second class of NSAIDs s...

journal_title：Biochemical pharmacology

authors： Imanishi J,Morita Y,Yoshimi E,Kuroda K,Masunaga T,Yamagami K,Kuno M,Hamachi E,Aoki S,Takahashi F,Nakamura K,Miyata S,Ohkubo Y,Mutoh S

更新日期：2011-10-01 00:00:00

abstract：:The dithiol-reducing thioredoxin/thioredoxin reductase system normally maintains the reduced state of key enzymes responsible for the cell's anti-oxidant defences. We therefore addressed the question of whether AW 464--a novel thioredoxin inhibitor--as well as broad spectrum dithiol ligands diamide and phenylarsine ox...

journal_title：Biochemical pharmacology

authors： Pallis M,Bradshaw TD,Westwell AD,Grundy M,Stevens MF,Russell N

更新日期：2003-11-01 00:00:00

abstract：:Aldehyde dehydrogenase (ALDH) is well known for its involvement in the resistance of tumor cells to cyclophosphamide (CPA) and its activated derivatives, such as 4-hydroperoxy-CPA (4HC). The role of other drug-metabolizing enzymes such as glutathione S-transferase (GST) in CPA resistance is, however, less certain. In ...

journal_title：Biochemical pharmacology

authors： Chen G,Waxman DJ

更新日期：1995-05-26 00:00:00

abstract：:SAD-128 was found to be an effective protector of acetylcholinesterase against inhibition by soman, due to its ability to function as a reversible inhibitor and allosteric modifier of the AChE active site. It also attenuated aging of the soman-inhibited enzyme. In order to study the connection between some of these ef...

journal_title：Biochemical pharmacology

authors： Stalc A,Sentjurc M

更新日期：1990-12-01 00:00:00

abstract：:The 20-epi-vitamin D3 analogues are a novel class of vitamin D3 derivatives, structurally related to 1 alpha,25-dihydroxycholecalciferol (1 alpha,25(OH)2D3). They are characterized by an altered stereochemistry at carbon 20 in the side-chain. In vitro, these new analogues were found to be considerably more potent as r...

journal_title：Biochemical pharmacology

authors： Binderup L,Latini S,Binderup E,Bretting C,Calverley M,Hansen K

更新日期：1991-09-27 00:00:00

abstract：:Chronic inflammation has been implicated as the underlying factor in the pathogenesis of many disorders. In the past decade, inflammation-related endogenous production of reactive nitrogen species, similar to oxygen free radicals, has also been suggested as a risk factor for cancer, in addition to the well-studied exo...

journal_title：Biochemical pharmacology

authors： Chan MM,Fong D,Ho CT,Huang HI

更新日期：1997-12-15 00:00:00

abstract：:Anandamide and 2-arachidonoylglycerol (2-AG) are two endogenous ligands for the cannabinoid receptors, and their cannabimimetic activities are lost when they are hydrolyzed enzymatically. Cytosol and particulate fractions of porcine brain exhibited a high 2-AG hydrolyzing activity of 100 nmol/min/mg protein. Most of t...

journal_title：Biochemical pharmacology

authors： Goparaju SK,Ueda N,Taniguchi K,Yamamoto S

更新日期：1999-02-15 00:00:00

abstract：:We report here studies on the regulation of the metabolism of adenosine 3',5'-monophosphate (cAMP) in established and primary cultures of rat pulmonary microvascular endothelial cells (RPMVEC). Inhibition by rolipram, a selective inhibitor of cAMP phosphodiesterase (PDE) of the PDE4 gene family, was required to achiev...

journal_title：Biochemical pharmacology

authors： Thompson WJ,Ashikaga T,Kelly JJ,Liu L,Zhu B,Vemavarapu L,Strada SJ

更新日期：2002-02-15 00:00:00

abstract：:The glycolipid alpha-galactosylceramide (alpha-GalCer), when presented on CD1 molecules by antigen presenting cells (APCs) to invariant NKT (iNKT cells), is a potent immunomodulator. Indoleamine 2,3-dioxygenase (IDO), an enzyme catalyzing the catabolism of L-tryptophan along the kynurenine pathway, is inducible in APC...

journal_title：Biochemical pharmacology

authors： Fallarini S,Paoletti T,Panza L,Lombardi G

更新日期：2008-09-15 00:00:00

abstract：:Alzheimer disease (AD) is a progressive neurodegenerative disorder characterized by severe cognitive impairment, inability to perform activities of daily living and mood changes. Statins, long known to be beneficial in conditions where dyslipidemia occurs by lowering serum cholesterol levels, also have been proposed f...

journal_title：Biochemical pharmacology

authors： Barone E,Di Domenico F,Butterfield DA

更新日期：2014-04-15 00:00:00

abstract：:To investigate the potential interactions between the angiotensin II (Ang II) and insulin signaling systems, regulation of IRS-1 phosphorylation and insulin-induced Akt activation by Ang II were examined in clone 9 (C9) hepatocytes. In these cells, Ang II specifically inhibited activation of insulin-induced Akt Thr(30...

journal_title：Biochemical pharmacology

authors： Arellano-Plancarte A,Hernandez-Aranda J,Catt KJ,Olivares-Reyes JA

更新日期：2010-03-01 00:00:00

abstract：:5-Fluorouracil (FUra) has been administered to mice bearing xenografts of human colon adenocarcinomas. In two tumor lines, HxGC3 and HxVRC5, intrinsically resistant to FUra, 2'-deoxyuridylate (dUMP) accumulated 13.4- and 23.9-fold above basal levels. In HxELC2 xenografts, which demonstrated some sensitivity to FUra, t...

journal_title：Biochemical pharmacology

authors： Houghton JA,Weiss KD,Williams LG,Torrance PM,Houghton PJ

更新日期：1986-04-15 00:00:00

abstract：:The effects of two new phthalazinone derivatives, azelastine (AZ) and flezelastine (FZ), on the reversal of resistance to doxorubicin (dox) were studied using two variants of the rat C6 glioblastoma cell line, selected with dox (C6 0.5) or with vincristine (C6 1V). Both lines presented a multidrug-resistant phenotype ...

journal_title：Biochemical pharmacology

authors： Hu YP,Robert J

更新日期：1995-07-17 00:00:00

abstract：:We reported previously that the flavoprotein inhibitor diphenyleneiodonium sulfate (DPI) irreversibly inhibited the metabolic activation of glyceryl trinitrate (GTN) in isolated aorta, possibly through inhibition of vascular NADPH-cytochrome P450 reductase (CPR). We report that the content of CPR represents 0.03 to 0....

journal_title：Biochemical pharmacology

authors： McGuire JJ,Anderson DJ,McDonald BJ,Narayanasami R,Bennett BM

更新日期：1998-10-01 00:00:00

abstract：:The specific binding of three cardiac glycosides, 3H-ouabain, 3H-digitoxin and 3H-dihydrodigitoxin, to beef cardiac (Na+ + K+)-ATPase was compared. Non-specific binding was defined as that in the presence of 0.1 mM unlabelled compound, or in the absence of ligands. The dissociation constants (KD-values) calculated fro...

journal_title：Biochemical pharmacology

authors： Brown L,Erdmann E

更新日期：1983-11-01 00:00:00

abstract：:Griseofulvin is an anti-fungal drug whose mechanism of action is directed against microtubules. Although it inhibits the assembly of mammalian brain tubulin, its binding to tubulin has not been directly measured successfully. We have examined the interaction of griseofulvin with tubulin fluorometrically by measuring t...

journal_title：Biochemical pharmacology

authors： Chaudhuri AR,Ludueña RF

更新日期：1996-04-12 00:00:00

abstract：:The effect of loxoprofen-Na, a novel non-steroidal anti-inflammatory drug with a prodrug property, on prostaglandin (PG) levels in the inflammatory tissue was investigated with a carrageenin-induced pleurisy model in rats. The intrapleural injection of carrageenin caused a marked increase in the levels of PGE2 and 6-k...

journal_title：Biochemical pharmacology

authors： Sugimoto M,Kojima T,Asami M,Iizuka Y,Matsuda K

更新日期：1991-11-27 00:00:00

abstract：:The inductive effects of phenobarbitone (PB) and 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene (TCPOBOP) were compared in C57BL/6J mice. Induction parameters included six substrates: ethylmorphine (EM), benzphetamine (Bph), biphenyl, ethoxycoumarin (EtoC), pentoxyresorufin and dichloro-p-nitroanisole (DPNA). In order to ...

journal_title：Biochemical pharmacology

authors： Heubel F,Reuter T,Gerstner E

更新日期：1989-04-15 00:00:00

abstract：:Cardiorenal syndrome type-3 (CRS-3) is characterized by acute cardiac injury induced by acute kidney injury. Here, we investigated the causes of CRS-3 by analyzing cardiac function after renal ischemia-reperfusion injury (IRI) using echocardiography and evaluation of pro-inflammatory markers, calcium balance, mitochon...

journal_title：Biochemical pharmacology

authors： Wang J,Toan S,Li R,Zhou H

更新日期：2020-04-01 00:00:00