L-carnitine effect on halothane-treated mitochondria.

abstract：:Dravet syndrome (DS) is a catastrophic epileptic encephalopathy characterised by childhood-onset polymorphic seizures, multiple neuropsychiatric comorbidities, and increased risk of sudden death. Heterozygous loss-of-function mutations in one allele of SCN1A, the gene encoding the voltage-gated sodium channel 1.1 (NaV...

journal_title：Biochemical pharmacology

authors： Chow CY,Chin YKY,Ma L,Undheim EAB,Herzig V,King GF

更新日期：2020-11-01 00:00:00

abstract：:HOE 731, a substituted thienoimidazole derivative, was studied on [14C] aminopyrine uptake and oxygen consumption in isolated rabbit gastric glands. HOE 731 caused a concentration-dependent inhibition of [14C]aminopyrine uptake during histamine and dbcAMP stimulation. The inhibition during dbcAMP stimulation was in ac...

journal_title：Biochemical pharmacology

authors： Herling AW,Becht M,Lang HJ,Scheunemann KH,Weidmann K,Scholl T,Rippel R

更新日期：1990-10-15 00:00:00

abstract：:5-Substituted-2,2'-anhydrouridines are a new class of competitive inhibitors of uridine phosphorylase. The most potent member of the series is 2,2'-anhydro-5-ethyluridine with an apparent Ki value of 25 nM. These compounds are selective inhibitors of uridine phosphorylase and have no effect on thymidine phosphorylase....

journal_title：Biochemical pharmacology

authors： Veres Z,Szabolcs A,Szinai I,Dénes G,Kajtár-Peredy M,Otvös L

更新日期：1985-05-15 00:00:00

abstract：:Menadione (2-methyl-1,4-naphthoquinone) induces oxidative stress in cells causing perturbations in the cytoplasm as well as nicking of DNA. The mechanisms by which DNA damage occurs are still unclear, but a widely discussed issue is whether menadione-generated reactive oxygen species (ROS) directly damage DNA. In the ...

journal_title：Biochemical pharmacology

authors： Fischer-Nielsen A,Corcoran GB,Poulsen HE,Kamendulis LM,Loft S

更新日期：1995-05-17 00:00:00

abstract：:Blood platelets are central to haemostasis, and reactions in platelets involving sulfhydryl groups play important roles in platelet function. Reduced glutathione (GSH) plays an important role in platelet aggregation and glutathione-depleting chemicals inhibit platelet aggregation. The lipophilic drug disulfiram, becau...

journal_title：Biochemical pharmacology

authors： Rossi R,Giustarini D,Dalle-Donne I,Milzani A

更新日期：2006-08-28 00:00:00

abstract：:Administration of phenobarbital, a known inducer of glutathione S-transferase activity in rat liver, failed to stimulate sulfobromophthalein (BSP) conjugation by liver cytosol in hamsters. The latter displayed poor ability to conjugate this substrate, despite very high glutathione-conjugating activity with the broad-s...

journal_title：Biochemical pharmacology

authors： Foliot A,Touchard D,Myara A,Trivin F,Chauffert M

更新日期：1987-08-15 00:00:00

abstract：:Rats fed 1% paracetamol in the diet failed to grow and a dose-dependent inhibition of growth was observed and found to be independent of hepatoxicity. Addition of 0.5% D- or L-methionine, or L-cysteine to a diet containing 1% paracetamol restored growth. Addition of L-methionine to the drinking water was equally effec...

journal_title：Biochemical pharmacology

authors： McLean AE,Armstrong GR,Beales D

更新日期：1989-01-15 00:00:00

abstract：:Stimulation of hepatic glycogenolysis and vasoconstriction of the hepatic vasculature in response to acetyl glyceryl ether phosphocholine (AGEPC; platelet activating factor) was inhibited by two structural analogues of AGEPC, U66985 (1-O-octadecyl-2-O-acetyl-sn-glycero-3-phosphoric acid-6'-trimethyl ammonium hexyl est...

journal_title：Biochemical pharmacology

authors： Buxton DB,Hanahan DJ,Olson MS

更新日期：1986-03-15 00:00:00

abstract：:Sodium nitroprusside (SNP) stimulates cGMP formation to a greater extent in 20,000 g supernatant fractions of the human neuroblastoma clones NB1-G and SH-SY5Y than in the human astrocytoma clone D384. This suggests that these cell lines contain the soluble form of guanylate cyclase. Arachidonic, 8,11,14- and 11,14,17-...

journal_title：Biochemical pharmacology

authors： Vaughan PF,Ball SG

更新日期：1990-02-01 00:00:00

abstract：:Cytarabine (ara-C), a major antileukemic agent, is phosphorylated in the cell to cytarabine triphosphate (ara-CTP), which is then partly incorporated into DNA. The drug incorporation into DNA poisons the extending primer against further incorporation of deoxyribonucleotides including dCTP, ultimately inhibiting DNA sy...

journal_title：Biochemical pharmacology

authors： Yamauchi T,Ueda T

更新日期：2005-06-15 00:00:00

abstract：:Although it is known that the pathogenic mechanism of Helicobacter pylori involves the stimulated production of interleukin-8 (IL-8) as an inflammatory mediator, the details of the pathway remain unclear. The role of mitogen-activated protein kinase (MAPK) in IL-8 production by H. pylori has been examined in an in vit...

journal_title：Biochemical pharmacology

authors： Yamada H,Aihara T,Okabe S

更新日期：2001-06-15 00:00:00

abstract：:Homocysteine has been shown to increase glutathione levels in C3H/10T1/2 Cl 8 cells. The present paper confirms that this increase was specific for non-dividing cells. Several other thiols and disulfides, including cysteamine, mercaptoethanol and dithioerythritol, also increased glutathione, but the specificity for qu...

journal_title：Biochemical pharmacology

authors： Djurhuus R,Svardal AM,Ueland PM

更新日期：1990-02-01 00:00:00

abstract：:Glutathione reductase (GR) one of the enzymes of the glutathione redox cycle, plays a salient role in maintaining appropriate cellular levels of reduced glutathione. The enzyme in human red blood cells is inhibited in vitro by the anticonvulsant drug valproic acid (VPA). The inhibition is dose-dependent, reversible, u...

journal_title：Biochemical pharmacology

authors： Cotariu D,Evans S,Lahat E,Theitler J,Bistritzer T,Zaidman JL

更新日期：1992-02-04 00:00:00

abstract：:Structure-activity studies on a series of analogues of N-(3-methyl-S-(1-pyrrolidinyl carbonyl) butyl)-D-alanine ethyl ester hydrochloride (SC42619) have defined the features of this dipeptide analogue required for observation of thrombin receptor antagonist activity on the human platelet. The affinity for SC42619, and...

journal_title：Biochemical pharmacology

authors： Ruda EM,Scrutton MC,Manley PW,Tuffin DP

更新日期：1990-01-15 00:00:00

abstract：:Brain penetration of drugs which are subject to P-glycoprotein (Pgp)-mediated efflux is attenuated, as manifested by the fact that the cerebrospinal fluid concentration (C(CSF)), a good surrogate of the unbound brain concentration (C(ub)), is lower than the unbound plasma concentration (C(up)) for Pgp substrates. In r...

journal_title：Biochemical pharmacology

authors： Tang C,Kuo Y,Pudvah NT,Ellis JD,Michener MS,Egbertson M,Graham SL,Cook JJ,Hochman JH,Prueksaritanont T

更新日期：2009-09-15 00:00:00

abstract：:We have previously shown that structural modification of chlorpromazine to introduce a basic side chain converts this chloroquine (CQ) resistance-reversing agent into a compound that has activity against Plasmodium falciparum in vitro. In an effort to further dissect the structural features that determine quinoline an...

journal_title：Biochemical pharmacology

authors： Kalkanidis M,Klonis N,Tschan S,Deady LW,Tilley L

更新日期：2004-04-01 00:00:00

abstract：:The effects of thiamine thiazolone (TT) and thiamine thiazolone pyrophosphate (TTPP) on the in vitro and in vivo inhibition of pyruvate dehydrogenase complex (PDHC) from rat cortex and hippocampus were characterized. TTPP decreased PDHC activity in vitro but had no effect in vivo following its direct chronic administr...

journal_title：Biochemical pharmacology

authors： Kandiko CT,Smith D,Yamamoto BK

更新日期：1988-11-15 00:00:00

abstract：:Rational approaches to targeted cancer therapy have begun to predominate the pipelines of oncology drug development. Our rapidly increasing understanding of the "wiring" of tumor cells and the vulnerabilities of such cells that can potentially be exploited through targeted treatments has opened up enormous opportuniti...

journal_title：Biochemical pharmacology

authors： Sharma SV,Settleman J

更新日期：2010-09-01 00:00:00

abstract：:In congenital jaundice, which is due to defects of bilirubin gluruconidation, bilirubin is degraded by an alternative pathway into unidentified products. Previously, it was shown that plasma bilirubin levels can be decreased in rats with this defect by inducers of CYP1A enzymes. Here, liver microsomes from rats or mic...

journal_title：Biochemical pharmacology

authors： Zaccaro C,Sweitzer S,Pipino S,Gorman N,Sinclair PR,Sinclair JF,Nebert DW,De Matteis F

更新日期：2001-04-01 00:00:00

abstract：:Doxorubicin is shown to be present in albumin microspheres (10-40 microns) in two forms: the native drug and a fraction of drug covalently coupled to the protein matrix probably via glutaraldehyde. Upon trypsin digestion the fraction covalently coupled is released and can be resolved from native doxorubicin by high pe...

journal_title：Biochemical pharmacology

authors： Cummings J,Willmott N,Marley E,Smyth J

更新日期：1991-06-15 00:00:00

abstract：:Previous work has shown that 5-hydroxytryptamine (5-HT)2A receptors can be radiolabelled with various radioligands, including partial agonists, such as [125I]-DOI and [3H]-DOB, and antagonists, such as [3H]-ketanserin and [3H]-spiperone. Because 5-HT has high affinity for the 5-HT2A receptor when displacing [3H]-DOB, ...

journal_title：Biochemical pharmacology

authors： Sleight AJ,Stam NJ,Mutel V,Vanderheyden PM

更新日期：1996-01-12 00:00:00

abstract：:The proinflammatory cytokine interleukin (IL)-18 appears to be involved in the pathogenesis of diseases associated with immunoactivation and inflammation. Consequently, blockage of IL-18 bioactivity by use of IL-18 binding protein (IL-18 BP) is likely a promising therapeutic concept. In the present study, we investiga...

journal_title：Biochemical pharmacology

authors： Nold M,Hauser IA,Höfler S,Goede A,Eberhardt W,Ditting T,Geiger H,Pfeilschifter J,Mühl H

更新日期：2003-08-01 00:00:00

abstract：:Major antidepressant agents increase synaptic levels of monoamines. Although the monoamine hypothesis of depression remains a cornerstone of our understanding of the pathophysiology of depression, emerging data has suggested that the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor subtype of g...

journal_title：Biochemical pharmacology

authors： Alt A,Nisenbaum ES,Bleakman D,Witkin JM

更新日期：2006-04-28 00:00:00

abstract：:In this study we analyse the effects of the anti-tumor compound distamycin on the binding of nuclear factor(s) to a synthetic oligonucleotide (GTATA/IFN-gamma) mimicking a putative regulatory region of the human HLA-DR alpha gene. This region contains the sequence (GTATA), that is required for nuclear protein binding ...

journal_title：Biochemical pharmacology

authors： Gambari R,Barbieri R,Nastruzzi C,Chiorboli V,Feriotto G,Natali PG,Giacomini P,Arcamone F

更新日期：1991-02-15 00:00:00

abstract：:The genetically controlled polymorphic oxidation of debrisoquine and sparteine is caused by the absence or functional deficiency of a cytochrome P-450 isozyme. In order to elucidate the mechanisms underlying the differences in cytochrome P-450 function we have studied the 1'-hydroxylation of the prototype drug bufural...

journal_title：Biochemical pharmacology

authors： Dayer P,Kronbach T,Eichelbaum M,Meyer UA

更新日期：1987-12-01 00:00:00

abstract：:N-Nitrosoguanidines are potential carcinogens. However, the toxicity of these agents is attenuated significantly in laboratory rodents by processes that remove the nitroso group to generate the relatively innocuous parent guanidinium compound. The denitrosation of 1,3-dimethyl-2-cyano-1-nitrosoguanidine (CyanoDMNG) me...

journal_title：Biochemical pharmacology

authors： Jensen DE,Belka GK,Dworkin C

更新日期：1997-05-09 00:00:00

abstract：:Toll-like receptors (TLRs) are key components of the innate immune system, functioning as pattern recognition receptors that recognise a wide range of microbial pathogens. TLRs represent a primary line of defence against invading pathogens in mammals, plants and insects. Recognition of microbial components by TLRs tri...

journal_title：Biochemical pharmacology

authors： Doyle SL,O'Neill LA

更新日期：2006-10-30 00:00:00

abstract：:Phentermine was shown in the 1970s to inhibit the metabolism of serotonin by monoamine oxidase (MAO), but never was labeled as an MAO inhibitor; hence, it was widely used in combination with fenfluramine, and continues to be used, in violation of their labels, with other serotonin uptake blockers. We examined the effe...

journal_title：Biochemical pharmacology

authors： Ulus IH,Maher TJ,Wurtman RJ

更新日期：2000-06-15 00:00:00

abstract：:Polyphenolic anthocyanins are major colorful compounds in red fruits, known to prevent cardiovascular and other diseases. Grape polyphenols are a mixture of various molecules and their exact contribution to above bioactivities remains to be clarified. In the present study, we first analyzed the effect of purified grap...

journal_title：Biochemical pharmacology

authors： Decendit A,Mamani-Matsuda M,Aumont V,Waffo-Teguo P,Moynet D,Boniface K,Richard E,Krisa S,Rambert J,Mérillon JM,Mossalayi MD

更新日期：2013-11-15 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