Initiation of in vitro lipid peroxidation by N-hydroxynorcocaine and norcocaine nitroxide.

abstract：:Benzbromarone (BBR), a potent uricosuric agent for the management of gout, is known to cause fatal fulminant hepatitis. While the mechanism of BBR-induced idiosyncratic hepatotoxicity remains unelucidated, cytochrome P450 enzyme (CYP450)-mediated bioactivation of BBR to electrophilic reactive metabolites is commonly r...

journal_title：Molecular pharmacology

authors： Tang LWT,Verma RK,Fan H,Chan ECY

更新日期：2021-01-12 00:00:00

abstract：:Recently, inositol hexakisphosphate (phytic acid) was shown to bind to photoreceptor arrestin and block its interaction with rhodopsin. Such an interaction might predict that inositol polyphosphates could alter G protein-coupled receptor desensitization. To investigate the possible roles of higher inositol polyphospha...

journal_title：Molecular pharmacology

authors： Sasakawa N,Ferguson JE,Sharif M,Hanley MR

更新日期：1994-08-01 00:00:00

abstract：:Corticotropin-releasing factor (CRF) receptors encoded by two distinct genes have recently been identified and termed CRF1 and CRF2. CRF and the non-mammalian-related peptide sauvagine bind to and activate CRF1 receptors with high affinity and equal potency. Although CRF is significantly weaker at the CRF2 receptor, s...

journal_title：Molecular pharmacology

authors： Grigoriadis DE,Liu XJ,Vaughn J,Palmer SF,True CD,Vale WW,Ling N,De Souza EB

更新日期：1996-09-01 00:00:00

abstract：:We reported previously the formation of a glutathionyl conjugate of the active metabolite (AM) of clopidogrel and the covalent modification of a cysteinyl residue of human cytochrome P450 2B6 in a reconstituted system (Mol Pharmacol 80:839-847, 2011). In this work, we extended our studies of the metabolism of clopidog...

journal_title：Molecular pharmacology

authors： Zhang H,Lau WC,Hollenberg PF

更新日期：2012-08-01 00:00:00

abstract：:C57BL/6J (C57) and DBA/JBOMf (DBA) mice were used to study the role of adipose tissue as a modifier of tissue distribution, biological effects, and elimination of a lipophilic foreign chemical, 2,4,5,2',4',5'-hexachlorobiphenyl (HCB). As an indication of biological potency of the model compound, the activities of hepa...

journal_title：Molecular pharmacology

authors： Ahotupa M,Mäntylä E

更新日期：1983-11-01 00:00:00

abstract：:We cloned and expressed a human metabotropic glutamate receptor 1 alpha (HmGluR1 alpha) in a novel cell line. The human mGluR1 alpha cDNA was found to be 86% identical to rat mGluR1 alpha, and the predicted protein sequence was found to be 93% identical to rat mGluR1 alpha. We expressed HmGluR1 alpha in AV12-664, an a...

journal_title：Molecular pharmacology

authors： Desai MA,Burnett JP,Mayne NG,Schoepp DD

更新日期：1995-10-01 00:00:00

abstract：:The successful synthesis of dolastatin 11, a depsipeptide originally isolated from the mollusk Dolabella auricularia, permitted us to study its effects on cells. The compound arrested cells at cytokinesis by causing a rapid and massive rearrangement of the cellular actin filament network. In a dose-and time-dependent ...

journal_title：Molecular pharmacology

authors： Bai R,Verdier-Pinard P,Gangwar S,Stessman CC,McClure KJ,Sausville EA,Pettit GR,Bates RB,Hamel E

更新日期：2001-03-01 00:00:00

abstract：:The irreversible proteolytic nature of protease-activated receptor-2 (PAR2) activation suggests that mechanism(s) responsible for termination of receptor signaling are critical determinants of the magnitude and duration of PAR2-elicited cellular responses. Rapid desensitization of activated G-protein-coupled receptors...

journal_title：Molecular pharmacology

authors： Stalheim L,Ding Y,Gullapalli A,Paing MM,Wolfe BL,Morris DR,Trejo J

更新日期：2005-01-01 00:00:00

abstract：:An 'epoxygenase' eicosanoid analog, 14, 15-cis-episulfide-eicosatrienoic acid, has several unique pharmacological effects on platelets. These include (i) inhibition of ionophore A23187- but not thrombin-induced activation, (ii) inhibition of thromboxane B2 biosynthesis derived from endogenous but not exogenous arachid...

journal_title：Molecular pharmacology

authors： Bernstrom K,Malcolm K,McGee J,Maclouf J,Levy-Toledano S,Falck JR,Fitzpatrick FA

更新日期：1991-02-01 00:00:00

abstract：:Resveratrol (RES), a natural plant polyphenol, has gained interest as a nontoxic chemopreventive agent capable of inducing tumor cell death in a variety of cancer types. However, the early molecular mechanisms of RES-induced apoptosis are not well defined. Using the human breast cancer cell lines MDA-MB-231 and MCF-7,...

journal_title：Molecular pharmacology

authors： Sareen D,Darjatmoko SR,Albert DM,Polans AS

更新日期：2007-12-01 00:00:00

abstract：:α-Conotoxins are subtype-selective nicotinic acetylcholine receptor (nAChR) antagonists. Although potent α3β2 nAChR-selective α-conotoxins have been identified, currently characterized α-conotoxins show no or only weak affinity for α4β2 nAChRs, which are, besides α7 receptors, the most abundant nAChRs in the mammalian...

journal_title：Molecular pharmacology

authors： Beissner M,Dutertre S,Schemm R,Danker T,Sporning A,Grubmüller H,Nicke A

更新日期：2012-10-01 00:00:00

abstract：:The epithelial sodium channel (ENaC) is believed to represent the rate-limiting step for sodium absorption in the renal collecting duct. Consequently, ENaC is a central effector affecting systemic blood volume and pressure. Sodium and water transport are dysregulated in diabetes mellitus. Peroxisome proliferator-activ...

journal_title：Molecular pharmacology

authors： Pavlov TS,Levchenko V,Karpushev AV,Vandewalle A,Staruschenko A

更新日期：2009-12-01 00:00:00

abstract：:A methylcholanthrene-induced rat sarcoma that can be propagated in vitro or in vivo was evaluated for resistance to antifolates and was found to be relatively resistant to methotrexate and 10-ethyl-10-deazaaminopterin but sensitive to trimetrexate. Rat sarcoma cell extracts contained low levels of dihydrofolate reduct...

journal_title：Molecular pharmacology

authors： Li WW,Lin JT,Schweitzer BI,Bertino JR

更新日期：1991-11-01 00:00:00

abstract：:Glutamatergic synaptic transmitters are cleared from the synaptic cleft through excitatory amino acid transporters (EAATs) that are responsible for recycling glutamate and transporting it into neurons and glial cells. To probe the structural role of the TM4b-4c loop of EAAT1 (Rattus norvegicus), each of the 57 amino a...

journal_title：Molecular pharmacology

authors： Zhang W,Zhang X,Qu S

更新日期：2018-07-01 00:00:00

abstract：:The fluorogenic sulfhydryl probe 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin (CPM) (1-50 nM) is used to characterize the functional role and location of highly reactive thiol groups on the ryanodine-sensitive Ca2+ release channel complex [i.e., ryanodine receptors (RyRs)] of skeletal and cardiac junctional...

journal_title：Molecular pharmacology

authors： Liu G,Abramson JJ,Zable AC,Pessah IN

更新日期：1994-02-01 00:00:00

abstract：:There is no approved means to prevent the toxic actions of cocaine. Cocaine esterase (CocE) is found in a rhodococcal strain of bacteria that grows in the rhizosphere soil around the coca plant and has been found to hydrolyze cocaine in vitro. The esteratic activity of CocE (0.1-1.0 mg, i.v.) was characterized and con...

journal_title：Molecular pharmacology

authors： Cooper ZD,Narasimhan D,Sunahara RK,Mierzejewski P,Jutkiewicz EM,Larsen NA,Wilson IA,Landry DW,Woods JH

更新日期：2006-12-01 00:00:00

abstract：:The anti-human immunodeficiency virus (-HIV) nucleoside analogs azidothymidine (AZT), dideoxycytidine (ddC), dideoxyinosine (ddl), dideoxydidehydrothymidine (D4T), and dideoxydidehydrocytidine (D4C) and the anticancer drug cytosine arabinoside (AraC) were compared for their effects on the mitochondrial DNA (mtDNA) con...

journal_title：Molecular pharmacology

authors： Chen CH,Vazquez-Padua M,Cheng YC

更新日期：1991-05-01 00:00:00

abstract：:Combining chemotherapeutics to treat malignant tumors has been shown to be effective in preventing drug resistance, tumor recurrence, and reducing tumor size. We modeled combination drug therapy in PC-3 human prostate cancer cells using mixture design response surface methodology (MDRSM), a statistical technique desig...

journal_title：Molecular pharmacology

authors： Oblad R,Doughty H,Lawson J,Christensen M,Kenealey J

更新日期：2018-08-01 00:00:00

abstract：:The nicotinic acetylcholine receptor can be expressed in Xenopus oocytes by injection of in vitro synthesized RNA for the alpha, beta, gamma, and delta mouse muscle subunits. However, detectable responses can also be obtained by injection of alpha, beta, and delta subunit RNA only. The receptors expressed in this case...

journal_title：Molecular pharmacology

authors： Charnet P,Labarca C,Lester HA

更新日期：1992-04-01 00:00:00

abstract：:Signaling by the insulin-like growth factor (IGF)-1 receptor (IGF-1R) has been implicated in the promotion and aggressiveness of breast, prostate, colorectal, and lung cancers. The IGF binding proteins (IGFBPs) represent a class of natural IGF antagonists that bind to and sequester IGF-1/2 from the IGF-1R, making them...

journal_title：Molecular pharmacology

authors： Kibbey MM,Jameson MJ,Eaton EM,Rosenzweig SA

更新日期：2006-03-01 00:00:00

abstract：:Reversible binding of warfarin to defatted serum albumin was studied by equilibrium dialysis at pH 7.4, in a 66 mM sodium phosphate buffer at 37 degrees. The binding isotherm could be described by two stoichiometric binding constants, K1 in the range 141,000 to 192,000 M-1 and K2 at 39,000 to 57,000 M-1. At least two ...

journal_title：Molecular pharmacology

authors： Larsen FG,Larsen CG,Jakobsen P,Brodersen R

更新日期：1985-02-01 00:00:00

abstract：:The ligand specificity of rat adenohypophyseal vasopressin receptors was directly compared to that of peripheral receptors of the V1 and V2 types. For this purpose a series of 15 recently designed vasopressin antagonists was used. The affinities of these antagonists for rat adenohypophyseal membranes were deduced from...

journal_title：Molecular pharmacology

authors： Jard S,Gaillard RC,Guillon G,Marie J,Schoenenberg P,Muller AF,Manning M,Sawyer WH

更新日期：1986-08-01 00:00:00

abstract：:The powerful analgesic effects of opioid drugs have captivated the interest of physicians and scientists for millennia, and the ability of opioid drugs to produce serious undesired effects has been recognized for a similar period of time (Kieffer and Evans, 2009). Many of these develop progressively with prolonged or ...

journal_title：Molecular pharmacology

authors： Jullié D,Gondin AB,von Zastrow M,Canals M

更新日期：2020-10-01 00:00:00

abstract：:The effects of the dihydropyridine calcium channel agonist Bay K 8644 on indo-1-loaded Jurkat human leukemia T lymphocytes was assessed by flow cytometry. Bay K 8644 from 10(-9) to 10(-4) M caused a dose-dependent rise in the intracellular free Ca concentration, an effect that was not mimicked by the dihydropyridine C...

journal_title：Molecular pharmacology

authors： Young W,Chen J,Jung F,Gardner P

更新日期：1988-09-01 00:00:00

abstract：:Previous studies revealed that phenylhistamines and histaprodifens possess higher potency and affinity at guinea pig histamine H(1)-receptor (gpH(1)R) than at human histamine H(1)-receptor (hH(1)R). However, we recently identified an imidazolylpropylguanidine [N(1)-(3-cyclohexylbutanoyl)-N(2)-[3-(1H-imidazol-4-yl)-pro...

journal_title：Molecular pharmacology

authors： Strasser A,Wittmann HJ,Kunze M,Elz S,Seifert R

更新日期：2009-03-01 00:00:00

abstract：:A collection of analogues of atrial natriuretic peptide (ANP) were screened for their ability to inhibit ANP-induced cGMP stimulation. The antagonists revealed through this screen are structurally related; almost all are substituted at either aspartate-13 or phenylalanine-26. This tendency is consistent throughout sev...

journal_title：Molecular pharmacology

authors： von Geldern TW,Budzik GP,Dillon TP,Holleman WH,Holst MA,Kiso Y,Novosad EI,Opgenorth TJ,Rockway TW,Thomas AM

更新日期：1990-12-01 00:00:00

abstract：:Tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione (TIBO) derivatives (e.g., R82150) are potent, human immunodeficiency virus-1 (HIV-1)-specific, inhibitors of reverse transcriptase (RT) that are undergoing initial evaluation in clinical trials. Because HIV-1 has become resistant to other RT inhibitor...

journal_title：Molecular pharmacology

authors： Mellors JW,Im GJ,Tramontano E,Winkler SR,Medina DJ,Dutschman GE,Bazmi HZ,Piras G,Gonzalez CJ,Cheng YC

更新日期：1993-01-01 00:00:00

abstract：:The X-ray and NMR structural study of 3-carbomethoxy rifamycin S5 was undertaken in order to determine whether its low antimicrobial activity was related to a conformation of the molecule which was unfavorable for interaction with bacterial DNA-dependent RNA polymerase. However, the molecule assumes a conformation sim...

journal_title：Molecular pharmacology

authors： Brufani M,Cellai L,Cerrini S,Fedeli W,Segre A,Vaciago A

更新日期：1982-03-01 00:00:00

abstract：:Glucocorticoid-induced tumor necrosis factor receptor-related (GITR) protein is a costimulatory molecule that plays a role in inflammation so that GITR-Fc fusion protein can exert an anti-inflammatory effect. To investigate the mechanism by which GITR-Fc exerts its effects, we first used GITR knock-out (GITR(-/-)) mic...

journal_title：Molecular pharmacology

authors： Nocentini G,Cuzzocrea S,Genovese T,Bianchini R,Mazzon E,Ronchetti S,Esposito E,Rosanna DP,Bramanti P,Riccardi C

更新日期：2008-06-01 00:00:00

abstract：:Adenosine uptake via nucleoside transporters is inhibited when S49 and NG108-15 cell lines cells are exposed to ethanol. This inhibition leads to an accumulation of extracellular adenosine that binds to adenosine A2 receptors and increases cAMP production. Subsequently, there is a heterologous desensitization of recep...

journal_title：Molecular pharmacology

authors： Krauss SW,Ghirnikar RB,Diamond I,Gordon AS

更新日期：1993-11-01 00:00:00