Characterization of alpha 1- and alpha 2-adrenoceptors directly associated with basolateral membranes from rat kidney proximal tubules.


:We have used 2-(beta-(3-125iodo-4-hydroxyphenyl)-ethylaminoethyl)-tetr alo ne ([125I]HEAT or BE2254), an alpha 1-selective antagonist, and [3H]yohimbine, an alpha 2-selective antagonist, to demonstrate and characterize binding sites in basolateral membranes from rat kidney cortex. Parathyroid hormone (PTH) stimulated the adenylate cyclase activity of the basolateral membranes, whereas thyrocalcitonin, arginine vasopressin (AVP) and isoproterenol did not. Therefore, the basolateral membranes were probably derived from the proximal tubules. The specific binding of [125I]HEAT and [3H]yohimbine to basolateral membranes was rapid, reversible, saturable and of high affinity. The maximum densities of alpha 1- and alpha 2-receptors were 364 and 1130 fmoles/mg protein, indicating that the ratio of alpha 1- to alpha 2-adrenoceptors was about 1:3. The specific binding of [125I]HEAT and [3H]yohimbine to the basolateral membranes was displaced by various adrenergic agents in a manner that suggests that the labeled sites probably represent alpha 1- and alpha 2-adrenoceptors respectively. These results suggest that the binding sites of [125I]HEAT and [3H]yohimbine, which appear to be alpha 1- and alpha 2-adrenoceptors, exist in the basolateral membranes of the proximal tubules.


Biochem Pharmacol


Biochemical pharmacology


Matsushima Y,Akabane S,Ito K




Has Abstract


1986-08-01 00:00:00














  • Therapeutic implications of the prostaglandin pathway in Alzheimer's disease.

    abstract::An important pathologic hallmark of Alzheimer's disease (AD) is neuroinflammation, a process characterized in AD by disproportionate activation of cells (microglia and astrocytes, primarily) of the non-specific innate immune system within the CNS. While inflammation itself is not intrinsically detrimental, a delicate ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Cudaback E,Jorstad NL,Yang Y,Montine TJ,Keene CD

    更新日期:2014-04-15 00:00:00

  • Clavilactones, a novel class of tyrosine kinase inhibitors of fungal origin.

    abstract::Targeting of deregulated protein tyrosine kinases has been proposed as a new approach in the therapeutic intervention against pathological processes including proliferative disorders and cancer. Using a screening approach based on a comparative evaluation of antiproliferative effects in a panel of tumor cells with dif...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Cassinelli G,Lanzi C,Pensa T,Gambetta RA,Nasini G,Cuccuru G,Cassinis M,Pratesi G,Polizzi D,Tortoreto M,Zunino F

    更新日期:2000-06-15 00:00:00

  • Selective action of the iminosugar isofagomine, a pharmacological chaperone for mutant forms of acid-beta-glucosidase.

    abstract::Gaucher disease is a lysosomal glycolipid storage disorder characterized by defects in acid-beta-glucosidase (GlcCerase), the enzyme responsible for the catabolism of glucosylceramide. We recently demonstrated that isofagomine (IFG), an iminosugar that binds to the active site of GlcCerase, enhances the folding, trans...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Steet R,Chung S,Lee WS,Pine CW,Do H,Kornfeld S

    更新日期:2007-05-01 00:00:00

  • Antibiotic efflux pumps.

    abstract::Active efflux from procaryotic as well as eucaryotic cells strongly modulates the activity of a large number of antibiotics. Effective antibiotic transport has now been observed for many classes of drug efflux pumps. Thus, within the group of primary active transporters, predominant in eucaryotes, six families belongi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Van Bambeke F,Balzi E,Tulkens PM

    更新日期:2000-08-15 00:00:00

  • 5-Substituted-2,2'-anhydrouridines, potent inhibitors of uridine phosphorylase.

    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

    pub_type: 杂志文章


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

    更新日期:1985-05-15 00:00:00

  • The Bcr-Abl inhibitor GNF-7 inhibits necroptosis and ameliorates acute kidney injury by targeting RIPK1 and RIPK3 kinases.

    abstract::Necroptosis is a form of programmed, caspase-independent cell death that is involved in various pathologic disorders such as ischemia/reperfusion injury, acute kidney injury and inflammatory bowel diseases. Identification of necroptosis inhibitors has great therapeutic potential for the treatment of necroptosis-associ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Qin X,Hu L,Shi SN,Chen X,Zhuang C,Zhang W,Jitkaew S,Pang X,Yu J,Tan YX,Wang HY,Cai Z

    更新日期:2020-07-01 00:00:00

  • Poly(ADP-ribose) polymerase regulates myocardial calcium handling in doxorubicin-induced heart failure.

    abstract::Reactive oxygen and nitrogen species are overproduced in the cardiovascular system in response to the exposure to doxorubicin, a cardiotoxic anticancer compound. Oxidant-induced cell injury involves the activation of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) and pharmacological inhibition of PARP has recen...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Szenczi O,Kemecsei P,Holthuijsen MF,van Riel NA,van der Vusse GJ,Pacher P,Szabó C,Kollai M,Ligeti L,Ivanics T

    更新日期:2005-03-01 00:00:00

  • Interaction of permanently charged analogs of dopamine with the D-2 dopaminergic receptor.

    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

    pub_type: 杂志文章


    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

  • Therapeutic and preventive properties of quercetin in experimental arthritis correlate with decreased macrophage inflammatory mediators.

    abstract::Pentahydroxyflavone dihydrate, quercetin (QU) is one of common flavonols biosynthesized by plants and has been suggested to modulate inflammatory responses in various models. In the present study, we investigated in vivo effects of oral or intra-cutaneous QU in chronic rat adjuvant-induced arthritis (AA). Growth delay...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mamani-Matsuda M,Kauss T,Al-Kharrat A,Rambert J,Fawaz F,Thiolat D,Moynet D,Coves S,Malvy D,Mossalayi MD

    更新日期:2006-11-15 00:00:00

  • Cellular pharmacokinetics of carboplatin and cisplatin in relation to their cytotoxic action.

    abstract::We have studied the cellular pharmacokinetics of carboplatin (CBDCA), as part of the evaluation of the antitumor activity of CBDCA in cancers limited to the peritoneal cavity in comparison with cisplatin (cDDP). The uptake of CBDCA into L1210 (lymphosarcoma), CC531 (colonic carcinoma), COV413.B (human ovarian carcinom...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Los G,Verdegaal E,Noteborn HP,Ruevekamp M,de Graeff A,Meesters EW,ten Bokkel Huinink D,McVie JG

    更新日期:1991-07-05 00:00:00

  • Uptake and cytofluorescence localization of ellipticine derivatives in sensitive and resistant Chinese hamster lung cells.

    abstract::Uptake of two ellipticine derivatives, 2-N-methyl-ellipticinium (NME) and 2-N-methyl-9-hydroxy-ellipticinium, by sensitive and resistant Chinese hamster lung cells was studied. The results show that uptake and retention of these molecules by both types of cells were identical, thus indicating that the resistance to el...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Charcosset JY,Salles B,Jacquemin-Sablon A

    更新日期:1983-03-15 00:00:00

  • CagA protein of Helicobacter pylori: a hijacker of gastric epithelial cell signaling.

    abstract::Epidemiological study has shown strong correlation between the Helicobacter pylori (H. pylori) infection and gastric carcinogenesis. However, the mechanism by which H. pylori induces gastric carcinogenesis is not known. In this review, we focused on the product of cytotoxin-associated gene A (CagA), one of the importa...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Handa O,Naito Y,Yoshikawa T

    更新日期:2007-06-01 00:00:00

  • Involvement of tumor necrosis factor (TNF)-alpha in phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin edema in mice.

    abstract::Topical application of 12-O-tetradecanoylphorbol-13-acetate (TPA) to mouse ear induced a prolonged skin inflammation. Histological analysis revealed that the early stage (approximately 3 h) and later stage (6-24 h) of the skin reaction are characterized by dermal edema and cell accumulation, respectively. Topical appl...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Murakawa M,Yamaoka K,Tanaka Y,Fukuda Y

    更新日期:2006-04-28 00:00:00

  • Broad specificity of human phosphoglycerate kinase for antiviral nucleoside analogs.

    abstract::Nucleoside analogs used in antiviral therapies need to be phosphorylated to their tri-phospho counterparts in order to be active on their cellular target. Human phosphoglycerate kinase (hPGK) was recently reported to participate in the last step of phosphorylation of cytidine L-nucleotide derivatives [Krishnan PGE, La...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gallois-Montbrun S,Faraj A,Seclaman E,Sommadossi JP,Deville-Bonne D,Véron M

    更新日期:2004-11-01 00:00:00

  • Curcumin induces electrical activity in rat pancreatic beta-cells by activating the volume-regulated anion channel.

    abstract::Curcumin, the principal active component of turmeric, is reported to exert a number of therapeutic actions, including a hypoglycaemic/antidiabetic action. The underlying mechanisms to this action are essentially unknown. We have investigated the hypothesis that a direct stimulatory action on the pancreatic beta-cell c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Best L,Elliott AC,Brown PD

    更新日期:2007-06-01 00:00:00

  • Enhanced expression of organic anion transporting polypeptides (OATPs) in androgen receptor-positive prostate cancer cells: possible role of OATP1A2 in adaptive cell growth under androgen-depleted conditions.

    abstract::The biological mechanisms underlying castration resistance of prostate cancer are not fully understood. In the present study, we examined the role of organic anion transporting polypeptides (OATPs) as importers of dehydroepiandrosterone sulfate (DHEAS) into cells to support growth under androgen-depleted conditions. C...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Arakawa H,Nakanishi T,Yanagihara C,Nishimoto T,Wakayama T,Mizokami A,Namiki M,Kawai K,Tamai I

    更新日期:2012-10-15 00:00:00

  • Zardaverine as a selective inhibitor of phosphodiesterase isozymes.

    abstract::The pyridazinone derivative zardaverine has recently been introduced as a potent bronchodilator in vivo and in vitro. In addition, zardaverine exerts a positive inotropic action on heart muscle in vitro. The actions of zardaverine are thought to be mediated via inhibition of phosphodiesterase (PDE) activity. Recent da...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Schudt C,Winder S,Müller B,Ukena D

    更新日期:1991-06-21 00:00:00

  • The non-steroidal mineralocorticoid receptor antagonist finerenone prevents cardiac fibrotic remodeling.

    abstract::Mineralocorticoid receptor (MR) overactivation promotes cardiac fibrosis. We studied the ability of the non-steroidal MR antagonist finerenone to prevent fibrotic remodeling. In neonatal rat cardiac fibroblasts, finerenone prevented aldosterone-induced nuclear MR translocation. Treatment with finerenone decreased the ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lavall D,Jacobs N,Mahfoud F,Kolkhof P,Böhm M,Laufs U

    更新日期:2019-10-01 00:00:00

  • Enforced expression of the tumor suppressor p53 renders human leukemia cells (U937) more sensitive to 1-[beta-D-arabinofuranosyl]cytosine (ara-C)-induced apoptosis.

    abstract::The effects of enforced expression of p53 on the sensitivity of p53(-/-) human monocytic leukemia cells (U937) to apoptosis following exposure to the S-phase-specific antimetabolite 1-[beta-D-arabinofuranosyl]cytosine (ara-C) were examined. Cells were stably transfected with a plasmid containing a chimeric DNA constru...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Decker RH,Levin J,Kramer LB,Dai Y,Grant S

    更新日期:2003-06-15 00:00:00

  • Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. I. Description of an enzymatic activity in spleen membranes.

    abstract::The mechanism for formation of high-affinity binding of 1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine (guanoxabenz) to alpha2-adrenoceptors was studied in particulate fractions from the rat spleen. The proportion of apparent high versus low-affinity alpha2-adrenoceptor binding sites increased with increasing in...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Uhlén S,Dambrova M,Tiger G,Oliver DW,Wikberg JE

    更新日期:1998-11-01 00:00:00

  • The modulation of the DNA-damaging effect of polycyclic aromatic agents by xanthines. Part I. Reduction of cytostatic effects of quinacrine mustard by caffeine.

    abstract::Recently, accumulated statistical data indicate the protective effect of caffeine consumption against several types of cancer diseases. There are also reports about protective effect of caffeine and other xanthines against tumors induced by polycyclic aromatic hydrocarbons. One of the explanations is based on biologic...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kapuscinski J,Ardelt B,Piosik J,Zdunek M,Darzynkiewicz Z

    更新日期:2002-02-15 00:00:00

  • DNA-DNA interstrand crosslinking by dimethyanesulphonic acid esters. Correlation with cytotoxicity and antitumour activity in the Yoshida lymphosarcoma model and relationship to chain length.

    abstract::Members of the homologous series of nine antitumour dimethanesulphonic acid esters, with the exception of ethylene dimethanesulphonate (EDMS), were found to cause DNA-DNA interstrand crosslinking in cells derived from the transplantable rodent Yoshida lymphosarcoma. The ability of the series to induce interstrand cros...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Bedford P,Fox BW

    更新日期:1983-08-01 00:00:00

  • Modulation of GSH levels in ABCC1 expressing tumor cells triggers apoptosis through oxidative stress.

    abstract::The over-expression of ABCC1 transmembrane protein has been shown to cause multidrug resistance in tumor cell lines. ABCC1 is a member of the ABC transmembrane proteins that function as efflux pumps with diverse substrate specificity. Several endogenous cell metabolites, including the leukotriene C4 (LTC(4)) and gluta...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Laberge RM,Karwatsky J,Lincoln MC,Leimanis ML,Georges E

    更新日期:2007-06-01 00:00:00

  • Stereoselective binding of the glucuronide conjugates of carprofen enantiomers to human serum albumin.

    abstract::The stereoselective binding of carprofen enantiomers and carprofen glucuronide diastereomers to human serum albumin (HSA) was studied using an ultrafiltration method. Carprofen glucuronides exhibit a considerable and stereoselective affinity to HSA, although less than that seen for the parent enantiomers. The (S)-gluc...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Iwakawa S,Spahn H,Benet LZ,Lin ET

    更新日期:1990-03-01 00:00:00

  • Adiponectin induces apoptosis in hepatocellular carcinoma through differential modulation of thioredoxin proteins.

    abstract::Adiponectin blocks hepatocellular carcinoma (HCC) progression by inducing cell apoptosis through the modulation of C-Jun N-terminal kinase and mammalian target of rapamycin. However, the precise upstream signaling pathways or molecules remain elusive. In the present study, we analyzed the role of antioxidant protein t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Xing SQ,Zhang CG,Yuan JF,Yang HM,Zhao SD,Zhang H

    更新日期:2015-01-15 00:00:00

  • Stimulation by chelerythrine of the phosphorylation of the amino acid serine in an approximately 20 kDa protein present in the mitochondrial fraction of the rat retina.

    abstract::It has been reported that chelerythrine chloride, a benzophenanthridine alkaloid, with a wide variety of biologic effects stimulates the phosphorylation of an approximately 20 kDa protein present in the mitochondrial fraction of the rat retina. It has also been shown previously that both the serine and threonine resid...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lombardini JB

    更新日期:1996-07-26 00:00:00

  • Inter-strand cross-links and single-strand breaks produced by gold(I) and gold(III) coordination complexes.

    abstract::The ability of gold coordination complexes to bind to DNA and produce inter-strand cross-links in DNA was assessed in an assay system based on the fluorescence properties of the DNA intercalative dye, ethidium bromide. Results from these studies using a variety of gold(I) and gold(III) complexes suggest that the abili...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mirabelli CK,Zimmerman JP,Bartus HR,Sung CM,Crooke ST

    更新日期:1986-05-01 00:00:00

  • Role of NADPH:cytochrome P450 reductase in the hypoxic accumulation and metabolism of BRU59-21, a technetium-99m-nitroimidazole for imaging tumor hypoxia.

    abstract::Nitroimidazoles labeled with technetium-99m are being investigated as non-invasive markers of tumor hypoxia. They are bioreductive compounds that require enzymatic reduction for retention in hypoxic cells, but little is known about the cellular factors affecting their accumulation in hypoxic cells. If the absolute acc...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Melo T,Ballinger JR,Rauth AM

    更新日期:2000-09-01 00:00:00

  • Catalase expression in MCF-7 breast cancer cells is mainly controlled by PI3K/Akt/mTor signaling pathway.

    abstract::Catalase is an antioxidant enzyme that catalyzes mainly the transformation of hydrogen peroxide into water and oxygen. Although catalase is frequently down-regulated in tumors the underlying mechanism remains unclear. Few transcription factors have been reported to directly bind the human catalase promoter. Among them...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Glorieux C,Auquier J,Dejeans N,Sid B,Demoulin JB,Bertrand L,Verrax J,Calderon PB

    更新日期:2014-05-15 00:00:00

  • Acute and chronic in vivo therapeutic resistance.

    abstract::The response and engagement of host normal tissues in malignant disease are major factors in therapeutic resistance. Physically, solid tumors have regions of hypoxia and acidosis. These physical stresses can lead to a more aggressive malignant phenotype through activation of HIF, GLUT-1, carbonic anhydrase IX, and sub...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Teicher BA

    更新日期:2009-06-01 00:00:00