当前位置： SCI文献检索 > MOLECULAR PHARMACOLOGY期刊下所有文献 > Characterization of serotonin uptake in cultured pheochromocytoma cells. Comparison with norepinephrine uptake.

Characterization of serotonin uptake in cultured pheochromocytoma cells. Comparison with norepinephrine uptake.

Abstract：

:PC-12 cells, derived from a rat pheochromocytoma, were found to take up tritiated serotonin ([3H]5-HT) from the external medium by means of a saturable mechanism which follows Michaelis-Menten kinetics. The apparent Km of uptake was 0.39 microM and the Vmax was 0.40 pmole/min/10(6) cells. The uptake was temperature-dependent, partially sodium-dependent, and inhibited by selected metabolic inhibitors (sodium azide, 2,4-dinitrophenol, and iodoacetamide), PC-12 cells also accumulated tritiated norepinephrine ([3H]NE) by a saturable process, with an apparent Km of 1.13 microM and a Vmax of 1.72 pmole/min/10(6) cells. This NE uptake process was also temperature- and sodium-dependent and inhibited by metabolic inhibitors and ouabain. Desmethylimipramine (DMI, IC50 = 3.8 microM) was a better inhibitor of [3H]NE uptake than fluoxetine (IC50 = 24.6 microM). The NE uptake process was structurally specific, since unlabeled NE was a better inhibitor of [3H]NE uptake than 5-HT (IC50 = 19.6 and 171 microM, respectively). However, [3H]5-HT uptake in PC-12 cells appeared to be a less structurally specific process, as it was equally inhibited by unlabeled 5-HT and NE (IC50 4.9 microM and 4.3 microM, respectively). DMI was also a better inhibitor of [3H]5-HT uptake than fluoxetine (IC50 = 85 and 411 microM, respectively). The neurotoxins 6-hydroxydopamine and 5,6-dihydroxytryptamine were cytotoxic to PC-12 cells, causing a time- and concentration-dependent inhibition of [3H]thymidine incorporation into DNA. 5,7-Dihydroxytryptamine had little cytotoxic effect toward PC-12 cells in culture.

journal_name

Mol Pharmacol

journal_title

Molecular pharmacology

authors

Yoffe JR,Borchardt RT

subject

Has Abstract

pub_date

1982-03-01 00:00:00

pages

368-73

issue

2

eissn

0026-895X

issn

1521-0111

journal_volume

21

pub_type

杂志文章

相关文献

MOLECULAR PHARMACOLOGY文献大全
  • N-methyl-D-aspartate excitotoxicity: relationships among plasma membrane potential, Na(+)/Ca(2+) exchange, mitochondrial Ca(2+) overload, and cytoplasmic concentrations of Ca(2+), H(+), and K(+).

    abstract：:A high cytoplasmic Na(+) concentration may contribute to N-methyl-D-aspartate (NMDA)-induced excitotoxicity by promoting Ca(2+) influx via reverse operation of the Na(+)/Ca(2+) exchanger (NaCaX), but may simultaneously decrease the electrochemical Ca(2+) driving force by depolarizing the plasma membrane (PM). Digital ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.56.3.619

    authors： Kiedrowski L

    更新日期：1999-09-01 00:00:00

  • Catalytic properties of NAD(P)H:quinone acceptor oxidoreductase: study involving mouse, rat, human, and mouse-rat chimeric enzymes.

    abstract：:NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, C...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Chen S,Knox R,Lewis AD,Friedlos F,Workman P,Deng PS,Fung M,Ebenstein D,Wu K,Tsai TM

    更新日期：1995-05-01 00:00:00

  • State-dependent etomidate occupancy of its allosteric agonist sites measured in a cysteine-substituted GABAA receptor.

    abstract：:A central axiom of ligand-receptor theory is that agonists bind more tightly to active than to inactive receptors. However, measuring agonist affinity in inactive receptors is confounded by concomitant activation. We identified a cysteine substituted mutant γ-aminobutyric acid type A (GABAA) receptor with unique chara...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.112.084558

    authors： Stewart DS,Hotta M,Desai R,Forman SA

    更新日期：2013-06-01 00:00:00

  • Altered G-protein coupling in an mGluR6 point mutant associated with congenital stationary night blindness.

    abstract：:The highly specialized metabotropic glutamate receptor type 6 (mGluR6) is postsynaptically localized and expressed only in the dendrites of ON bipolar cells. Upon activation of mGluR6 by glutamate released from photoreceptors, a nonselective cation channel is inhibited, causing these cells to hyperpolarize. Mutations ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.109.058628

    authors： Beqollari D,Betzenhauser MJ,Kammermeier PJ

    更新日期：2009-11-01 00:00:00

  • Alteration in accumulated aldosterone synthesis as a result of N-terminal cleavage of aldosterone synthase.

    abstract：:Aldosterone synthase (AS) regulates blood volume by synthesizing the mineralocorticoid aldosterone. Overproduction of aldosterone in the adrenal gland can lead to hypertension, a major cause of heart disease and stroke. Aldosterone production depends upon stimulation of AS expression by the renin-angiotensin system, w...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.111.076471

    authors： Adams BP,Bose HS

    更新日期：2012-03-01 00:00:00

  • Repeated electroconvulsive shock: effect on sodium dependency and regional distribution of opioid-binding sites.

    abstract：:The effects of single and repeated electroconvulsive shock (ECS) on the binding of [3H]diprenorphine to rat brain membranes was studied. Repeated but not single ECS significantly increased the Bmax of [3H]diprenorphine binding when measured in the absence but not in the presence of NaCl. On a regional basis the effect...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Hitzemann RJ,Hitzemann BA,Blatt S,Meyerhoff JL,Tortella FC,Kenner JR,Belenky GL,Holaday JW

    更新日期：1987-05-01 00:00:00

  • Expression of beta-adrenergic receptors in synchronous and asynchronous S49 lymphoma cells. II. Relationship between receptor number and response.

    abstract：:We have used two experimental approaches--receptor inactivation with an irreversible antagonist and changes in receptor expression during passage of cells through the cell cycle--to explore the relationship between beta-adrenergic receptor number and response in intact S49 lymphoma cells. beta-Receptors in asynchronou...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Mahan LC,Insel PA

    更新日期：1986-01-01 00:00:00

  • Molecular basis of pimarane compounds as novel activators of large-conductance Ca(2+)-activated K(+) channel alpha-subunit.

    abstract：:Effects of pimaric acid (PiMA) and eight closely related compounds on large-conductance K(+) (BK) channels were examined using human embryonic kidney (HEK) 293 cells, in which either the alpha subunit of BK channel (HEKBKalpha) or both alpha and beta1 (HEKBKalphabeta1) subunits were heterologously expressed. Effects o...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.62.4.836

    authors： Imaizumi Y,Sakamoto K,Yamada A,Hotta A,Ohya S,Muraki K,Uchiyama M,Ohwada T

    更新日期：2002-10-01 00:00:00

  • A crucial role for the mitogen-activated protein kinase pathway in nicotinic cholinergic signaling to secretory protein transcription in pheochromocytoma cells.

    abstract：:The mitogen-activated protein kinase (MAPK) pathway plays a pivotal role in intracellular signaling, and this cascade may impinge on cAMP response elements (CREs) of target genes. Both the MAPK pathway and chromogranin A expression may be activated by cytosolic calcium influx, and calcium-dependent signals map onto th...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.54.1.59

    authors： Tang K,Wu H,Mahata SK,O'Connor DT

    更新日期：1998-07-01 00:00:00

  • Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators.

    abstract：:The compound 4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid (DQP-1105) is a representative member of a new class of N-methyl-d-aspartate (NMDA) receptor antagonists. DQP-1105 inhibited GluN2C- and GluN2D-containing receptors with IC(50) values ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.111.073239

    authors： Acker TM,Yuan H,Hansen KB,Vance KM,Ogden KK,Jensen HS,Burger PB,Mullasseril P,Snyder JP,Liotta DC,Traynelis SF

    更新日期：2011-11-01 00:00:00

  • DNA interactions of a novel platinum drug, cis-[PtCl(NH3)2(N7-acyclovir)]+.

    abstract：:We synthesized a novel platinum drug, cis-[PtCl(NH3)2(N7-ACV)]+, in which ACV is the antiviral drug acyclovir [a deoxyriboguanosine analogue, 9-(2-hydroxyethoxymethyl)guanine]. This new compound exhibits antiviral efficacy in vitro and exhibits an antitumor activity profile different from that of cisplatin [Metal-Base...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Balcarová Z,Kaspárková J,Zákovská A,Nováková O,Sivo MF,Natile G,Brabec V

    更新日期：1998-05-01 00:00:00

  • Cysteine Scanning Mutagenesis of TM4b-4c Loop of Glutamate Transporter EAAT1 Reveals Three Conformationally Sensitive Residues.

    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

    pub_type： 杂志文章

    doi：10.1124/mol.117.111245

    authors： Zhang W,Zhang X,Qu S

    更新日期：2018-07-01 00:00:00

  • Activation of the c-jun protooncogene in human myeloid leukemia cells treated with etoposide.

    abstract：:The epipodophyllotoxin etoposide is an inhibitor of topoisomerase II. The effects of this agent on gene expression, particularly the transcriptional induction of genes implicated in growth control, are unknown. The present results demonstrate that etoposide induces expression of the c-jun protooncogene in HL-60 myeloi...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Rubin E,Kharbanda S,Gunji H,Kufe D

    更新日期：1991-06-01 00:00:00

  • Paclitaxel-induced immune suppression is associated with NF-kappaB activation via conventional PKC isotypes in lipopolysaccharide-stimulated 70Z/3 pre-B lymphocyte tumor cells.

    abstract：:Paclitaxel, a potent antitumor agent, has been shown to be lipopolysaccharide (LPS) mimetic in mice, stimulating signaling pathways and gene expression indistinguishably from LPS. In the present study, we showed the intracellular signaling pathway of paclitaxel-induced nuclear factor-kappaB (NF-kappaB) activation and ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.59.2.248

    authors： Lee M,Jeon YJ

    更新日期：2001-02-01 00:00:00

  • Competitive antagonism of recombinant P2X(2/3) receptors by 2', 3'-O-(2,4,6-trinitrophenyl) adenosine 5'-triphosphate (TNP-ATP).

    abstract：:TNP-ATP has become widely recognized as a potent and selective P2X receptor antagonist, and is currently being used to discriminate between subtypes of P2X receptors in a variety of tissues. We have investigated the ability of TNP-ATP to inhibit alpha,beta-methylene ATP (alpha,beta-meATP)-evoked responses in 1321N1 hu...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.58.6.1502

    authors： Burgard EC,Niforatos W,van Biesen T,Lynch KJ,Kage KL,Touma E,Kowaluk EA,Jarvis MF

    更新日期：2000-12-01 00:00:00

  • Enantioselective effects of hydroxy metabolites of bupropion on behavior and on function of monoamine transporters and nicotinic receptors.

    abstract：:Bupropion is an atypical antidepressant that also has usefulness as a smoking-cessation aid. Because hydroxybupropion, a major metabolite of bupropion, is believed to contribute to its antidepressant activity, this metabolite may also contribute to the smoking-cessation properties of bupropion. This study investigated...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.104.001313

    authors： Damaj MI,Carroll FI,Eaton JB,Navarro HA,Blough BE,Mirza S,Lukas RJ,Martin BR

    更新日期：2004-09-01 00:00:00

  • Transcriptional Regulation of Human Cytosolic Sulfotransferase 1C3 by Peroxisome Proliferator-Activated Receptor γ in LS180 Human Colorectal Adenocarcinoma Cells.

    abstract：:Cytosolic sulfotransferase 1C3 (SULT1C3) is the least characterized of the three human SULT1C subfamily members. Originally identified as an orphan SULT by computational analysis of the human genome, we recently reported that SULT1C3 is expressed in human intestine and LS180 colorectal adenocarcinoma cells and is upre...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.116.106005

    authors： Dubaisi S,Fang H,Kocarek TA,Runge-Morris M

    更新日期：2016-11-01 00:00:00

  • In GH3 pituitary cells, acetylcholine and vasoactive intestinal peptide antagonistically modulate adenylate cyclase, cyclic AMP content, and prolactin secretion.

    abstract：:In GH3 pituitary cell homogenates, acetylcholine (ACh) (IC50 200 nM) inhibits adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] activity in a concentration- and GTP-dependent manner. Maximal inhibition was obtained with 10 microM ACh and corresponded to approximately a 50% decrease in basal enzyme ac...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Onali P,Eva C,Olianas MC,Schwartz JP,Costa E

    更新日期：1983-09-01 00:00:00

  • Untranslated region-dependent exclusive expression of high-sensitivity subforms of alpha4beta2 and alpha3beta2 nicotinic acetylcholine receptors.

    abstract：:alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are recognized as the principal nicotine binding site in brain. Recombinant alpha4beta2 nAChR demonstrate biphasic concentration-response relationships with low- and high-EC50 components. This study shows that untranslated regions (UTR) can influence expression of...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.105.020198

    authors： Briggs CA,Gubbins EJ,Marks MJ,Putman CB,Thimmapaya R,Meyer MD,Surowy CS

    更新日期：2006-07-01 00:00:00

  • Correction to"The LRRC26 Protein Selectively Alters the Efficacy of BK Channel Activators".

    abstract：:[This corrects the article on p. 21 in vol. 81, PMID: 21984254.]. ...

    journal_title：Molecular pharmacology

    pub_type： 已发布勘误

    doi：10.1124/mol.115.075234err

    authors：

    更新日期：2016-01-01 00:00:00

  • Methamphetamine causes coordinate regulation of Src, Cas, Crk, and the Jun N-terminal kinase-Jun pathway.

    abstract：:The clinical abuse of methamphetamine (METH) is a major concern because it can cause long-lasting neurodegenerative effects in humans. Current concepts of the molecular mechanisms underlying these complications have centered on the formation of reactive oxygen species. Herein, we provide cDNA microarray evidence that ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.61.5.1124

    authors： Jayanthi S,McCoy MT,Ladenheim B,Cadet JL

    更新日期：2002-05-01 00:00:00

  • High affinity agonist binding to the dopamine D3 receptor: chimeric receptors delineate a role for intracellular domains.

    abstract：:The dopamine D3 receptor, although structurally similar to the dopamine D2 receptor, has 100-fold higher affinity for agonists such as dopamine and quinpirole, when these receptors are expressed in 293 cells. Additionally, the D3 receptor has generally lower affinity for several antagonists than does the D2 receptor. ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Robinson SW,Jarvie KR,Caron MG

    更新日期：1994-08-01 00:00:00

  • Differential effects of melanocortin peptides on neural melanocortin receptors.

    abstract：:Melanocortins (MCs) have various physiological actions on the brain. The recent cloning of neural MC receptors opened new avenues to study the effects of these neuropeptides on the nervous system. Here we investigated the structure-activity relationships (SARs) of peptides derived from adrenocorticotropic hormone (ACT...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Adan RA,Cone RD,Burbach JP,Gispen WH

    更新日期：1994-12-01 00:00:00

  • Characterization of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one as a heme-site inhibitor of nitric oxide-sensitive guanylyl cyclase.

    abstract：:Nitric oxide (NO) binds with high affinity to the heme of soluble guanylyl cyclase (sGC), resulting in accumulation of the second messenger cGMP in many biological systems. 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) was recently described as potent and selective inhibitor of sGC, providing an invaluable tool wi...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Schrammel A,Behrends S,Schmidt K,Koesling D,Mayer B

    更新日期：1996-07-01 00:00:00

  • Properties of expressed and native flavin-containing monooxygenases: evidence of multiple forms in rabbit liver and lung.

    abstract：:Our laboratory recently isolated and sequenced cDNAs encoding the microsomal flavin-containing monooxygenases (FMOs) from rabbit liver and rabbit lung. As a first step in understanding the molecular bases for the catalytic and physical differences between these enzymes, we have expressed them in COS-1 cells and compar...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Lawton MP,Kronbach T,Johnson EF,Philpot RM

    更新日期：1991-11-01 00:00:00

  • Mechanisms of cell killing by drugs that trap covalent complexes between DNA topoisomerases and DNA.

    abstract：:DNA topoisomerases are the molecular targets of a range of anticancer and antimicrobial therapeutics. Many of these drugs act by converting their target enzyme to a DNA-damaging agent through the trapping of the covalent enzyme/DNA intermediate. This drug-mediated trapping of the intermediate is reversible, and the le...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Nitiss JL,Wang JC

    更新日期：1996-11-01 00:00:00

  • Identification and characterization of three new alternatively spliced mu-opioid receptor isoforms.

    abstract：:We have identified four new mu-opiod receptor (MOR)-1 exons, indicating that the gene now contains at least nine exons spanning more than 200 kilobases. Replacement of exon 4 by combinations of the new exons yields three new receptors. When expressed in Chinese hamster ovary cells, all three variants displayed high af...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.56.2.396

    authors： Pan YX,Xu J,Bolan E,Abbadie C,Chang A,Zuckerman A,Rossi G,Pasternak GW

    更新日期：1999-08-01 00:00:00

  • Oxidative Stress and Response to Thymidylate Synthase-Targeted Antimetabolites.

    abstract：:Thymidylate synthase (TYMS; EC 2.1.1.15) catalyzes the reductive methylation of 2'-deoxyuridine-5'-monophosphate (dUMP) by N(5),N(10)-methyhlenetetrahydrofolate, forming dTMP for the maintenance of DNA replication and repair. Inhibitors of TYMS have been widely used in the treatment of neoplastic disease. A number of ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.115.099614

    authors： Ozer U,Barbour KW,Clinton SA,Berger FG

    更新日期：2015-12-01 00:00:00

  • Bezafibrate induces plasminogen activator inhibitor-1 gene expression in a CLOCK-dependent circadian manner.

    abstract：:A functional interaction between peroxisome proliferator-activated receptor alpha (PPARalpha) and components of the circadian clock has been suggested, but whether these transcriptional factors interact to regulate the expression of their target genes remains obscure. Here we used a PPARalpha ligand, bezafibrate, to s...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.110.064402

    authors： Oishi K,Koyanagi S,Matsunaga N,Kadota K,Ikeda E,Hayashida S,Kuramoto Y,Shimeno H,Soeda S,Ohdo S

    更新日期：2010-07-01 00:00:00

  • The relationship between the catalytic activities of rabbit pulmonary cytochrome P-450 isozymes and the lung-specific toxicity of the furan derivative, 4-ipomeanol.

    abstract：:Metabolism of the pulmonary toxin, 4-ipomeanol, in microsomal preparations from rabbit liver and lung and in purified cytochrome P-450-dependent monooxygenase systems was investigated. The rate of formation of reactive electrophilic products from 4-ipomeanol was estimated by measuring covalent binding to protein or gl...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Wolf CR,Statham CN,McMenamin MG,Bend JR,Boyd MR,Philpot RM

    更新日期：1982-11-01 00:00:00