Comparison of the ability of dopamine receptor agonists to inhibit forskolin-stimulated adenosine 3'5'-cyclic monophosphate (cAMP) accumulation via D2L (long isoform) and D3 receptors expressed in Chinese hamster ovary (CHO) cells.

Abstract:

:The pharmacological properties of the human D2L (long isoform) and rat D3 dopamine receptors in functional assays were examined. A range of dopamine agonists were assessed for their ability to inhibit adenosine 3'5'-cyclic monophosphate (cAMP) accumulation via the two receptors expressed stably in Chinese hamster ovary cells. Dopamine caused a significantly greater maximal inhibition (P < 0.05) of cAMP accumulation via the D2L receptor (approximately 70%) as compared to the D3 receptor (approximately 50%). The pattern of agonist effects was different at the two receptors. The absolute and relative potencies for inhibition of cAMP accumulation were different for a range of agonists acting at the two receptors. Similarly, the maximal inhibitions achieved by a range of agonists were different for the two receptors.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Hall DA,Strange PG

doi

10.1016/s0006-2952(99)00101-x

subject

Has Abstract

pub_date

1999-07-15 00:00:00

pages

285-9

issue

2

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(99)00101-X

journal_volume

58

pub_type

杂志文章
  • Inhibition of cytochrome P-450p (P450IIIA1) gene expression during liver regeneration from two-thirds hepatectomy in the rat.

    abstract::Regenerating liver from partial hepatectomy (HPX) is known to exhibit a strong and transient deficiency in both spectrally detectable microsomal cytochrome P-450 (P-450) and related monooxygenase activities. Male Wistar rats (250-300 g) were HPX or sham operated and liver was excised at different times after operation...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90705-8

    authors: Marie IJ,Dalet C,Blanchard JM,Astre C,Szawlowski A,Saint Aubert B,Joyeux H,Maurel P

    更新日期:1988-09-15 00:00:00

  • Serine protease inhibition and mitochondrial dysfunction associated with cisplatin resistance in human tumor cell lines: targets for therapy.

    abstract::Indicators of mitochondrial function were studied in two different cell culture models of cis-diamminedichloroplatinum-II (CDDP) resistance: the intrinsically resistant human ovarian cancer cell line CI-80-13S, and resistant clones (HeLa-S1a and HeLa-S1b) generated by stable expression of the serine protease inhibitor...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)00015-4

    authors: Dong Y,Berners-Price SJ,Thorburn DR,Antalis T,Dickinson J,Hurst T,Qiu L,Khoo SK,Parsons PG

    更新日期:1997-06-01 00:00:00

  • Docosahexaenoic acid inhibits insulin-induced activation of sterol regulatory-element binding protein 1 and cyclooxygenase-2 expression through upregulation of SIRT1 in human colon epithelial cells.

    abstract::Multiple lines of compelling evidence from clinical and population-based studies support that hyperinsulinemia often accompanying obesity-associated insulin insensitivity promotes colon carcinogenesis. Insulin can acetylate, thereby activating sterol regulator element-binding protein 1 (SREBP-1), a prime transcription...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.08.030

    authors: Song NY,Na HK,Baek JH,Surh YJ

    更新日期:2014-11-01 00:00:00

  • Selectivity of the molecular chaperone-specific immunosuppressive agent 15-deoxyspergualin: modulation of Hsc70 ATPase activity without compromising DnaJ chaperone interactions.

    abstract::The immunosuppressive and cytostatic agent 15-deoxyspergualin (DSG) binds to the Hsc70 class of molecular chaperones with a K(D) = 4 microM. Because Hsc70s represent a diverse group of cellular effectors and because Hsc70 function frequently requires a DnaJ molecular chaperone, the specificity of DSG for different Hsc...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(98)00376-1

    authors: Brodsky JL

    更新日期:1999-04-15 00:00:00

  • Catecholamines and the kinetics of lipolysis in isolated rat adipocytes. Statistical analysis and handling of day-to-day variability in dose-response curves: a general procedure for assessing and manipulating dose-response data.

    abstract::(1) As a first step in studying the kinetics of the lipolytic system of rat adipocytes, the day-to-day variation between dose-response curves has been analysed. (2) Methods are described for the evaluation of large quantities of data relating noradrenaline to lipolysis. (3) A 'clustering' technique is presented which ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90455-5

    authors: Davies JI,Cooper DM,Everett D

    更新日期:1982-03-01 00:00:00

  • In vivo and in vitro effects of cyclosporin A on glucose transport by soleus muscles of mice.

    abstract::The effect of cyclosporin A (CyA) on 2-deoxyglucose (2DG) uptake by soleus muscles of ICR mice was studied in vivo and in vitro. The basal and insulin-stimulated uptakes of 2DG by the muscles as well as the plasma insulin level were significantly decreased by the in vivo treatment of mice with 20 mg/kg/day of CyA for ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90202-t

    authors: Ikeuchi M,Kida K,Goto Y,Kaino Y,Matsuda H

    更新日期:1992-04-01 00:00:00

  • Effect of culture conditions on the expression and function of Bsep, Mrp2, and Mdr1a/b in sandwich-cultured rat hepatocytes.

    abstract::Rat hepatocytes cultured in a sandwich configuration form functional canalicular networks. The influence of extracellular matrix configuration, medium composition, and confluency on the expression and function of Bsep, Mrp2, and Mdr1a/b in sandwich-cultured (SC) rat hepatocytes was examined. Primary rat hepatocytes we...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.02.004

    authors: Turncliff RZ,Tian X,Brouwer KL

    更新日期:2006-05-14 00:00:00

  • Similar pyruvate kinase modifications in glioblastoma cells by 7β-hydroxycholesterol and glutamine withdrawal.

    abstract::Oxysterols possess anti-proliferative properties that may be used with much effect in the treatment of cancer. We have demonstrated previously that 7 beta-hydroxycholesterol (7b-HC) provokes both metabolic stress, as witnessed by AMPK activation, and changes in lipid raft composition in C6 glioblastoma cells. These ob...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2013.03.012

    authors: de Weille J,Fabre C,Gaven C,Bakalara N

    更新日期:2013-07-01 00:00:00

  • A water-soluble derivative of prazosin prazosinamine hydrochloride [1-(4'-amino-6',7'-dimethoxyquinazolin-2'-yl)-4-(6''-aminohexanoyl) piperazine hydrochloride], reversibly inhibits the calcium-mobilizing action of alpha 1-adrenergic agonists in the perfu

    abstract::A newly-synthesized derivative of prazosin, prazosinamine hydrochloride, was examined for its ability to antagonize the interaction of the alpha 1-adrenergic agonist phenylephrine with liver cells. Using a Ca2--selective electrode to measure changes in perfusate Ca2+ concentration, prazosinamine was found to be as eff...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90040-2

    authors: Armarego WL,Altin JG,Weir RC,Bygrave FL

    更新日期:1987-05-15 00:00:00

  • Inverse gene expression patterns for macrophage activating hepatotoxicants and peroxisome proliferators in rat liver.

    abstract::Macrophage activation contributes to adverse effects produced by a number of hepatotoxic compounds. Transcriptional profiles elicited by two macrophage activators, LPS and zymosan A, were compared to those produced by 100 paradigm compounds (mostly hepatotoxicants) using cDNA microarrays. Several hepatotoxicants previ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2004.01.029

    authors: McMillian M,Nie AY,Parker JB,Leone A,Kemmerer M,Bryant S,Herlich J,Yieh L,Bittner A,Liu X,Wan J,Johnson MD

    更新日期:2004-06-01 00:00:00

  • Activation of 6-aminochrysene to genotoxic products by different forms of rat liver cytochrome P450 in an O-acetyltransferase-overexpressing Salmonella typhimurium strain (NM2009).

    abstract::Metabolic activation of a potent mutagen, 6-aminochrysene, to genotoxic products in a newly developed tester strain, Salmonella typhimurium NM2009, was studied in a rat liver microsomal monooxygenase system containing cytochrome P450 (P450). Since the tester strain was constructed by introducing an O-acetyltransferase...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90123-z

    authors: Yamazaki H,Shimada T

    更新日期:1992-09-01 00:00:00

  • 5,10-Dideazatetrahydrofolic acid reduces toxicity and deoxyadenosine triphosphate pool, expansion in cultured L1210 cells treated with inhibitors of thymidylate synthase.

    abstract::5,10-Dideazatetrahydrofolic acid (DDATHF) reduces de nova purine biosynthesis by inhibiting glycinamide ribonucleotide transformylase. ICI D1964 and CB3717 are folate-based inhibitors of thymidylate synthase (TS). Fluorodeoxyuridine (FdUrd) following metabolism to FdUMP also inhibits TS. In cultured L1210 cells DDATHF...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)00458-x

    authors: Chong LK,Tattersall MH

    更新日期:1995-03-15 00:00:00

  • MZF1 possesses a repressively regulatory function in ERCC1 expression.

    abstract::ERCC1 is a critical gene within the nucleotide excision repair pathway. Overexpression of ERCC1 through promoter-mediating transcriptional regulation is associated with repair of cisplatin-induced DNA damage and clinical resistance to platinum-chemotherapy. Several transcriptional repressors and activators within the ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2005.12.015

    authors: Yan QW,Reed E,Zhong XS,Thornton K,Guo Y,Yu JJ

    更新日期:2006-03-14 00:00:00

  • Influence of delta 9-tetrahydrocannabinol on expression of histone and ribosomal genes in normal and transformed human cells.

    abstract::The influence of delta 9-tetrahydrocannabinol (delta 9-THC) on the cellular levels of histone mRNAs and ribosomal RNAs was examined in several normal and transformed human cell lines--HeLa S3 cells, WI-38 human diploid fibroblasts, SV40-transformed WI-38 cells, and A549 lung carcinoma cells. RNA sequences were quantit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90510-0

    authors: Green LG,Stein JL,Stein GS

    更新日期:1984-04-01 00:00:00

  • Microglia-neuron interactions in the models of neuropathic pain.

    abstract::Chronic pain is a debilitating condition that often emerges as a clinical symptom of inflammatory diseases. It has therefore been widely accepted that the immune system critically contributes to the pathology of chronic pain. Microglia, a type of immune cell in the central nervous system, has attracted researchers' at...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2019.08.016

    authors: Tozaki-Saitoh H,Tsuda M

    更新日期:2019-11-01 00:00:00

  • The mitochondrial uncoupler dicumarol disrupts the MTT assay.

    abstract::Dicumarol is routinely added to the 3-[4,4-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay to study the role of NAD(P)H:quinone oxido-reductase in drug activation and detoxification. We assessed the direct impact of dicumarol (a mitochondrial uncoupler) on the MTT assay. Mouse mammary tumor (EMT6) an...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(03)00240-5

    authors: Collier AC,Pritsos CA

    更新日期:2003-07-15 00:00:00

  • Depression of constitutive murine cytochromes P450 by staphylococcal enterotoxin B.

    abstract::Most in vivo studies demonstrating decreased activities of hepatic cytochromes P450 with inflammation have used Gram-negative bacterial lipopolysaccharide (LPS) as the inflammatory stimulant. But products of Gram-positive bacteria, such as staphylococcal enterotoxin B (SEB), also stimulate inflammatory mediators, albe...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(00)00250-1

    authors: Shedlofsky SI,Tosheva RT,Snawder JA

    更新日期:2000-05-15 00:00:00

  • RACking up ceramide-induced islet β-cell dysfunction.

    abstract::The International Diabetes Federation predicts that by 2045 the number of individuals afflicted with diabetes will increase to 629 million. Furthermore, ∼352 million individuals with impaired glucose tolerance are at increased risk for developing diabetes. Several mechanisms have been proposed for the onset of metabol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2018.04.026

    authors: Kowluru A,Kowluru RA

    更新日期:2018-08-01 00:00:00

  • Reversal of chemoresistance and enhancement of apoptosis by statins through down-regulation of the NF-kappaB pathway.

    abstract::We recently found that simvastatin can modulate the nuclear factor-kappaB (NF-kappaB) activation pathway, but whether other statins have similar effects to those of simvastatin is unknown. Therefore, we evaluated the effect six different statins on TNF-induced NF-kappaB activation in human myeloid leukemia cells. We t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2007.10.010

    authors: Ahn KS,Sethi G,Aggarwal BB

    更新日期:2008-02-15 00:00:00

  • Effects of chronic administration of the peroxisome proliferator, clofibrate, on cytosolic acetyl-CoA hydrolase in rat liver.

    abstract::The hypolipidemic drug ethyl chlorophenoxyisobutyrate (clofibrate) is known to induce peroxisome proliferation and to be carcinogenic after long term administration to rats and mice. We examined the effects of treatment with this drug for periods of up to 18 months on cytosolic ATP-stimulated and ADP-inhibited acetyl-...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90038-x

    authors: Nakanishi Y,Okamoto K,Isohashi F

    更新日期:1993-04-06 00:00:00

  • Metabolic alterations by clofibric acid in the formation of molecular species of phosphatidylcholine in rat liver.

    abstract::The mechanism by which p-chlorophenoxyisobutyric acid (clofibric acid) induces striking changes in the proportion of the molecular species of phosphatidylcholine (PC) in rat liver was studied. Treatment of rats with clofibric acid strikingly increased the content of 1-palmitoyl-2-oleoyl (16:0-18:1) PC, but decreased t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(01)00735-3

    authors: Mizuguchi H,Kudo N,Kawashima Y

    更新日期:2001-10-01 00:00:00

  • Regulatory effects of zinc and copper on the calcium transport system in rat liver nuclei. Relation to SH groups in the releasing mechanism.

    abstract::In isolated hepatic nuclei, the heavy metals Zn2+ and Cu2+ (10 microM) inhibited Ca2+ uptake and caused a prompt release of Ca2+ from preloaded nuclei in a concentration-dependent manner, with Zn2+ being more effective than Cu2+. The sulfhydryl group reducing agent dithiothreitol (DTT) protected the nuclei from the ef...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90180-5

    authors: Yamaguchi M

    更新日期:1993-02-24 00:00:00

  • Formation of tetrahydro-beta-carbolines in human saliva.

    abstract::When human saliva obtained after cigarette smoking was incubated in the presence of tryptamine, the formation of 1,2,3,4-tetrahydro-beta-carboline (TBC) and 1-methyl-1,2,3,4-tetrahydro-beta-carboline (MTBC) was observed in a short time. After incubation with tryptamine (2.5 micrograms/microliter) for 10 min, the conce...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)02068-3

    authors: Tsuchiya H,Ohtani S,Yamada K,Tajima K,Sato M

    更新日期:1995-12-22 00:00:00

  • Paracetamol, 3-monoalkyl- and 3,5-dialkyl derivatives. Comparison of their microsomal cytochrome P-450 dependent oxidation and toxicity in freshly isolated hepatocytes.

    abstract::The effects of 3-monoalkyl- and 3,5-dialkyl-substitution on the cytotoxicity of paracetamol (PAR) in rat hepatocytes was studied. PAR is known to be bioactivated by the hepatic microsomal cytochrome P-450 containing a mixed-function oxidase system presumably to N-acetyl-para-benzoquinone imine (NAPQI), a reactive meta...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90653-2

    authors: Van De Straat R,De Vries J,Kulkens T,Debets AJ,Vermeulen NP

    更新日期:1986-11-01 00:00:00

  • Effect of the antidepressant minaprine on both forms of monoamine oxidase in the rat.

    abstract::The antidepressant minaprine (3-(2-morpholino-ethylamino) 4-methyl 6-phenyl pyridazine, dihydrochloride) and its main metabolites were examined for their monoamine oxidase (MAO) inhibitory effects in the rat. In our experimental conditions, minaprine displayed in vitro a very weak affinity for brain MAO A and B with I...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90085-7

    authors: Kan JP,Mouget-Goniot C,Worms P,Biziere K

    更新日期:1986-03-15 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

    doi:10.1016/0006-2952(90)90212-4

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

    更新日期:1990-03-01 00:00:00

  • My close encounter with GABA(B) receptors.

    abstract::In this review, I summarize the sequence of events involved in characterizing the functional role of GABA(B) receptors in the CNS and their involvement in synaptic transmission. The story was launched with the realization that baclofen was a selective agonist of GABA(B) receptors. This lead to the discovery in the CNS...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2004.07.024

    authors: Nicoll RA

    更新日期:2004-10-15 00:00:00

  • High sensitivity of leukemic peripheral blood lymphocytes to triethyllead action.

    abstract::In a previous study we reported that triethyllead (Et3Pb+) inhibits cell proliferation of normal human lymphocytes. To further characterize this interaction, we studied herein the effects of Et3Pb+ on the cell viability of normal and leukemic human lymphocytes and analysed the expression and dynamics of the monomer/po...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)00435-8

    authors: Stiakaki E,Stournaras C,Dimitriou H,Kalmanti M

    更新日期:1997-12-15 00:00:00

  • Enzymatic basis of the debrisoquine/sparteine-type genetic polymorphism of drug oxidation. Characterization of bufuralol 1'-hydroxylation in liver microsomes of in vivo phenotyped carriers of the genetic deficiency.

    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

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90573-9

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

    更新日期:1987-12-01 00:00:00

  • Enhancement by beraprost sodium, a stable analogue of prostacyclin, in thrombomodulin expression on membrane surface of cultured vascular endothelial cells via increase in cyclic AMP level.

    abstract::Prostacyclin and beraprost sodium (beraprost), a stable analogue of prostacyclin, increased cyclic AMP (cAMP) levels of cultured human umbilical vein endothelial cells (HUVEC) in a concentration-dependent manner. The elevation of cAMP by beraprost was sustained longer than that by prostacyclin. The expression of throm...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90651-k

    authors: Kainoh M,Maruyama I,Nishio S,Nakadate T

    更新日期:1991-04-15 00:00:00