当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Effects of full and partial beta-adrenergic agonists and antagonists on human lung adenylate cyclase.

Effects of full and partial beta-adrenergic agonists and antagonists on human lung adenylate cyclase.

Abstract：

:The beta-adrenergic stimulation of adenylate cyclase in membranes from human lung was compared to that of adenylate cyclase in membranes with a majority of beta 2-adrenergic receptors (from rat lung) and in membranes with a homogeneous population of beta 2-adrenergic receptors (from rat erythrocytes and reticulocytes). In terms of adenylate cyclase stimulation, three full agonists (isoproterenol, epinephrine and norepinephrine), four partial agonists (procaterol, salbutamol, fenoterol and zinterol), and four antagonists (propranolol, metoprolol, atenolol and practolol) were tested. The potency (Kact or Ki) of the eleven beta-adrenergic agents, and the Hill coefficient (of 1) for the four antagonists tested indicated that the activation of human lung adenylate cyclase occurred through receptors of the beta 2-subtype only. Partial beta-adrenergic agonists were efficiently discriminated by the human lung preparation, as shown by distinct intrinsic activities. The mediocre efficacy and the relatively low potency of all beta-adrenergic agonists on adenylate cyclase suggested a relatively low density of beta 2-adrenergic receptors, as compared to the enzyme density.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Delhaye M,Taton G,Camus JC,Chatelain P,Robberecht P,Waelbroeck M,Christophe J

doi

10.1016/0006-2952(83)90046-1

subject

Has Abstract

pub_date

1983-06-15 00:00:00

pages

1831-5

issue

12

eissn

0006-2952

issn

1873-2968

pii

0006-2952(83)90046-1

journal_volume

32

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • Zinc protoporphyrin suppresses cancer cell viability through a heme oxygenase-1-independent mechanism: the involvement of the Wnt/β-catenin signaling pathway.

    abstract：:Zinc protoporphyrin (ZnPP), a known inhibitor of heme oxygenase-1 (HO-1), has been reported to have anticancer activity in both in vitro and in vivo model systems. While the mechanisms of ZnPP's anticancer activity remain to be elucidated, it is generally believed that ZnPP suppresses tumor growth through inhibition o...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2013.03.011

    authors： Wang S,Avery JE,Hannafon BN,Lind SE,Ding WQ

    更新日期：2013-06-01 00:00:00

  • Inhibitions of acid secretion by E3810 and omeprazole, and their reversal by glutathione.

    abstract：:A substituted benzimidazole ([4-(3-methoxypropoxy)-3-methylpyridine-2-yl]methylsulfinyl)- 1H-benzimidazole sodium salt (E3810), is a gastric proton pump (H+, K(+)-ATPase) inhibitor. E3810 and omeprazole inhibited acid accumulation dose dependently as measured with aminopyrine uptake in isolated rabbit gastric glands, ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90719-l

    authors： Fujisaki H,Shibata H,Oketani K,Murakami M,Fujimoto M,Wakabayashi T,Yamatsu I,Yamaguchi M,Sakai H,Takeguchi N

    更新日期：1991-07-05 00:00:00

  • Glipentide and glucose metabolism in isolated rat hepatocytes.

    abstract：:Glipentide, a second generation sulfonylurea, raised the cellular concentration of fructose 2,6-bisphosphate in isolated rat hepatocytes. Parallel to accumulating this regulatory metabolite, glipentide inhibited basal gluconeogenesis and increased the rate of L-lactate production, as well as the metabolic flux through...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(88)90317-6

    authors： López-Alarcón L,Berbil-Bautista PR,Guijarro C,Felíu JE

    更新日期：1988-08-15 00:00:00

  • Potentiation by febrifugine of host defense in mice against Plasmodium berghei NK65.

    abstract：:The effect of febrifugine, the main alkaloidal constituent of an antimalarial crude drug, Dichroa febrifuga Lour., on protective immunity in mice infected with erythrocytic stage Plasmodium berghei NK65 was investigated. Febrifugine was administered orally, at a dose of 1 mg/kg/day, to mice before and/or after they we...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00244-0

    authors： Murata K,Takano F,Fushiya S,Oshima Y

    更新日期：1999-11-15 00:00:00

  • Induction of human breast cancer cell apoptosis from G2/M preceded by stimulation into the cell cycle by Z-1,1-dichloro-2,3-diphenylcyclopropane.

    abstract：:We have shown previously that Z-1,1-dichloro-2,3-diphenylcyclopropane (a.k.a. Analog II, A(II)) inhibits human breast cancer cell proliferation regardless of estrogen receptor status or estrogen sensitivity, and that its cellular targets include microtubules. In the present study, we investigated the apoptosis-inducin...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(98)00289-5

    authors： Balachandran R,ter Haar E,Yalowich JC,Welsh MJ,Grant SG,Day BW

    更新日期：1999-01-01 00:00:00

  • Development of resistance to photodynamic therapy (PDT) in human breast cancer cells is photosensitizer-dependent: Possible mechanisms and approaches for overcoming PDT-resistance.

    abstract：:Here we report on the induction of resistance to photodynamic therapy (PDT) in the ABCG2-high human breast cancer cell line MA11 after repetitive PDT, using either Pheophorbide A (PhA) or di-sulphonated meso-tetraphenylchlorin (TPCS2a) as photosensitizer. Resistance to PhA-PDT was associated with enhanced expression o...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2017.08.002

    authors： Olsen CE,Weyergang A,Edwards VT,Berg K,Brech A,Weisheit S,Høgset A,Selbo PK

    更新日期：2017-11-15 00:00:00

  • Stereoselective metabolism of 3-isopropyl-5-(1-naphthoxymethyl)oxazolidine, a prodrug of propranolol.

    abstract：:This investigation suggests that the oxazolidine derivative of propranolol is a prodrug which is hydrolysed stereoselectively to propranolol by hepatic post-mitochondrial supernatant. The (S)-form of the prodrug is more stable in the biological system than its (R)-form. ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90113-j

    authors： Kamal A,Rao AB,Rao MV

    更新日期：1991-05-01 00:00:00

  • Multiple high-affinity cAMP-phosphodiesterases in human T-lymphocytes.

    abstract：:Cyclic nucleotide phosphodiesterases (PDEs) are the only enzymes that inactivate intracellular cyclic AMP (cAMP). Because the functions of T-lymphocytes are modulated by cAMP levels, the isozymes of PDE in these cells are potential targets for new drugs designed to modify the body's immunity through selective alterati...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90047-9

    authors： Robicsek SA,Blanchard DK,Djeu JY,Krzanowski JJ,Szentivanyi A,Polson JB

    更新日期：1991-07-25 00:00:00

  • Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure.

    abstract：:The effects of two competitive antagonists and two allosteric ligands on the rate of dissociation of [3H]N-methylscopolamine ([3H]NMS) were studied at atrial muscarinic acetylcholine M2 receptors by the technique of "infinite dilution." The dissociation rate for [3H]NMS, initiated by diluting the incubation mixture in...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(96)00814-3

    authors： Christopoulos A,Lanzafame A,Ziegler A,Mitchelson F

    更新日期：1997-03-21 00:00:00

  • Azatoxin derivatives with potent and selective action on topoisomerase II.

    abstract：:Azatoxin was rationally designed as a DNA topoisomerase II (top2) inhibitor [Leteurtre et al., Cancer Res 52: 4478-4483, 1992] and was also found to inhibit tubulin polymerization. Its cytotoxicity is due to action on tubulin at lower concentrations and on top2 at higher concentrations. At intermediate concentrations,...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)00047-4

    authors： Leteurtre F,Sackett DL,Madalengoitia J,Kohlhagen G,MacDonald T,Hamel E,Paull KD,Pommier Y

    更新日期：1995-05-11 00:00:00

  • Inhibition of thioredoxin reductase by alantolactone prompts oxidative stress-mediated apoptosis of HeLa cells.

    abstract：:The mammalian thioredoxin reductase (TrxR) isoenzymes, TrxR1 in cytosol or nucleus, TrxR2 in mitochondria, and TrxR3 in testis, are essential seleno-flavoenzymes with a conserved penultimate selenocysteine (Sec) residue at the C-terminus, and have attracted increasing interests as potential targets for development of ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2015.12.004

    authors： Zhang J,Li Y,Duan D,Yao J,Gao K,Fang J

    更新日期：2016-02-15 00:00:00

  • Differential inhibition of human neutrophil functions. Role of cyclic AMP-specific, cyclic GMP-insensitive phosphodiesterase.

    abstract：:Multiple molecular forms of cyclic nucleotide phosphodiesterase have been characterized in various tissues and cells according to their substrate specificity, intracellular location, and calmodulin dependence. The purpose of this study was to evaluate the possible involvement of different molecular forms of phosphodie...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90304-4

    authors： Wright CD,Kuipers PJ,Kobylarz-Singer D,Devall LJ,Klinkefus BA,Weishaar RE

    更新日期：1990-08-15 00:00:00

  • Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.

    abstract：:Activation of the P2Y(1) nucleotide receptor in platelets by ADP causes changes in shape and aggregation, mediated by activation of phospholipase C (PLC). Recently, MRS2500(2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate) was introduced as a highly potent and selective antagonist for this rece...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2004.06.026

    authors： Cattaneo M,Lecchi A,Ohno M,Joshi BV,Besada P,Tchilibon S,Lombardi R,Bischofberger N,Harden TK,Jacobson KA

    更新日期：2004-11-15 00:00:00

  • Changes in methionine metabolism induced by D-galactosamine in isolated rat hepatocytes.

    abstract：:We studied several steps of methionine metabolism in isolated rat hepatocytes both with and without the presence of a hepatotoxic agent (D-galactosamine). By use of selective labelling either on methyl or on carboxyl groups, we showed that intracellular methionine is used preferentially for the methylation of phosphol...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(86)90699-4

    authors： Ozturk M,Lemonnier F,Cresteil D,Lemonnier A

    更新日期：1986-12-01 00:00:00

  • Differential signaling of human Mel1a and Mel1b melatonin receptors through the cyclic guanosine 3'-5'-monophosphate pathway.

    abstract：:Cyclic guanosine 3'-5'-monophosphate (cGMP) has recently been shown to constitute a second messenger for Xenopus laevis melatonin Mel1c receptors. To verify whether cGMP levels are also modulated by mammalian melatonin receptors, we cloned the genes encoding the human Mel1a and Mel1b receptor subtypes and expressed th...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00134-3

    authors： Petit L,Lacroix I,de Coppet P,Strosberg AD,Jockers R

    更新日期：1999-08-15 00:00:00

  • The interactions of apamin and tetraethylammonium are differentially affected by single mutations in the pore mouth of small conductance calcium-activated potassium (SK) channels.

    abstract：:Valine residues in the pore region of SK2 (V366) and SK3 (V520) were replaced by either an alanine or a phenylalanine to evaluate the impact on the interactions with the allosteric blocker apamin. Unlike TEA which showed high sensitivity to phenylalanine mutated channels, the binding affinity of apamin to the phenylal...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2012.12.015

    authors： Dilly S,Philippart F,Lamy C,Poncin S,Snyders D,Seutin V,Liégeois JF

    更新日期：2013-02-15 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

  • Modification of the plasma clearance and liver uptake of steroid ester-conjugated oligodeoxynucleotides by association with (lactosylated) low-density lipoprotein.

    abstract：:Low-density lipoprotein (LDL) has been proposed as carrier for the selective delivery of anticancer drugs to tumor cells. We reported earlier the association of several lipidic steroid-conjugated anticancer oligodeoxynucleotides (ODNs) with LDL. In the present study, we determined the stability of these complexes. Whe...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00243-4

    authors： Rump ET,de Vrueh RL,Manoharan M,Waarlo IH,van Veghel R,Biessen EA,van Berkel TJ,Bijsterbosch MK

    更新日期：2000-06-01 00:00:00

  • Characterisation of cytosolic phospholipase A2 as mediator of the enhanced arachidonic acid release from dimethyl sulphoxide differentiated U937 cells.

    abstract：:Studies were performed to characterise the phospholipase A2 (PLA2) responsible for the greatly increased capacity to release arachidonic acid (AA) of dimethyl sulphoxide (DMSO) differentiated U937 monocytic cells compared to undifferentiated cells (18-fold increase in response to Ca2+ ionophore A23187). Cytosolic PLA2...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)02084-5

    authors： Withnall MT,Pennington A,Wiseman D

    更新日期：1995-11-27 00:00:00

  • Regulation of p53: intricate loops and delicate balances.

    abstract：:The p53 tumor suppressor protein provides a major anti-cancer defense mechanism, as underscored by the fact that the p53 gene is the most frequent target for genetic alterations in human cancer. Recent work has led to the realization that p53 lies at the hub of a very complex network of signaling pathways, which integ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,收录出版

    doi：10.1016/s0006-2952(02)01149-8

    authors： Oren M,Damalas A,Gottlieb T,Michael D,Taplick J,Leal JF,Maya R,Moas M,Seger R,Taya Y,Ben-Ze'ev A

    更新日期：2002-09-01 00:00:00

  • Inhibition of indoleamine 2,3-dioxygenase activity in IFN-gamma stimulated astroglioma cells decreases intracellular NAD levels.

    abstract：:Astroglia provide essential metabolic and neurotropic support to cells within the CNS and participate in the cellular immune response with microglia/macrophages following activation by the pro-inflammatory cytokine IFN-gamma. Activation of glial cells results in local oxidative stress and induction of a number of prot...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(03)00464-7

    authors： Grant R,Kapoor V

    更新日期：2003-09-15 00:00:00

  • Site-specific DNA damage induced by sulfite in the presence of cobalt(II) ion. Role of sulfate radical.

    abstract：:The reactivities of sulfite (SO23-) with DNA in the presence of metal ions were investigated by a DNA sequencing technique using 32P-labeled DNA fragments obtained from human c-Ha-ras-1 protooncogene. Sulfite caused DNA damage in the presence of Co2+, Cu2+ and Mn2+, although sulfite alone or metal ion alone did not. T...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90119-6

    authors： Kawanishi S,Yamamoto K,Inoue S

    更新日期：1989-10-15 00:00:00

  • From astrocytes to satellite glial cells and back: A 25 year-long journey through the purinergic modulation of glial functions in pain and more.

    abstract：:Fundamental progresses have been made in pain research with a comprehensive understanding of the neuronal pathways which convey painful sensations from the periphery and viscera to the central nervous system and of the descending modulating pathways. Nevertheless, many patients still suffer from various painful condit...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2020.114397

    authors： Ceruti S

    更新日期：2020-12-28 00:00:00

  • Inhibition of nitric oxide-guanylate cyclase-dependent and -independent signaling contributes to impairment of beta-adrenergic vasorelaxations by cyclosporine.

    abstract：:This study investigated the role of endothelium- and smooth muscle-dependent mechanisms in the interaction of cyclosporine (CyA), an immunosuppressant drug, with beta-adrenoceptor (isoprenaline)-mediated relaxations in isolated rat aortas precontracted with phenylephrine. CyA effects were assessed in the absence and p...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2006.10.015

    authors： El-Mas MM,Sharabi FM,El-Gowilly SM,El-Din MM

    更新日期：2007-02-01 00:00:00

  • Thermodynamics of A2B adenosine receptor binding discriminates agonistic from antagonistic behaviour.

    abstract：:Thermodynamic parameters DeltaG degrees , DeltaH degrees and DeltaS degrees of the binding equilibrium of 12 ligands (six agonists and six antagonists) to the A(2B) adenosine receptor subtype have been determined by affinity measurements carried out on HEK 293 cells stably transfected with human A(2B) adenosine recept...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2007.09.003

    authors： Gessi S,Fogli E,Sacchetto V,Varani K,Merighi S,Leung E,Lennan SM,Borea PA

    更新日期：2008-01-15 00:00:00

  • Covalent coupling of doxorubicin in protein microspheres is a major determinant of tumour drug disposition.

    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

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90123-m

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

    更新日期：1991-06-15 00:00:00

  • Increased glutathione peroxidase activity in human blood mononuclear cells upon in vitro incubation with n-3 fatty acids.

    abstract：:Fish oil-enriched diets have been shown to increase the n-3 polyunsaturated fatty acid (PUFA) content of cell membranes, in vivo, and to simultaneously enhance the glutathione peroxidase (glutathione: H2O2 oxidoreductase, EC 1.11.1.9) (GSH-Px) activity of platelets and erythrocytes both in animals and humans. The pres...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)90329-8

    authors： Joulain C,Prigent AF,Némoz G,Lagarde M

    更新日期：1994-04-20 00:00:00

  • Src, N-methyl-D-aspartate (NMDA) receptors, and synaptic plasticity.

    abstract：:The protein tyrosine kinase Src is expressed widely in the central nervous system and is abundant in neurons. Over the past several years, evidence has accumulated showing that one function of Src is to regulate the activity of N-methyl-D-aspartate (NMDA) receptors and other ion channels. NMDA receptors are a principa...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/s0006-2952(98)00124-5

    authors： Salter MW

    更新日期：1998-10-01 00:00:00

  • Molecular characterization of functional UDP-glucuronosyltransferases 1A and 2B in common marmosets.

    abstract：:UDP-glucuronosyltransferases (UGTs) are essential drug-conjugation enzymes that metabolize a variety of endobiotic and xenobiotic substrates. The molecular characteristics of UGTs have been extensively investigated in humans, but remain to be investigated in common marmosets, a nonhuman primate species widely used in ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2019.113748

    authors： Uno Y,Uehara S,Inoue T,Kawamura S,Murayama N,Nishikawa M,Ikushiro S,Sasaki E,Yamazaki H

    更新日期：2020-02-01 00:00:00

  • Explanation of the non-hyperbolic kinetics of the glutathione S-transferases by the simplest steady-state random sequential Bi Bi mechanism.

    abstract：:We have demonstrated that the simplest steady-state random sequential Bi Bi mechanism is sufficient to explain the previously reported non-hyperbolic kinetics of glutathione S-transferase 3-3 [Pabst MJ et al., J Biol Chem 249: 7140-7150, 1974; Jakobson I et al., Biochem J 177: 861-868, 1979]. The metabolism of 1-chlor...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90621-q

    authors： Ivanetich KM,Goold RD,Sikakana CN

    更新日期：1990-06-15 00:00:00