Atypical characteristics of the beta-adrenoceptor mediating cyclic AMP generation and lipolysis in the rat adipocyte.

Abstract:

:The characteristics of the rat epidydimal adipocyte beta-adrenoceptor have been examined using lipolysis and cyclic AMP accumulation in adipocytes as well as adenylate cyclase activity in fat cell membranes. The pA2 values corrected for binding to bovine serum albumin of the selective antagonists betaxolol (beta 1-selective) and ICI 118.551 (beta 2-selective) against noradrenaline or fenoterol-stimulated lipolysis were indicative of an atypical beta-adrenoceptor associated with the lipolytic response. Antagonism of isoprenaline-stimulated cyclic AMP accumulation in whole cells and adenylate cyclase activity in membranes yielded pA2 values to betaxolol, ICI 118.551 and (-)-propranolol, which suggested that the atypical beta-adrenoceptor was coupled to adenylate cyclase. Comparisons of the Ki values obtained in binding studies using [125I]-cyanopindolol with pA2 values obtained in adenylate cyclase experiments suggest that the typical beta 1-receptor identified with radioligand binding studies is not the only receptor site mediating stimulation of adenylate cyclase activity and lipolysis.

journal_name

Br J Pharmacol

authors

Bojanic D,Jansen JD,Nahorski SR,Zaagsma J

subject

Has Abstract

pub_date

1985-01-01 00:00:00

pages

131-7

issue

1

eissn

0007-1188

issn

1476-5381

journal_volume

84

pub_type

杂志文章
  • Evidence that the accumulation of 5-hydroxytryptamine in the liver but not in the brain may cause the hypoglycaemia induced by 5-hydroxytryptophan.

    abstract::Experiments were undertaken to determine whether the site of the hypoglycaemic action of 5-hydroxytryptophan (5-HTP), a direct precursor of 5-hydroxytryptamine (5-HT), was in the central nervous system or in the liver. The fall in blood glucose followed the rapid increase in the amount of 5-HT both in the brain and li...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1985.tb10553.x

    authors: Endo Y

    更新日期:1985-07-01 00:00:00

  • Effects of ATP-sensitive K+ channel blockers on the action potential shortening in hypoxic and ischaemic myocardium.

    abstract::1. In order to determine whether activation of adenosine triphosphate (ATP)-sensitive K+ channels exclusively explains the hypoxia- and ischaemia-induced action potential shortening, effects of tolbutamide and glibenclamide on changes in action potential duration (APD) during hypoxia, metabolic blockade or experimenta...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12294.x

    authors: Nakaya H,Takeda Y,Tohse N,Kanno M

    更新日期:1991-05-01 00:00:00

  • Cannabinoids as therapeutic agents in cardiovascular disease: a tale of passions and illusions.

    abstract::In addition to their classical known effects, such as analgesia, impairment of cognition and learning and appetite enhancement, cannabinoids have also been related to the regulation of cardiovascular responses and implicated in cardiovascular pathology. Elevated levels of endocannabinoids have been related to the extr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707261

    authors: Mendizábal VE,Adler-Graschinsky E

    更新日期:2007-06-01 00:00:00

  • TNF-alpha, inefficient by itself, potentiates IL-1beta-induced PGHS-2 expression in human pulmonary microvascular endothelial cells: requirement of NF-kappaB and p38 MAPK pathways.

    abstract::1: Prostaglandin H synthase-2 (PGHS-2), is an inducible enzyme involved in various inflammatory responses. We established here that interleukin-1beta (IL-1beta) but not tumour necrosis factor-alpha (TNF-alpha) increased its expression in human pulmonary microvascular endothelial cells (HPMEC). However, associated with...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704811

    authors: Said FA,Werts C,Elalamy I,Couetil JP,Jacquemin C,Hatmi M

    更新日期:2002-08-01 00:00:00

  • The effects of evening primrose oil on nerve function and capillarization in streptozotocin-diabetic rats: modulation by the cyclo-oxygenase inhibitor flurbiprofen.

    abstract::1. The aims of this study were first, to examine whether deficits in nerve conduction in streptozotocin-diabetic rats could be reversed by a 10% dietary supplement of evening primrose oil. Second, to determine the time-course of reversal, and third, to assess whether the effects could be blocked by the cyclo-oxygenase...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13716.x

    authors: Cameron NE,Cotter MA,Dines KC,Robertson S,Cox D

    更新日期:1993-08-01 00:00:00

  • Structure and function of midkine as the basis of its pharmacological effects.

    abstract:UNLABELLED:Midkine (MK) is a heparin-binding growth factor or cytokine and forms a small protein family, the other member of which is pleiotrophin. MK enhances survival, migration, cytokine expression, differentiation and other activities of target cells. MK is involved in various physiological processes, such as devel...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.12353

    authors: Muramatsu T

    更新日期:2014-02-01 00:00:00

  • Comparative effects of anti-platelet agents as adjuncts to tissue plasminogen activator in a dog model of occlusive coronary thrombosis.

    abstract::1. This study compares a cyclo-oxygenase inhibitor (aspirin), a 5-HT2 antagonist (ZM170809) and a combined thromboxane synthase inhibitor/receptor antagonist (ZD1542) as adjuncts to tissue plasminogen activator (rt-PA). 2. Application of an anodal current (332 +/- 4.1 microA) to the stenosed left circumflex coronary a...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb13063.x

    authors: McAuliffe SJ,Moors JA,Jones HB

    更新日期:1994-05-01 00:00:00

  • Inhibition of carrageenin-induced rat paw oedema by crotapotin, a polypeptide complexed with phospholipase A2.

    abstract::1. The effect of purified crotapotin, a non-toxic non-enzymatic chaperon protein normally complexed to a phospholipase A2 (PLA2) in South America rattlesnake venom, was studied in the acute inflammatory response induced by carrageenin (1 mg/paw), compound 48/80 (3 micrograms/paw) and 5-hydroxytryptamine (5-HT) (3 micr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb17178.x

    authors: Landucci EC,Antunes E,Donato JL,Faro R,Hyslop S,Marangoni S,Oliveira B,Cirino G,de Nucci G

    更新日期:1995-02-01 00:00:00

  • Retracted: Addition of a single methyl group to a small molecule sodium channel inhibitor introduces a new mode of gating modulation, by L Wang, SG Zellmer, DM Printzenhoff and NA Castle. British Journal of Pharmacology, volume 172(20): 4905-4918, publish

    abstract::The above article, published by the British Journal of Pharmacology in October 2015 (https://bpspubs.onlinelibrary.wiley.com/doi/full/10.1111/bph.13259), has been retracted by agreement between the authors, the journal Editor in Chief and John Wiley & Sons Limited. The retraction has been agreed owing to the discovery...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,撤回出版物

    doi:10.1111/bph.14349

    authors:

    更新日期:2018-07-01 00:00:00

  • The potential health effects of dietary phytoestrogens.

    abstract::Phytoestrogens are plant-derived dietary compounds with structural similarity to 17-β-oestradiol (E2), the primary female sex hormone. This structural similarity to E2 enables phytoestrogens to cause (anti)oestrogenic effects by binding to the oestrogen receptors. The aim of the present review is to present a state-of...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13622

    authors: Rietjens IMCM,Louisse J,Beekmann K

    更新日期:2017-06-01 00:00:00

  • The role of adenosine in the hyperaemic response of the hepatic artery to portal vein occlusion (the 'buffer response').

    abstract::1. Adenosine has been shown to be responsible for the hyperaemic response of the hepatic artery to portal vein occlusion (the hepatic arterial 'buffer response'). 2. The effect of adenosine receptor blockade and of adenosine uptake inhibition on the hepatic arterial response to portal vein occlusion was investigated i...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1990.tb15857.x

    authors: Mathie RT,Alexander B

    更新日期:1990-07-01 00:00:00

  • Targeting TDP-43 proteinopathy with drugs and drug-like small molecules.

    abstract::Following the discovery of the involvement of the ribonucleoprotein TDP-43 in amyotrophic lateral sclerosis (ALS) and frontotemporal lobar degeneration (FTLD), a major research focus has been to develop treatments that can prevent or alleviate these disease conditions. One pharmacological approach has been to use TDP-...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.15148

    authors: Buratti E

    更新日期:2020-05-29 00:00:00

  • Contrasting effects of the imidazol(in)e alpha 2-adrenoceptor agonists, medetomidine, clonidine and UK 14,304 on extraneuronal levels of noradrenaline in the rat frontal cortex: evaluation using in vivo microdialysis and synaptosomal uptake studies.

    abstract::1. In vivo microdialysis in halothane-anaesthetized rats and synaptosomal [3H]-noradrenaline uptake studies in vitro were used to evaluate the effects of imidazole (medetomidine) and imidazoline (clonidine and UK 14,304) alpha 2-adrenoceptor agonists on extraneuronal levels of noradrenaline in the frontal cortex. 2. L...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb14962.x

    authors: Dalley JW,Stanford SC

    更新日期:1995-04-01 00:00:00

  • Modification of blood pressure and nictitating membrane response to sympathetic amines by selective monoamine oxidase inhibitors, types A and B, in the cat.

    abstract::The selective monoamine oxidase (MAO) inhibitors clorgyline, selegiline and AGN 1135 did not cause a change in responses of the cat nictitating membrane to preganglionic sympathetic nerve stimulation at 5 Hz. Both selective MAO-A and MAO-B inhibitors markedly potentiated nictitating membrane contractions in response t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1985.tb08891.x

    authors: Finberg JP,Youdim MB

    更新日期:1985-06-01 00:00:00

  • Methylene blue inhibits function of the 5-HT transporter.

    abstract:BACKGROUND AND PURPOSE:Methylene blue (MB) is commonly employed as a treatment for methaemoglobinaemia, malaria and vasoplegic shock. An increasing number of studies indicate that MB can cause 5-HT toxicity when administered with a 5-HT reuptake inhibitor. MB is a potent inhibitor of monoamine oxidases, but other targe...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01462.x

    authors: Oz M,Isaev D,Lorke DE,Hasan M,Petroianu G,Shippenberg TS

    更新日期:2012-05-01 00:00:00

  • Activity of botulinum toxin type A in cranial dura: implications for treatment of migraine and other headaches.

    abstract:BACKGROUND AND PURPOSE:Although botulinum toxin type A (BoNT/A) is approved for chronic migraine treatment, its mechanism of action is still unknown. Dural neurogenic inflammation (DNI) commonly used to investigate migraine pathophysiology can be evoked by trigeminal pain. Here, we investigated the reactivity of crania...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13366

    authors: Lacković Z,Filipović B,Matak I,Helyes Z

    更新日期:2016-01-01 00:00:00

  • A monobromobimane-based assay to measure the pharmacokinetic profile of reactive sulphide species in blood.

    abstract:BACKGROUND AND PURPOSE:Hydrogen sulphide (H(2)S) is a labile, endogenous metabolite of cysteine, with multiple biological roles. The development of sulphide-based therapies for human diseases will benefit from a reliable method of quantifying H(2)S in blood and tissues. EXPERIMENTAL APPROACH:Concentrations of reactive...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2010.00704.x

    authors: Wintner EA,Deckwerth TL,Langston W,Bengtsson A,Leviten D,Hill P,Insko MA,Dumpit R,VandenEkart E,Toombs CF,Szabo C

    更新日期:2010-06-01 00:00:00

  • The Scar-in-a-Jar: studying potential antifibrotic compounds from the epigenetic to extracellular level in a single well.

    abstract:BACKGROUND AND PURPOSE:Fibrosis, a pathological accumulation of collagen in tissues, represents a major global disease burden. Effective characterization of potential antifibrotic drugs has been constrained by poor formation of the extracellular matrix in vitro, due to tardy procollagen processing by collagen C-protein...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00387.x

    authors: Chen CZ,Peng YX,Wang ZB,Fish PV,Kaar JL,Koepsel RR,Russell AJ,Lareu RR,Raghunath M

    更新日期:2009-11-01 00:00:00

  • Nerve evoked P2X receptor contractions of rat mesenteric arteries; dependence on vessel size and lack of role of L-type calcium channels and calcium induced calcium release.

    abstract::1. Contractile responses to short trains of nerve stimulation have been characterized in small, medium and large arteries from the rat mesenteric circulation (5th - 6th, 2nd - 3rd and 1st order, respectively). In addition, sources of calcium for smooth muscle contraction have been investigated. 2. Nerve stimulation (1...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703925

    authors: Gitterman DP,Evans RJ

    更新日期:2001-03-01 00:00:00

  • Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.

    abstract:BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2012.01987.x

    authors: Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

    更新日期:2012-09-01 00:00:00

  • Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand.

    abstract::We investigated the ability of N-benzyl-N-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-yl)acetamide (AC-5216), a novel mitochondrial benzodiazepine receptor (MBR) ligand, to produce anti-anxiety and antidepressant-like effects in various animal models. AC-5216 showed high affinity for MBRs prepared from rat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705681

    authors: Kita A,Kohayakawa H,Kinoshita T,Ochi Y,Nakamichi K,Kurumiya S,Furukawa K,Oka M

    更新日期:2004-08-01 00:00:00

  • Sotalol for the protection of turkeys from the development of -aminopropionitrile-induced aortic ruptures.

    abstract::1. The influence of feeding 2 levels of sotalol on the incidence of beta-aminopropionitrile (BAPN)-induced aortic ruptures of immature turkeys was determined.2. Four of 22 turkeys fed 0.12% sotalol and 0.07% BAPN died of aortic ruptures, but 6 of 21 turkeys fed only BAPN died of the syndrome.3. Blood pressure, heart r...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1972.tb08095.x

    authors: Simpson CF

    更新日期:1972-07-01 00:00:00

  • The central and regional cardiovascular responses to intravenous and intracoronary administration of the phenyldihydropyridine elgodipine in anaesthetized pigs.

    abstract::1. The central and regional cardiovascular responses to intravenous (0.3, 1.0, 3.0 and 10.0 micrograms kg-1 min-1) and intracoronary (0.3, 0.9, 3.0 and 4.5 micrograms kg-1 min-1) infusions of elgodipine, a phenyldihydropyridine, and its solvent were studied in anaesthetized pigs. 2. Elgodipine (i.v.) caused dose-depen...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1990.tb14708.x

    authors: Sassen LM,Soei LK,Koning MM,Verdouw PD

    更新日期:1990-02-01 00:00:00

  • Acetylcholine-induced arteriolar dilation is reduced in streptozotocin-induced diabetic rats with motor nerve dysfunction.

    abstract::1. Diabetes mellitus produces marked abnormalities in motor nerve conduction, but the mechanism is not clear. In the present study we hypothesized that in the streptozotocin (STZ)-induced diabetic rat impaired vasodilator function is associated with reduced endoneural blood flow (EBF) which may contribute to nerve dys...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702856

    authors: Terata K,Coppey LJ,Davidson EP,Dunlap JA,Gutterman DD,Yorek MA

    更新日期:1999-10-01 00:00:00

  • Enhancement of opioid inhibition of GABAergic synaptic transmission by cyclo-oxygenase inhibitors in rat periaqueductal grey neurones.

    abstract::Cyclo-oxygenase (COX) inhibitors potentiate opioid inhibition of GABAergic synaptic transmission in rat periaqueductal grey (PAG) (Vaughan et al., 1997). In the present study, the relative contribution of cyclo-oxygenase-1 (COX-1) and COX-2 inhibition to this phenomenon was examined by use of whole-cell patch clamp re...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701818

    authors: Vaughan CW

    更新日期:1998-04-01 00:00:00

  • Inhibition of polycomb repressor complex 2 ameliorates neointimal hyperplasia by suppressing trimethylation of H3K27 in vascular smooth muscle cells.

    abstract:BACKGROUND AND PURPOSE:The increased proliferation and migration of vascular smooth muscle cells (VSMCs) after arterial injury contributes greatly to the pathogenesis of neointimal hyperplasia. As a major component of epigenetics, histone methylation plays an important role in several cardiovascular diseases. However, ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14754

    authors: Liang J,Li Q,Cai W,Zhang X,Yang B,Li X,Jiang S,Tian S,Zhang K,Song H,Ai D,Zhang X,Wang C,Zhu Y

    更新日期:2019-09-01 00:00:00

  • Resolvins are potent analgesics for arthritic pain.

    abstract::Arthritis-associated inflammatory pain represents a serious medical problem worldwide. Current treatments for arthritic pain are not very effective and cause unwanted side effects. Resolvins, including the resolvin D and resolvin E series, are a family of novel endogenous lipid mediators derived from ω-3 polyunsaturat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01348.x

    authors: Xu ZZ,Ji RR

    更新日期:2011-09-01 00:00:00

  • Antileukoproteinase protects against hepatic inflammation, but not apoptosis in the response of D-galactosamine-sensitized mice to lipopolysaccharide.

    abstract:BACKGROUND AND PURPOSE:There is major evidence for the strong bi-directional interrelation of parenchymal cell apoptosis and leukocyte accumulation and inflammation in acute liver injury. Therefore, the aim of this in vivo study was to investigate the anti-apoptotic and anti-inflammatory potential of antileukoproteinas...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707230

    authors: Eipel C,Kidess E,Abshagen K,Leminh K,Menger MD,Burkhardt H,Vollmar B

    更新日期:2007-06-01 00:00:00

  • Evidence that the agonist action of dynorphin A(1-8) in the guinea-pig myenteric-plexus may be mediated partly through conversion to [Leu5]enkephalin.

    abstract::1. The agonist action of the opioid peptide dynorphin A(1-8) on the myenteric plexus-longitudinal muscle of the guinea-pig ileum has been characterized. 2. The endogenous opioid peptide dynorphin A(1-8) was rapidly degraded by slices of myenteric plexus-longitudinal muscle of the guinea-pig ileum. 3. A product of the ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1990.tb14139.x

    authors: Dixon DM,Traynor JR

    更新日期:1990-11-01 00:00:00

  • DNA mismatch repair (MMR)-dependent 5-fluorouracil cytotoxicity and the potential for new therapeutic targets.

    abstract::The metabolism and efficacy of 5-fluorouracil (FUra) and other fluorinated pyrimidine (FP) derivatives have been intensively investigated for over fifty years. FUra and its antimetabolites can be incorporated at RNA- and DNA-levels, with RNA level incorporation provoking toxic responses in human normal tissue, and DNA...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1476-5381.2009.00423.x

    authors: Li LS,Morales JC,Veigl M,Sedwick D,Greer S,Meyers M,Wagner M,Fishel R,Boothman DA

    更新日期:2009-10-01 00:00:00