Characterization of atypical beta-adrenoceptors in the guinea pig duodenum.

Abstract:

:The atypical beta-adrenoceptors mediating relaxation in the guinea pig duodenum were studied using catecholamines (isoprenaline, noradrenaline and adrenaline), a selective beta3-adrenoceptor agonist BRL37344 ((R*,R*)-(+/-)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl)amino]propyl]phe noxyacetic acid sodium salt) and a non-conventional partial beta3-adrenoceptor agonist CGP12177A ((-)-4-(3-t-butylamino-2-hydroxypropoxy)benzimidazol-2-one)). Catecholamines and beta3-adrenoceptor agonists induced concentration-dependent relaxation in this preparation. Propranolol (1 microM) produced only small rightward shifts in the concentration-response curves of these agonists. In the presence of propranolol (1 microM), however, a non-selective beta1-, beta2- and beta3-adrenoceptor antagonist bupranolol caused a concentration-dependent rightward shift of the concentration-response curves for catecholamines and beta3-adrenoceptor agonists. Schild plot analyses of the effects of bupranolol against these agonists gave pA2 values of 6.02 (isoprenaline), 5.98 (noradrenaline), 5.93 (adrenaline), 6.51 (BRL37344) and 5.70 (CGP12177A), respectively, and all Schild slopes were not significantly different from unity. These results suggest that atypical beta-adrenoceptors are present in the guinea pig duodenum and involved in mediating the functional relaxant response.

journal_name

Eur J Pharmacol

authors

Horinouchi T,Koike K

doi

10.1016/s0014-2999(99)00355-6

keywords:

subject

Has Abstract

pub_date

1999-07-02 00:00:00

pages

61-6

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(99)00355-6

journal_volume

376

pub_type

杂志文章
  • The spinal potentiating effect and the supraspinal inhibitory effect of midazolam on opioid-induced analgesia in rats.

    abstract::The authors investigated the effects of spinal and supraspinal administration of the benzodiazepine receptor agonist midazolam alone and with opioids on tests of nociception (tail-flick and hot-plate tests) and motor function (catalepsy) in rats. At the spinal level, the dose-response curves for peak effect and area u...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)00759-z

    authors: Luger TJ,Hayashi T,Weiss CG,Hill HF

    更新日期:1995-03-06 00:00:00

  • Pharmacological properties of ATP-sensitive K+ channels in mammalian skeletal muscle cells.

    abstract::The patch-clamp technique (single-channel recordings) was used to study the effects of glibenclamide and some channel openers on the KATP channel in mouse skeletal muscle. In outside/out membrane patches, glibenclamide reversibly inhibited KATP channel activity in a dose-dependent manner with an apparent Ki of 190 nM....

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90480-6

    authors: Allard B,Lazdunski M

    更新日期:1993-06-04 00:00:00

  • Epigenetic changes in the hypothalamic pro-opiomelanocortin gene: a mechanism linking maternal undernutrition to obesity in the offspring?

    abstract::Maternal undernutrition is associated with programming of obesity in offspring. While previous evidence has linked programming to the hypothalamic, pituitary, and adrenal (HPA) axis it could also affect the hypothalamic neuropeptides which regulate food intake and energy balance. Alpha melanocyte stimulating hormone (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2010.10.111

    authors: Stevens A,Begum G,White A

    更新日期:2011-06-11 00:00:00

  • Dopamine D3 receptor density elevation in aged Fischer-344 x Brown-Norway (F1) rats.

    abstract::The density of dopamine D3 receptors was determined in young (4-month-old) and aged (37-month-old) Fischer-344 x Brown-Norway (F1) male rats using the putative D3 receptor-preferring agonist, [3H](+)-7.hydroxy-2-(N,N-di-n-propylamino)tetralin ([3H](+)-7-OH-DPAT). In the presence of the non-hydrolyzable GTP analog, 5'-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00354-8

    authors: Wallace DR,Booze RM

    更新日期:1996-07-25 00:00:00

  • Receptor polymorphisms and diseases.

    abstract::The aim of our review is to summarize common genetic variations of some receptors associated with clinical consequences, which were not outlined in the previous special issue of this journal. Because of the multiple pathomechanisms of diseases, a set of genetic variation can play a role in the development of pathologi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(01)00755-5

    authors: Császár A,Abel T

    更新日期:2001-02-23 00:00:00

  • Direct and indirect effects of ephedrine on heart rate and blood pressure in vehicle-treated and sympathectomised male rats.

    abstract::We have investigated the cardiac and pressor responses to (±)-ephedrine and (-)-ephedrine in pentobarbitone anaesthetized male wistar rats. The tachycardiac responses to (±)- and (-)-ephedrine were similar, but pressor responses to (-)-ephedrine (10 mg/kg) were significantly greater than those to (±)-ephedrine, and fo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.02.021

    authors: Alsufyani HA,Docherty JR

    更新日期:2018-04-15 00:00:00

  • Synergistic action of ursolic acid and metformin in experimental model of insulin resistance and related behavioral alterations.

    abstract::Chronic restraint stress (CRS) is known to cause metabolic and neurological complications in a number of ways. Prolonged exposure to stress evident by increased corticosterone level led to impaired altered insulin signaling and oxidative stress in mice, in the present study. Impaired insulin signaling or insulin resis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.07.056

    authors: Mourya A,Akhtar A,Ahuja S,Sah SP,Kumar A

    更新日期:2018-09-15 00:00:00

  • Receptor affinity and pharmacological potency of a series of narcotic analgesic, anti-diarrheal and neuroleptic drugs.

    abstract::A series of 26 drugs was tested for in vitro binding to opiate receptors in the presence and absence of 0.1 M NaCl. The results were correlated with assays for in vivo pharmacological potency. Highly significant correlation was found between binding in the presence and absence of sodium ions and analgesic potency. For...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90334-x

    authors: Stahl KD,van Bever W,Janssen P,Simon EJ

    更新日期:1977-12-01 00:00:00

  • The effect of the phenol compound ellagic acid on Ca(2+) homeostasis and cytotoxicity in liver cells.

    abstract::Ellagic acid, a natural phenol compound found in numerous fruits and vegetables, causes various physiological effects in different cell models. However, the effect of this compound on Ca(2+) homeostasis in liver cells is unknown. This study examined the effect of ellagic acid on intracellular Ca(2+) concentration ([Ca...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.03.057

    authors: Liang WZ,Chou CT,Cheng JS,Wang JL,Chang HT,Chen IS,Lu T,Yeh JH,Kuo DH,Shieh P,Chen FA,Kuo CC,Jan CR

    更新日期:2016-06-05 00:00:00

  • Electrophysiological and neurochemical investigations on the action of carbamazepine on the rat hippocampus.

    abstract::Carbamazepine moderately depressed the input fiber volley resulting in attenuation of the dendritic epsp and the population spike in CA1 of rat hippocampal slices with a threshold concentration of 20 microM. The depressant effect on the population spike was not antagonized by the adenosine receptor blocker caffeine. P...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90030-5

    authors: Olpe HR,Baudry M,Jones RS

    更新日期:1985-03-26 00:00:00

  • Calyculin-A inhibits nitrergic relaxations of the mouse anococcygeus.

    abstract::The aim was to determine whether blockade of store-operated Ca(2+) entry, or inhibition of Ca(2+) sensitisation, is the predominant mechanism by which neuronally released nitric oxide mediates relaxation of the mouse anococcygeus. Nitrergic relaxations to field stimulation (10 Hz, 10 s trains) were unaffected by the s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01866-1

    authors: Gibson A,Wallace P,McFadzean I

    更新日期:2003-06-27 00:00:00

  • Differentiation-inducing factor-1-induced growth arrest of K562 leukemia cells involves the reduction of ERK1/2 activity.

    abstract::The differentiation-inducing factor-1 (DIF-1) is a signal molecule that induces stalk cell differentiation in the cellular slime mold Dictyostelium discoideum. In addition, DIF-1 is a potent antileukemic agent that induces growth arrest in K562 cells. In this study, we investigated the mechanism of action of DIF-1 in ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2003.11.041

    authors: Akaishi E,Narita T,Kawai S,Miwa Y,Sasaguri T,Hosaka K,Kubohara Y

    更新日期:2004-02-06 00:00:00

  • Effects of yohimbine on naloxone-induced antinociception in a rat model of inflammatory hyperalgesia.

    abstract::Effects of the alpha2-adrenoceptor antagonist yohimbine on the antinociception produced by a low dose of naloxone were examined in a rat model of carrageenan-induced inflammation. In rats receiving saline prior to naloxone injection, the low dose of naloxone (5 microg/kg, i.p.) significantly prolonged paw withdrawal l...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00151-4

    authors: Tsuruoka M,Hiruma Y,Matsutani K,Matsui Y

    更新日期:1998-05-08 00:00:00

  • Prejunctional inhibition of non-adrenergic non-cholinergic transmission in the rat anococcygeus muscle.

    abstract::The muscarinic agonist McN-A-343 did not affect the tone or nitroprusside-induced relaxations of the rat anococcygeus, but inhibited non-adrenergic non-cholinergic (NANC) relaxations. Atropine, pirenzepine and gallamine blocked the McN-A-343 inhibition of NANC relaxations. Agonists of alpha 1-(methoxamine) or alpha 2-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90640-7

    authors: Li CG,Rand MJ

    更新日期:1989-09-01 00:00:00

  • Inhibition of platelet aggregation by capsaicin. An effect unrelated to actions on sensory afferent neurons.

    abstract::The effects of capsaicin on the ability of platelets to aggregate in response to thrombin, platelet-activating factor or calcium ionophore (A23187) were examined. At concentrations previously shown to activate sensory afferent neurons, capsaicin markedly inhibited the responsiveness of platelets to the three agonists....

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90267-t

    authors: Hogaboam CM,Wallace JL

    更新日期:1991-09-04 00:00:00

  • Functional identification of alpha 1-adrenoceptor subtypes in human prostate: comparison with those in rat vas deferens and spleen.

    abstract::The effects of some alpha 1-adrenoceptor antagonists (prazosin, nonselective for the alpha 1A- and alpha 1B-adrenoceptor subtypes; 5-methyl-urapidil, selective for the alpha 1A-adrenoceptor subtype; chloroethylclonidine, selective for the alpha 1B-adrenoceptor subtype) and nifedipine were compared on contractile respo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90223-2

    authors: Teng CM,Guh JH,Ko FN

    更新日期:1994-11-14 00:00:00

  • TFMPP and RU24969 enhance serotonin release from rat hippocampus.

    abstract::Using a batch method for incubation of hippocampal slices, we have examined the effects of 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole (RU24969) and (m-trifluoromethylphenyl)piperazine (TFMPP) on release of endogenous 5-hydroxytryotamine (5-HT). Release of 5-HT from slices was enhanced by RU24969 and TFMPP ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)94111-a

    authors: Auerbach SB,Kamalakannan N,Rutter JJ

    更新日期:1990-11-06 00:00:00

  • GABA antagonists enhance dopamine turnover in the rat retina in vivo.

    abstract::Previous results provided evidence for an inhibitory GABAergic influence on the dopamine neurons of the rat retina, without proving that endogenous GABA physiologically regulates the activity of these cells. We injected picrotoxinin intraocularly to dark-adapted rats and measured retinal dopamine turnover. Dopamine wa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90473-8

    authors: Kamp CW,Morgan WW

    更新日期:1981-01-29 00:00:00

  • Protective effects of selegiline and desmethylselegiline against N-methyl-D-aspartate-induced rat retinal damage.

    abstract::Selegiline, a therapeutic agent of Parkinson's disease, and its metabolite, desmethylselegiline, were explored for their neuroprotective effects against N-methyl-D-aspartate (NMDA)-induced cell death in rat retina. Morphometric analysis of the retina revealed that an intravitreal injection of NMDA induced a significan...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02729-2

    authors: Takahata K,Katsuki H,Kobayashi Y,Muraoka S,Yoneda F,Kume T,Kashii S,Honda Y,Akaike A

    更新日期:2003-01-01 00:00:00

  • The pharmacological manipulation of glutamate receptors and neuroprotection.

    abstract::The overactivation of glutamate receptors is a major cause of Ca(2+) overload in cells, potentially leading to cell damage and death. There is an abundance of agents and mechanisms by which glutamate receptor activation can be prevented or modulated in order to control these effects. They include the well-established,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(02)01851-4

    authors: Stone TW,Addae JI

    更新日期:2002-07-05 00:00:00

  • Endothelin-1 induces potent constriction of lymphatic vessels in situ.

    abstract::The response of lymph vessels, arterioles and venules in the exteriorized rat mesentery to endothelin-1, vasopressin and norepinephrine was examined with the aid of high-resolution television microscopy. On a molar basis, endothelin-1 was more potent than vasopressin to contract the three types of vessels. Norepinephr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90135-0

    authors: Fortes ZB,Scivoletto R,Garcia-Leme J

    更新日期:1989-10-24 00:00:00

  • Impact of Helicobacter pylori and nonsteroidal anti-inflammatory drugs on gastric ulcerogenesis in experimental animals and in humans.

    abstract::Helicobacter pylori (H. pylori) and nonsteroidal anti-inflammatory drugs (NSAID) are the most common pathogens in the gastroduodenal mucosa in animals and humans, but their relationship in ulcerogenesis has been little studied. According to some authors, H. pylori infection in humans does not act synergistically with ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(02)01909-x

    authors: Pawlik T,Konturek PC,Konturek JW,Konturek SJ,Brzozowski T,Cześnikiewicz M,Plonka M,Bielanski W,Areny H

    更新日期:2002-08-02 00:00:00

  • Antiangiogenic versus cytotoxic therapeutic approaches to human pancreas cancer: an experimental study with a vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor and gemcitabine.

    abstract::Pancreatic adenocarcinoma is a leading cause of cancer death in the United States and represents a challenging chemotherapeutic problem. The pharmacological control of angiogenesis might represent a novel approach to the management of pancreas cancer, since the pathological development of vascular supply is a critical...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.07.062

    authors: Bocci G,Danesi R,Marangoni G,Fioravanti A,Boggi U,Esposito I,Fasciani A,Boschi E,Campani D,Bevilacqua G,Mosca F,Del Tacca M

    更新日期:2004-09-13 00:00:00

  • Clozapine-induced Fos-protein expression in rat forebrain regions: differential effects of adrenalectomy and corticosterone supplement.

    abstract::Unlike classical antipsychotic drugs, clozapine activates the hypothalamo-pituitary-adrenal axis and induces a specific regional pattern of Fos-protein expression in the rat forebrain. Whether corticosterone plays a role in the clozapine-induced Fos response is the subject of this study. Some rats were adrenalectomize...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00870-6

    authors: Sebens JB,Middelveld RJ,Koch T,Ter Horst GJ,Korf J

    更新日期:2001-04-06 00:00:00

  • Role of mitogen-activated protein kinase phosphatase-1 in corticosteroid insensitivity of chronic oxidant lung injury.

    abstract::Oxidative stress plays an important role in the pathogenesis of chronic obstructive pulmonary disease (COPD) and in the induction of corticosteroid (CS) insensitivity. Chronic ozone exposure leads to a model of COPD with lung inflammation and emphysema. Mitogen-activated protein kinase phosphatase-1 (MKP-1) may underl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.10.003

    authors: Pinart M,Hussain F,Shirali S,Li F,Zhu J,Clark AR,Ammit AJ,Chung KF

    更新日期:2014-12-05 00:00:00

  • Pertussis toxin-sensitive G-proteins in the sino-atrial node and right atrium of bovine heart.

    abstract::Three apparently distinct pertussis toxin (PTX)-sensitive substrates, with Mrs of 39, 40 and 41 kDa, were identified in membranes prepared from the sino-atrial (SA) node and right atrium of bovine heart. Based on their biochemical characterization, the effects of guanine nucleotides/MgCl2 on their PTX-catalyzed [32P]A...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(90)90236-q

    authors: Braun AP,Gupta RC,Sulakhe PV

    更新日期:1990-07-31 00:00:00

  • ETB receptor antagonist, IRL 1038, selectively inhibits the endothelin-induced endothelium-dependent vascular relaxation.

    abstract::In isolated rat aorta, endothelin-1 induced contractions at lower concentrations than endothelin-3. The contractile effects were augmented by removing the endothelium. In contrast, endothelium-1 and endothelin-3 at similar concentrations induced endothelium-dependent relaxation in norepinephrine-stimulated aorta. IRL ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90112-u

    authors: Karaki H,Sudjarwo SA,Hori M,Sakata K,Urade Y,Takai M,Okada T

    更新日期:1993-02-16 00:00:00

  • Effect of aclarubicin on contractile response of rat aorta.

    abstract::The effect of aclarubicin on vasocontractility was investigated using aortic strips isolated from rats. The aortic strips from rats injected i.p. with aclarubicin (4 mg/kg body weight per day for 5 consecutive days) showed diminished contractile responses to KCl and phenylephrine in comparison with the controls inject...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90761-9

    authors: Wakabayashi I,Hatake K,Kakishita E

    更新日期:1989-08-11 00:00:00

  • Anti-inflammatory effect of dual nociceptin and opioid receptor agonist, BU08070, in experimental colitis in mice.

    abstract::Endogenous opioid and nociceptin systems are widely distributed in the gastrointestinal tract where they seem to play a crucial role in maintaining the intestinal homeostasis. The aim of our study was to assess whether activation of nociceptin (NOP) and µ-opioid (MOP) receptors by a mixed NOP/MOP receptor agonist, BU0...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.09.021

    authors: Zielińska M,Ben Haddou T,Cami-Kobeci G,Sałaga M,Jarmuż A,Padysz M,Kordek R,Spetea M,Husbands SM,Fichna J

    更新日期:2015-10-15 00:00:00

  • Time-dependent vascular actions of cannabidiol in the rat aorta.

    abstract::We have shown that the major active agent of Cannabis sativa, Delta(9)-tetrahydrocannabinol, activates peroxisome proliferator-activated receptor gamma [PPARgamma, O'Sullivan, S.E., Tarling, E.J., Bennett, A.J., Kendall, D.A., Randall, M.D., 2005c. Novel time-dependent vascular actions of delta9-tetrahydrocannabinol m...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.03.010

    authors: O'Sullivan SE,Sun Y,Bennett AJ,Randall MD,Kendall DA

    更新日期:2009-06-10 00:00:00