当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > High and low (Gpp(NH)p-sensitive) affinity sites for beta 2-adrenergic blockers as antagonists of isoproterenol in the field-stimulated rat vas deferens.

High and low (Gpp(NH)p-sensitive) affinity sites for beta 2-adrenergic blockers as antagonists of isoproterenol in the field-stimulated rat vas deferens.

Abstract：

:Schild plots for (-)-propranolol, timolol and IPS 339, but not penbutolol or carazolol, as antagonists of isoproterenol in the isolated, field-stimulated rat vas deferens exhibited biphasic curves indicating the presence of both high and low affinity sites for these agents in this preparation. Schild plots determined for (-)-propranolol in the presence of prazosin (0.3 micron) or using the prostatic end of the rat vas deferens yielded two similar affinity sites suggesting the lack of involvement of postsynaptic alpha 1-adrenergic mechanisms in the observed response. In the presence of Gpp(NH)p(4 micron), (-)-propranolol, timolol and IPS 339 exhibited only a single affinity site which corresponded to their high affinity site in antagonizing isoproterenol in the absence of Gpp(NH)p. Similarly, only a single high affinity site was observed for (-)-propranolol when salbutamol, rather than isoproterenol, was used as the agonist. The data suggest the two affinity sites observed with some beta-adrenergic blockers in this preparation reflects a possible action of isoproterenol and the antagonists upon two subpopulations of beta 2-adrenergic receptors, one of which is sensitive to Gpp(NH)p.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Lotti VJ,Kling P,Cerino D

doi

10.1016/0014-2999(82)90198-4

subject

Has Abstract

pub_date

1982-10-22 00:00:00

pages

161-7

issue

3-4

eissn

0014-2999

issn

1879-0712

pii

0014-2999(82)90198-4

journal_volume

84

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • Bioallethrin causes permanent changes in behavioural and muscarinic acetylcholine receptor variables in adult mice exposed neonatally to DDT.

    abstract：:We recently reported changes in the density of muscarinic acetylcholine receptors in cerebral cortex of mice treated neonatally with DDT (1,1,1-trichloro-2,2-bis(p-chlorophenyl)-ethane) and receiving bioallethrin as adults. We also found behavioural aberrations in adult mice treated with bioallethrin, whether neonatal...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0926-6917(95)00012-7

    authors： Johansson U,Fredriksson A,Eriksson P

    更新日期：1995-07-01 00:00:00

  • A role for endothelin ETA receptors in regulation of renal function in spontaneously hypertensive rats.

    abstract：:While there is evidence to suggest that endothelin-1 is involved in regulation of kidney function and blood pressure, the importance of endothelin ETA receptors in this area has not been clearly defined. The novel, non-peptide endothelin ETA receptor antagonist, BMS-182874, (5-(dimethylamino)-N-(3,4- dimethyl-5-isoxaz...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00537-4

    authors： Bird JE,Webb ML,Giancarli MR,Chao C,Dorso CR,Asaad MM

    更新日期：1995-12-27 00:00:00

  • Pharmacological and histochemical evidence for P2X receptors in human umbilical vessels.

    abstract：:The presence of P2X purinoceptors in human umbilical vessels were studied with organ bath recording, radioligand binding assays, autoradiography, and immunohistochemistry. In isolated umbilical arteries and veins from normal term pregnancy, both ATP and alpha,beta-methylene ATP caused concentration-dependent contracti...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00383-5

    authors： Bo X,Sexton A,Xiang Z,Nori SL,Burnstock G

    更新日期：1998-07-17 00:00:00

  • Regulation of electrolyte transport by nitric oxide in the mouse cecum.

    abstract：:The effect and role of nitric oxide (NO) in the regulation of ion transport in the mouse cecum were investigated. L-arginine, used to increase NO production, increased short-circuit current (Isc), a measure of ion transport, in a concentration-dependent manner with a maximal increase of 193.8+/-65.5 microA/cm2. This i...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00221-0

    authors： Homaidan FR,Martello LA,Melson SJ,Burakoff R

    更新日期：1998-05-29 00:00:00

  • Sodium-glucose transporter as a novel therapeutic target in disease.

    abstract：:Glucose is the primary energy fuel of life. A glucose transporter, the sodium-glucose transporter (SGLT), is receiving attention as a novel therapeutic target in disease. This review summarizes the physiological role of SGLT in cerebral ischemia, cancer, cardiac disease, and intestinal ischemia, which has encouraged a...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejphar.2018.01.003

    authors： Yamazaki Y,Harada S,Tokuyama S

    更新日期：2018-03-05 00:00:00

  • Cloricromene synergizes with antiplatelet drugs and nitric oxide-like factor derived from rat peritoneal polymorphonuclear cells.

    abstract：:We report that cloricromene (5-30 microM) inhibited thrombin-induced platelet aggregation and synergized with other antiplatelet compounds. The antiaggregatory effect of subthreshold concentrations of the prostaglandin (PG)I2 analogue, iloprost (0.2 nM), or of sodium nitroprusside (1 micron), acting through a nitric o...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(92)90853-v

    authors： Mollace V,Prosdocimi M,Nisticó G

    更新日期：1992-11-10 00:00:00

  • Spinal transection increases the potency of clonidine on the tail-flick and hindlimb flexion reflexes.

    abstract：:The effect of intrathecal clonidine on thermal nociception and hindlimb flexion was assessed in acute and chronic spinally transected rats. After an acute, 1-day spinalization, there was no change in the antinociceptive dose-response function to clonidine, relative to intact rats. However, there was a significant incr...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(02)01259-1

    authors： Advokat C

    更新日期：2002-02-15 00:00:00

  • Gastrins and cholecystokinins release acetylcholine but not substance P from neurons in the guinea-pig taenia coli.

    abstract：:Gastrins and cholecystokinins contract the isolated taenia coli of the guinea-pig. Porcine CCK-39 produced the greatest contractile response and human gastrin-17 I and -34 the weakest. Pentagastrin had the highest affinity to the receptors and non-sulphated CCK-8 the lowest. The contractions produced by the CCK peptid...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(83)90244-3

    authors： Nilsson S,Leander S,Vallgren S,Håkanson R

    更新日期：1983-06-03 00:00:00

  • Theanine from tea and its semi-synthetic derivative TBrC suppress human cervical cancer growth and migration by inhibiting EGFR/Met-Akt/NF-κB signaling.

    abstract：:Cervical cancer is the third most prevalent cancer among women worldwide. Theanine from tea and its derivatives show some anticancer activities. However, the role of theanine and its derivatives against human cervical cancer and the molecular mechanisms of action remain unclear. Thus, in this study, we aim to investig...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.09.007

    authors： Liu J,Sun Y,Zhang H,Ji D,Wu F,Tian H,Liu K,Zhang Y,Wu B,Zhang G

    更新日期：2016-11-15 00:00:00

  • The effect of cismethrin on the rat dorsal root potentials.

    abstract：:Dorsal root potentials were recorded from urethane-anaesthetised rats. Bicuculline, a recognised GABA antagonist, reduced the amplitude of the potential to 67% of control. Cismethrin, a synthetic pyrethroid insecticide, enhanced the potential to 142% of control values. The convulsions associated with cismethrin poison...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(80)90304-0

    authors： Smith PR

    更新日期：1980-08-22 00:00:00

  • A kinetic analysis of a catechol-specific binding site in the microsomal fraction from the rabbit aorta.

    abstract：:(-)-3/-Norepinephrine (3H-NE) binding to the microsomal fraction of the rabbit aorta has been studied. Binding appears to increase linearly with time up to at least 30 min, shows no evidence of stereoselectivity and may be inhibited only by compounds possessing the catechol or 3-methoxy-4hydroxyphenyl moieties, with t...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(76)90324-1

    authors： Ruffolo RR,Mccreery RL,Patil PN

    更新日期：1976-08-01 00:00:00

  • PTK, ERK and p38 MAPK contribute to impaired NMDA-induced vasodilation after brain injury.

    abstract：:N-Methyl-D-aspartate (NMDA)-induced pial artery dilation is reversed to vasoconstriction following fluid percussion brain injury (FPI). This study investigated the contribution of activation of protein tyrosine kinase (PTK) and the extracellular signal-regulated kinase (ERK) and p38 isoforms of mitogen-activated prote...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(03)02012-0

    authors： Armstead WM

    更新日期：2003-08-08 00:00:00

  • Effect of alpha 1-adrenoceptor blockade on the development of hypertension in the spontaneously hypertensive rat.

    abstract：:There is a large body of evidence to suggest that the sympathetic nervous system plays a critical role in the development of hypertension and vascular medial hypertrophy in the spontaneously hypertensive rat (SHR). The synthesis of a water soluble, specific alpha 1-adrenoceptor antagonist (terazosin) has permitted an ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(92)90538-f

    authors： Jonsson JR,Head RJ,Frewin DB

    更新日期：1992-02-11 00:00:00

  • Animal models of rheumatoid arthritis: How informative are they?

    abstract：:Animal models of arthritis are widely used to de-convolute disease pathways and to identify novel drug targets and therapeutic approaches. However, the high attrition rates of drugs in Phase II/III rates means that a relatively small number of drugs reach the market, despite showing efficacy in pre-clinical models. Th...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejphar.2015.03.047

    authors： McNamee K,Williams R,Seed M

    更新日期：2015-07-15 00:00:00

  • Inhibition by tamsulosin of tension responses of human hyperplastic prostate to electrical field stimulation.

    abstract：:Tamsulosin (10(-10)-10(-9) M) or prazosin (10(-9)-10(-8) M) concentration dependently blocked the tension responses to electrical field stimulation (0.3 ms duration, 80 V and 20 Hz) in human hyperplastic prostate with lC50 values of (1.93 +/- 0.26) x 10(-10) M and (2.11 +/- 0.21) x 10(-9) M, respectively. The relative...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(96)00197-5

    authors： Chueh SC,Guh JH,Chen J,Lai MK,Ko FN,Teng CM

    更新日期：1996-06-03 00:00:00

  • A new technique for selective cannulation of the sino-atrial node artery.

    abstract：:The electrical activity of the sino-atrial node was studied after the selective cannulation of its artery in the intact open-chest dog. After tetrodotoxin infusion and despite cardiac arrest, a slow rhythmic activity was recorded from the sinus epicardial electrode. ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(78)90227-3

    authors： Adamantidis M,Vincent A,Dupuis B

    更新日期：1978-05-01 00:00:00

  • Decrease in endogenous CGRP release in nitroglycerin tolerance: role of ALDH-2.

    abstract：:In the present study, we tested whether the decreased release of calcitonin gene-related peptide (CGRP) observed in nitroglycerin tolerance is associated with the decrease in aldehyde dehydrogenase (ALDH-2) activity. We further investigated the possible involvement of reactive oxygen species in the decrease in ALDH-2 ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2007.05.042

    authors： Chen YR,Nie SD,Shan W,Jiang DJ,Shi RZ,Zhou Z,Guo R,Zhang Z,Li YJ

    更新日期：2007-09-24 00:00:00

  • Differential dopaminergic regulation of the neurotensin striatonigral and striatopallidal pathways in the rat.

    abstract：:Recently the existence of a neurotensin striatonigral pathway strongly up-regulated by methamphetamine has been demonstrated. The aim of the present study was to investigate, using immunohistochemistry and radioimmunoassay, the modulation of this pathway by dopamine antagonists. Rats were injected either with methamph...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(94)90021-3

    authors： Castel MN,Morino P,Nylander I,Terenius L,Hökfelt T

    更新日期：1994-09-01 00:00:00

  • The glial cell modulator and phosphodiesterase inhibitor, AV411 (ibudilast), attenuates prime- and stress-induced methamphetamine relapse.

    abstract：:Stress and renewed contact with drug (a "slip") have been linked to persisting relapse of methamphetamine abuse. Human brain microglial activation has been linked with methamphetamine abuse, and inhibitors of glial cell activation, certain phosphodiesterase (PDE) inhibitors, and glial cell derived neurotrophic factor ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2010.04.010

    authors： Beardsley PM,Shelton KL,Hendrick E,Johnson KW

    更新日期：2010-07-10 00:00:00

  • Silibinin alleviates high glucose-suppressed osteogenic differentiation of human bone marrow stromal cells via antioxidant effect and PI3K/Akt signaling.

    abstract：:High glucose is one of the possible causes for osteoporosis and fracture in diabetes mellitus. Our previous study showed that silibinin can increase osteogenic effect by stimulating osteogenic genes expression in human bone marrow stem cells (hBMSCs). However, no study has yet investigated the effect of silibinin on o...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2015.09.005

    authors： Ying X,Chen X,Liu H,Nie P,Shui X,Shen Y,Yu K,Cheng S

    更新日期：2015-10-15 00:00:00

  • Gender difference of atorvastatin's vasoprotective effect in balloon-injured rat carotid arteries.

    abstract：:The effect of estrogen on neointimal formation in injured rat arteries has been reported to be a sexual dimorphic effect. Recently, it has been reported that 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) exhibit vasoprotective effects, which are independent of their cholesterol-lowerin...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2006.09.036

    authors： Kurumazuka D,Mori T,Matsumoto N,Shirakawa H,Kimura S,Nakano D,Hayashi T,Kitaura Y,Matsumura Y

    更新日期：2006-12-28 00:00:00

  • Rat pup ultrasonic vocalization: effects of benzodiazepine receptor ligands.

    abstract：:The involvement of the GABA(A)-benzodiazepine receptor complex in rat pup ultrasonic vocalisations was studied by testing benzodiazepine receptor ligands with varying intrinsic activity and selectivity for benzodiazepine subtype receptors. Ultrasonic vocalisations were recorded under two temperature conditions (37 deg...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00603-7

    authors： Olivier B,Molewijk E,van Oorschot R,van der Heyden J,Ronken E,Mos J

    更新日期：1998-10-02 00:00:00

  • The selective tachykinin neurokinin 1 (NK1) receptor antagonist, GR 205,171, stereospecifically inhibits light-induced phase advances of hamster circadian activity rhythms.

    abstract：:Circadian rhythms in mammals are generated by master pacemaker cells located within the suprachiasmatic nucleus of the hypothalamus. In hamsters, the suprachiasmatic nucleus contains a small collection of cells immunoreactive for substance P, the endogenous ligand of tachykinin neurokinin 1 (NK1) receptors. In additio...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2005.10.012

    authors： Gannon RL,Millan MJ

    更新日期：2005-12-19 00:00:00

  • Comparison of pharmacological activities of Neuropeptide FF1 and Neuropeptide FF2 receptor agonists.

    abstract：:The pharmacological effects of Neuropeptide FF (NPFF) analogs exhibiting different selectivities towards Neuropeptide FF1 (NPFF1) and Neuropeptide FF2 (NPFF2) receptors were investigated after supraspinal administration in mice. Injected into the third ventricle, VPNLPQRF-NH2, which is selective for Neuropeptide FF1 r...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2004.12.002

    authors： Quelven I,Roussin A,Zajac JM

    更新日期：2005-01-31 00:00:00

  • [D-Met2,Pro5]enkephalinamide activates cardioinhibitory efferents in anaesthetized dogs.

    abstract：:[D-Met2,Pro5]enkephalinamide (DMPEA) strongly activated cardioinhibitory vagal efferents and elicited bradycardia when perfused through the cerebroventricular system of anaesthetized dogs. These effects were concentration-dependent but plateaued at an intraventricular concentration of 200 micrograms/ml. At this maxima...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(85)90216-x

    authors： Inoue K,Nashan B,Arndt JO

    更新日期：1985-04-02 00:00:00

  • Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds.

    abstract：:SK channels are small conductance, Ca(2+)-activated K(+) channels that underlie neuronal slow afterhyperpolarization and mediate spike frequency adaptation. Using the patch clamp technique, we tested the effects of eight clinically relevant psychoactive compounds structurally related to the tricyclic antidepressants, ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(00)00401-5

    authors： Dreixler JC,Bian J,Cao Y,Roberts MT,Roizen JD,Houamed KM

    更新日期：2000-07-28 00:00:00

  • Kappa-opiates and urination: pharmacological evidence for an endogenous role of the kappa-opiate receptor in fluid and electrolyte balance.

    abstract：:In prehydrated rats, the administration of kappa-opiate agonists such as bremazocine, ethylketocyclazocine or compound Upjohn-50,488 produced a dose-dependent increase in urine output and decreased the concentration of Na+ and K+ in the urine as compared to that of saline-treated rats. The diuretic effect of bremazoci...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(84)90084-0

    authors： Huidobro-Toro JP,Parada S

    更新日期：1984-12-15 00:00:00

  • Rutin ameliorates diabetic neuropathy by lowering plasma glucose and decreasing oxidative stress via Nrf2 signaling pathway in rats.

    abstract：:Rutin exhibits antidiabetic, antioxidant and anti-inflammatory properties, which makes rutin an attractive candidate for diabetic complications. The present study was designed to investigate the potential effect of rutin on diabetic neuropathy. After induction of diabetic neuropathy, rutin (5mg/kg, 25mg/kg and 50mg/kg...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2015.12.021

    authors： Tian R,Yang W,Xue Q,Gao L,Huo J,Ren D,Chen X

    更新日期：2016-01-15 00:00:00

  • N-(3-acetylaminophenyl)piperazine hydrochloride (BEA 1654), a putative 5-HT1 agonist, causes constriction of arteriovenous anastomoses and dilatation of arterioles.

    abstract：:Using 3H-ligands and radioactive microspheres we studied the binding characteristics and the effects on the distribution of carotid arterial blood flow of n-(3-acetylaminophenyl)piperazine hydrochloride (BEA 1654). The compound had a Ki value of 32 nM (5-HT: 8 nM) on 5-HT1 but no or very weak affinity for 5-HT2, alpha...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(85)90259-6

    authors： Verdouw PD,Jennewein HM,Mierau J,Saxena PR

    更新日期：1985-01-08 00:00:00

  • Role of 5-hydroxytryptamine and mast cells in the tachykinin-induced contraction of rat trachea in vitro.

    abstract：:The in vivo bronchoconstrictor effect of tachykinins in Fisher 344 rats is accompanied by release into the airways of 5-hydroxytryptamine (5-HT). 5-HT is possibly derived from mast cells. In the present study the presumed mast cell-tachykinin interaction was studied in isolated trachea from Fisher 344 rats. Contractio...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(97)81929-2

    authors： Joos GF,Lefebvre RA,Bullock GR,Pauwels RA

    更新日期：1997-11-12 00:00:00