Homologous vs. heterologous desensitization of the adenylate cyclase system in heart cells.


:Exposure of cultured heart muscle cells to noradrenaline led to a decrease in the effects of isoproterenol and prostaglandin E1 on cAMP formation and contraction velocity. However, heterologous desensitization, as measured by prostaglandin E1 stimulation, only occurred at higher noradrenaline concentrations than homologous desensitization (isoproterenol stimulation). As the defects of the adenylate cyclase system in heart failure are attributed to noradrenaline-induced desensitization, it is concluded from the results that, in comparison to the subsensitivity to beta-adrenoceptor agonists in failing human hearts, a decrease in the responsiveness to other receptor-dependent adenylate cyclase stimulators should also occur but only at higher degrees of heart failure.


Eur J Pharmacol


Reithmann C,Werdan K




Has Abstract


1988-09-01 00:00:00














  • Dopamine receptor agonist potencies for inhibition of cell firing correlate with dopamine D3 receptor binding affinities.

    abstract::The potencies for in vivo inhibition of substantia nigra pars compacta dopamine single cell firing were determined for apomorphine, BHT 920, N-0923, (+/-)-7-hydroxy-dipropylaminotetralin (7-OH-DPAT), (+)-3-(3-hydroxyphenyl)-N-propylpiperidine (3-PPP), pramipexole, quinelorane, quinpirole, RU 24926, U-86170, and U-9135...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Kreiss DS,Bergstrom DA,Gonzalez AM,Huang KX,Sibley DR,Walters JR

    更新日期:1995-04-24 00:00:00

  • Heme oxygenase is expressed in human pulmonary artery smooth muscle where carbon monoxide has an anti-proliferative role.

    abstract::Heme oxygenase is the rate-limiting enzyme in the catabolism of heme to carbon monoxide, bilirubin and free iron. Many cell types express heme oxygenase-2 constitutively while heme oxygenase-1 is induced at sites of inflammation and oxidative stress. In systemic blood vessels, carbon monoxide may have an important hom...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Stanford SJ,Walters MJ,Hislop AA,Haworth SG,Evans TW,Mann BE,Motterlini R,Mitchell JA

    更新日期:2003-07-25 00:00:00

  • An aspartate in the second extracellular loop of the α(1B) adrenoceptor regulates agonist binding.

    abstract::The extracellular loops of the adrenoceptors present a potential therapeutic target in the design of highly selective adrenergic drugs. These regions are less conserved than the orthosteric binding site but have to date not been implicated in activation of adrenoceptors. A previously generated homology model identifie...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Campbell AP,MacDougall IJ,Griffith R,Finch AM

    更新日期:2014-06-15 00:00:00

  • Cannabinoid modulation of intestinal propulsion in mice.

    abstract::The effect of cannabinoid receptor activation and blockade on the propulsive activity in the mouse small intestine was assessed in the present study by measuring the transit of an orally administered, non-absorbable marker. The cannabinoid receptor agonist WIN 55,212-2 (R(+)-[2,3-dihydro-5-methyl-3[(morpholinyl)methyl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Colombo G,Agabio R,Lobina C,Reali R,Gessa GL

    更新日期:1998-02-26 00:00:00

  • Phenoxybenzamine is more potent in inactivating alpha 1- than alpha 2-adrenergic receptor binding sites.

    abstract::The effects of phenoxybenzamine on alpha 1- and alpha 2-adrenergic receptor binding sites were examined directly using radioligand binding assays of the antagonist drugs [125I]BE 2254 and [3H]rauwolscine, respectively, in homogenates of rat cerebral cortex. Treatment with phenoxybenzamine caused an irreversible, dose-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Minneman KP

    更新日期:1983-10-14 00:00:00

  • Design and screening of ASIC inhibitors based on aromatic diamidines for combating neurological disorders.

    abstract::Acid sensing ion channels (ASICs) are implicated in various brain functions including learning and memory and are involved in a number of neurological disorders such as pain, ischemic stroke, depression, and multiple sclerosis. We have recently defined ASICs as one of receptor targets of aromatic diamidines in neurons...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Chen X,Orser BA,MacDonald JF

    更新日期:2010-12-01 00:00:00

  • Evaluation of the rat bladder-derived relaxant factor by coaxial bioassay system.

    abstract::The release of bladder-derived relaxant factor in a coaxial bioassay system and the effects of reactive oxygen species were studied. After precontraction with phenylephrine (10(-6)-3x10(-6)) or 50 mM K+, acetylcholine (10(-8)-10(-3) M) induced relaxation in rat anococcygeus muscle mounted within rat bladder in a tissu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bozkurt TE,Sahin-Erdemli I

    更新日期:2004-07-14 00:00:00

  • Changes in motor activity and forebrain [propionyl-3H]propionylated-CCK-8 binding in mice after repeated administration of drugs affecting cholecystokinin receptors.

    abstract::The effects of acute or repeated treatment of male albino BKW mice with caerulein, a cholecystokinin octapeptide (CCK-8) agonist, and with devazepide (MK-329) and L-365,260, antagonists at CCKA ('peripheral') and CCKB ('central') receptors respectively, on motor activity and [propionyl-3H]propionylated-CCK-8 ([3H]pCCK...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Vasar E,Stephenson JD,Meldrum BS

    更新日期:1991-09-24 00:00:00

  • Proton inhibition of [3H]resiniferatoxin binding to vanilloid (capsaicin) receptors in rat spinal cord.

    abstract::Protons and capsaicin activate overlapping subsets of sensory nerves by opening ion conductances of similar properties. We have used the [3H]resiniferatoxin binding assay utilizing rat spinal cord membranes to elucidate the possible interaction of protons at the vanilloid (capsaicin) receptor. Using low pH (pH 6.0 and...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Szallasi A,Blumberg PM,Lundberg JM

    更新日期:1995-04-28 00:00:00

  • Morphine antagonizes U50,488's effects in a squirrel monkey shock titration procedure.

    abstract::To determine whether a mu opioid agonist modulates the effects of a kappa opioid agonist in squirrel monkeys responding under a shock titration procedure, morphine was administered in combination with an ED75 dose of U50,488. Morphine (0.03-0.3 mg/kg) did not alter U50,488's early peak effects (15-25 min post-injectio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Craft RM,Dykstra LA

    更新日期:1993-04-06 00:00:00

  • Apparent precoupling of kappa- but not mu-opioid receptors with a G protein in the absence of agonist.

    abstract::Rabbit and guinea-pig cerebellum membranes contain a very high (greater than 80%) proportion of mu- and kappa-opioid receptors, respectively. Rabbit (mu) and guinea-pig (kappa) cerebellum membranes were (i) labeled either with the opiate agonist, [3H]etorphine (Kd = 0.1-0.2 nM), or with the opiate antagonist, [3H]dipr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Frances B,Puget A,Moisand C,Meunier JC

    更新日期:1990-07-31 00:00:00

  • Behavioural and electrocortical power spectrum effects of 5-methoxytryptoline and other analogs after intraventricular administration in rats.

    abstract::The behavioural and electrocortical power spectrum effects of tryptoline and the 5-hydroxy and 5-methoxy derivatives were studied after microinjection of the drugs into the third cerebral ventricle in freely moving rats. The three compounds produced a dose-dependent desynchronication in electrocortical activity with a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Nistico G,De Sarro GB,Langer SZ

    更新日期:1987-10-06 00:00:00

  • Endothelium and cannabinoid receptor involvement in levcromakalim vasorelaxation.

    abstract::Levcromakalim was more potent at relaxing rat small mesenteric arteries with endothelium (EC50, 84+/-10 nM) than denuded vessels (EC50, 779+/-101 nM). The cannabinoid receptor antagonist SR 141716A (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-me thyl-1H-pyrazole-3-carboxamide hydrochloride; 1 microM...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: White R,Hiley CR

    更新日期:1997-11-27 00:00:00

  • Discriminative stimulus properties of physostigmine in rats.

    abstract::Sprague-Dawley rats were trained to discriminate a subcutaneous injection of physostigmine (0.2 mg/kg) from a similar injection of saline in a two-lever, food-reinforced behavior paradigm. The training dose of physostigmine reduced the response rate to about 50% of that in saline sessions. The discriminative stimulus ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Tang AH,Franklin SR

    更新日期:1988-08-09 00:00:00

  • Characterization of endothelium-dependent relaxation and modulation by treatment with pioglitazone in the hypercholesterolemic rabbit renal artery.

    abstract::The present study was undertaken to investigate vascular function in hypercholesterolemic rabbits and also to characterize the effects of pioglitazone on it. Rabbits were fed normal, 0.5% cholesterol chow, or 0.5% cholesterol chow plus 300 ppm pioglitazone for 5 or 10 weeks. The tension of isolated renal artery rings ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Moroe H,Fujii H,Honda H,Arai K,Kanazawa M,Notoya Y,Kogo H

    更新日期:2004-08-30 00:00:00

  • Effects of the peroxynitrite decomposition catalyst, FeTMPyP, on function of corpus cavernosum from diabetic mice.

    abstract::Peroxynitrite, the reaction product of nitric oxide and superoxide, may contribute to vascular tissue oxidant stress in diabetes mellitus. The aim was to establish whether the peroxynitrite decomposition catalyst 5,10,15,20-tetrakis(N-methyl-4'-pyridyl)porphyrinato iron III (FeTMPyP) could improve nitric oxide-depende...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Nangle MR,Cotter MA,Cameron NE

    更新日期:2004-10-11 00:00:00

  • The non-psychoactive cannabis constituent cannabidiol is an orally effective therapeutic agent in rat chronic inflammatory and neuropathic pain.

    abstract::Cannabidiol, the major psycho-inactive component of cannabis, has substantial anti-inflammatory and immunomodulatory effects. This study investigated its therapeutic potential on neuropathic (sciatic nerve chronic constriction) and inflammatory pain (complete Freund's adjuvant intraplantar injection) in rats. In both ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Costa B,Trovato AE,Comelli F,Giagnoni G,Colleoni M

    更新日期:2007-02-05 00:00:00

  • L-arginine-induced dilatation of goat coronary artery involves activation of K(ATP) channels.

    abstract::In the present study, the mechanism of relaxant response of nitric oxide precursor, L-arginine, was investigated in goat isolated coronary artery. L-arginine (1 mM) reversed the U-46619 (1 microM)-induced contraction both in endothelium-intact and endothelium-denuded arterial ring preparations. L-arginine analogues, L...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Deka DK,Mishra SK,Raviprakash V

    更新日期:2009-05-01 00:00:00

  • Further evidence that extrinsic acetylcholine acts preferentially on extrajunctional receptors in the chick biventer cervicis muscle.

    abstract::The specificity of action of extrinsic acetylcholine on extrajunctional and junctional receptors in the chick biventer cervicis muscle was studied by determining its ability to protect the responses evoked by acetylcholine and by tetanic nerve stimulation from the blockade by alpha-bungarotoxin, an irreversible bindin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Chang CC,Su MJ

    更新日期:1975-09-01 00:00:00

  • Contribution of receptor for advanced glycation end products to vasculature-protecting effects of exercise training in aged rats.

    abstract::The aim of present work was to investigate the underlying mechanism of vasculature-protecting effects of exercise training in aged rats. Experiment 1: aged rats were given moderate-intensity exercise for 12 weeks. Exercise training suppressed advanced glycation evidenced by reduced activity of aldose reductase, increa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Gu Q,Wang B,Zhang XF,Ma YP,Liu JD,Wang XZ

    更新日期:2014-10-15 00:00:00

  • Diversion of prostaglandin endoperoxide metabolism by selective inhibition of thromboxane A2 biosynthesis in lung, spleen or platelets.

    abstract::Infusion of arachidonic acid through the guinea pig lung or the cat spleen causes a release of thromboxane A2 and prostaglandins, as measured by bioassay. After incubation of human platelets with arachidonate similar metabolites are formed, as demonstrated chromatographically. Infusion of imidazole (50-75 microgram/ml...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Nijkamp FP,Moncada S,White HL,Vane JR

    更新日期:1977-07-15 00:00:00

  • Neonatal damage to neocortex abolishes the anxiolytic action of diazepam in adult rats.

    abstract::A neonatal cerebral cortical lesion was made in rats and the effects of diazepam on ultrasonic isolation calls in pups and footshock-elicited ultrasonic distress calls in young adult rats were assessed. There was no indication that the cortical lesion influenced the production of the ultrasonic distress calls in eithe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Naito H,Arishima K,Tonoue T

    更新日期:1995-01-16 00:00:00

  • Effect of Ca2+ entry blockers on myosin light-chain kinase and protein kinase C.

    abstract::Thirteen Ca2+ entry blockers were compared with respect to their inhibitory effects on the activity of smooth muscle myosin light-chain kinase and smooth muscle protein kinase C, and the Ca2+-induced contraction of basilar artery rings. Comparison of the IC50 values obtained for these compounds, suggests that with the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Schächtele C,Wagner B,Rudolph C

    更新日期:1989-04-12 00:00:00

  • Effects of MDMA and related analogs on plasma 5-HT: relevance to 5-HT transporters in blood and brain.

    abstract::(±)-3,4-Methylenedioxymethamphetamine (MDMA) is an illicit drug that evokes transporter-mediated release of serotonin (5-HT) in the brain. 5-HT transporter (SERT) proteins are also expressed in non-neural tissues (e.g., blood), and evidence suggests that MDMA targets platelet SERT to increase plasma 5-HT. Here we test...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Yubero-Lahoz S,Ayestas MA Jr,Blough BE,Partilla JS,Rothman RB,de la Torre R,Baumann MH

    更新日期:2012-01-15 00:00:00

  • Epidermal growth factor-induced rapid relaxation of the isolated rabbit mesenteric artery.

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    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Petitclerc E,Poubelle PE,Marceau F

    更新日期:1994-06-23 00:00:00

  • KF17837: a novel selective adenosine A2A receptor antagonist with anticataleptic activity.

    abstract::KF17837 is a novel selective adenosine A2A receptor antagonist. Oral administration of KF17837 (2.5, 10.0 and 30.0 mg/kg) significantly ameliorated the cataleptic responses induced by intracerebroventricular administration of an adenosine A2A receptor agonist, CGS 21680 (10 micrograms), in a dose-dependent manner. KF1...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Kanda T,Shiozaki S,Shimada J,Suzuki F,Nakamura J

    更新日期:1994-05-02 00:00:00

  • Effect of various antidepressant drugs on the spontaneous firing rate of locus coeruleus and dorsal raphe neurons of the rat.

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    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Scuvée-Moreau JJ,Dresse AE

    更新日期:1979-08-01 00:00:00

  • Anticancer effect of pan-PI3K inhibitor on multiple myeloma cells: Shedding new light on the mechanisms involved in BKM120 resistance.

    abstract::The correlation between the Phosphoinositide 3-kinase (PI3K) axis and crucial mechanisms involved in the maintenance of the neoplastic nature of multiple myeloma (MM) has recently evolved a general agreement that PI3K inhibition-based therapies could construct an exciting perspective for the future treatment strategie...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Safaroghli-Azar A,Bashash D,Kazemi A,Pourbagheri-Sigaroodi A,Momeny M

    更新日期:2019-01-05 00:00:00

  • The effects of HGCl2 and mersalyl on mechanisms regulating intracellular calcium and transmitter release.

    abstract::HgCl2 and mersalyl increased and later decreased both the spontaneous and evoked transmitter liberation at the frog neuromuscular junction. Lower concentration of HgCl2 exhibited only an inhibitory effect on transmitter release. These mercurials inhibited calcium transport of mitochondria and synaptosomal vesicles. Lo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Binah O,Meiri U,Rahamimoff H

    更新日期:1978-10-15 00:00:00

  • The putative imidazoline receptor agonist, harmane, promotes intracellular calcium mobilisation in pancreatic beta-cells.

    abstract::beta-Carbolines (including harmane and pinoline) stimulate insulin secretion by a mechanism that may involve interaction with imidazoline I(3)-receptors but which also appears to be mediated by actions that are additional to imidazoline receptor agonism. Using the MIN6 beta-cell line, we now show that both the imidazo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Squires PE,Hills CE,Rogers GJ,Garland P,Farley SR,Morgan NG

    更新日期:2004-10-06 00:00:00