Insurmountable angiotensin AT1 receptor antagonists: the role of tight antagonist binding.

abstract：:The human 5-HT transporter (hSERT) has two binding sites for 5-HT and 5-HT uptake inhibitors: the orthosteric high-affinity site and a low-affinity allosteric site. Activation of the allosteric site increases the dissociation half-life for some uptake inhibitors. The objectives of this study were 1) to identify hSERT ...

journal_title：European journal of pharmacology

authors： Plenge P,Gether U,Rasmussen SG

更新日期：2007-07-12 00:00:00

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

authors： Armstead WM

更新日期：2003-08-08 00:00:00

abstract：:There is controversy concerning the inhibitory effect of arginine-vasopressin (AVP) on human platelet adenylate cyclase activity, which putatively involves Gi as the G-protein. To clarify this point, the effects of AVP on human platelet membranes were studied by measuring the activities of the high-affinity GTPase, as...

journal_title：European journal of pharmacology

authors： Vittet D,Mathieu MN,Cantau B,Chevillard C

更新日期：1988-06-10 00:00:00

abstract：:Corticotropin-releasing factor (CRF) is a neurohormone that mediates stress, anxiety, and affects serotonergic activity. Studies have shown that CRF has dose-dependent opposing effects on serotonergic activity. This effect has been hypothesized to be differentially mediated by CRF(1) and CRF(2) receptors in the dorsal...

journal_title：European journal of pharmacology

authors： Lukkes JL,Forster GL,Renner KJ,Summers CH

更新日期：2008-01-14 00:00:00

abstract：:Induction of anaphylactic shock in mice by i.v. antigen challenge (bovine serum albumin, 100 micrograms) or i.v. treatment with the mast cell degranulator compound 48/80 resulted in 80 and 90% mortality rate, respectively. Inhibition of nitric oxide (NO) synthesis from L-arginine by co-injection of the L-arginine anal...

journal_title：European journal of pharmacology

authors： Amir S,English AM

更新日期：1991-10-02 00:00:00

abstract：:Oleuropein (OLE) was found to have anti-inflammatory and anti-oxidant effects. The latest study has shown that it can resist myocardial injury that follows an acute myocardial infarction and can rescue impaired spinal nerve cells. In this study, we investigated the neuroprotective effects of OLE on cerebral ischemia a...

journal_title：European journal of pharmacology

authors： Yu H,Liu P,Tang H,Jing J,Lv X,Chen L,Jiang L,Xu J,Li J

更新日期：2016-03-15 00:00:00

abstract：:The mesolimbic dopaminergic innervation is supposed to be involved in the mechanisms of central effects exerted by various classes of psychotropic drugs. Antidepressants have been found to interact with the brain dopaminergic system as well, although the precise central location of this interaction is unknown. Some da...

journal_title：European journal of pharmacology

authors： Plaznik A,Kostowski W

更新日期：1987-03-31 00:00:00

abstract：:Although hypoxia induces adrenomedullin gene expression in cultured rat cardiac myocytes, it is still unknown whether oxidative stress is involved in the hypoxia-induced adrenomedullin production. We investigated whether oxidative stress might participate in hypoxia-induced adrenomedullin secretion and whether adrenom...

journal_title：European journal of pharmacology

authors： Yoshihara F,Horio T,Nishikimi T,Matsuo H,Kangawa K

更新日期：2002-02-01 00:00:00

abstract：:Unlike the situation with the vas deferens of rats, guinea-pigs, rabbits and dogs, neither phentolamine nor yohimbine enhanced electrically-evoked release of [3H]norepinephrine from the in vitro human vas deferens. However, clonidine produced, by a phentolamine-sensitive mechanism, a concentration-related inhibition o...

journal_title：European journal of pharmacology

authors： Belis JA,Colby JE,Westfall DP

更新日期：1982-03-26 00:00:00

abstract：:The involvement of a central mechanism in the antiemetic effect of AS-8112 ((R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1H-1,4-diazepin-6-yl)-2-methoxy-6-methylamino-3-pyridinecarboxamide x 2 fumarate), a novel and potent dopamine D2, D3, and 5-HT(3) receptor antagonist, was investigated in ferrets. Intracerebroventricul...

journal_title：European journal of pharmacology

authors： Yoshikawa T,Yoshida N,Oka M

更新日期：2001-11-23 00:00:00

abstract：:Various opiate ligands were bound to brain membranes of mice of the Recombinant Inbred System. The specific binding of low levels of [3H]naloxone, [3H]dihydromorphine and [3H]ethylketocyclazocine was disturbed in a similar fashion among the inbred strains, and in a pattern different from that observed for [3H](D-Ala2,...

journal_title：European journal of pharmacology

authors： Reith ME,Sershen H,Vadasz C,Lajtha A

更新日期：1981-09-24 00:00:00

abstract：:The rapid breakout of the coronavirus disease of 2019 (COVID-19) has been declared pandemic with serious global concern due to high morbidity and mortality. As we enter the phase beyond limitations there is an urgent need for explicit treatment against COVID-19. To face this immediate global challenge, drug developmen...

journal_title：European journal of pharmacology

authors： Bibi N,Gul S,Ali J,Kamal MA

更新日期：2020-10-15 00:00:00

abstract：:We directly compared the effects of YM337, the Fab fragment of the humanized monoclonal antibody C4G1, on platelet aggregation and template bleeding time with those of abciximab, the Fab fragment of the human/murine chimeric monoclonal antibody 7E3, in rhesus monkeys. The duration of inhibition of platelet aggregation...

journal_title：European journal of pharmacology

authors： Suzuki K,Sakai Y,Hisamichi N,Taniuchi Y,Sato K,Terazaki C,Kaku S,Kawasaki T,Yano S,Inagaki O,Masuho Y

更新日期：1997-10-08 00:00:00

abstract：:The action of 9(0)-thiaprostacyclin (PGI2-S) was compared with that of prostacyclin (PGI2) and papaverine in the femoral circulation of dogs. PGI2-S, injected into the dog femoral artery in a dose of 0.1 microgram or higher, produced marked vasodilation in the femoral artery without any change in blood pressure. The p...

journal_title：European journal of pharmacology

authors： Horii D,Kanayama T,Mori M,Shibasaki M,Ikegami S

更新日期：1978-10-01 00:00:00

abstract：:Acute respiratory and metabolic acidosis as well as metabolic alkalosis increased (by 11, 11, 21%) whereas respiratory alkalosis antagonized (by 10%) the partial steady state block produced by pipecuronium infusion on the anterior tibialis muscle of the cat. The duration of neuromuscular block following six successive...

journal_title：European journal of pharmacology

authors： Biró K

更新日期：1988-09-23 00:00:00

abstract：:An unbiased place preference conditioning procedure was used to examine the role of delta-opioid receptors in mediating the aversive effects of opioid withdrawal. Rats were implanted s.c. with two pellets each containing placebo or 75 mg morphine. Single-trial conditioning sessions with saline and the opioid receptor ...

journal_title：European journal of pharmacology

authors： Funada M,Schutz CG,Shippenberg TS

更新日期：1996-04-04 00:00:00

abstract：:Low doses of BHT 920, LY 171555 and (+)3PPP, three dopamine agonists selective for D-2 receptors, induced yawning in rats. This effect was reduced by the selective D-1 antagonist SCH 23390 but the antagonism did not exceed a 50% reduction from the control values. In contrast, the selective D-2 antagonist (-)sulpiride ...

journal_title：European journal of pharmacology

authors： Longoni R,Spina L,Di Chiara G

更新日期：1987-02-10 00:00:00

abstract：:RES-701-1 (cyclic (Gly1-Asp9)(Gly-Asn-Trp-His-Gly-Thr-Ala-Pro-Asp-Trp-Phe- Phe-Asn-Tyr-Tyr-Trp)), a peptide isolated from Streptomyces sp., has been reported to inhibit the endothelin ETB receptor. We examined the effects of this peptide on the blood vessels and the small intestine. In isolated rat aorta without endot...

journal_title：European journal of pharmacology

authors： Karaki H,Sudjarwo SA,Hori M,Tanaka T,Matsuda Y

更新日期：1994-09-12 00:00:00

abstract：:We examined the feasibility of coupling the 5-HT(6) receptor to a Ca(2+) signaling read-out using a chimeric G-protein, comprising of G(alphaq) with the C-terminal five amino acids from G(alphas), to facilitate assays on the fluorometric imaging plate reader (FLIPR). Using a transient transfection assay in human embry...

journal_title：European journal of pharmacology

authors： Zhang JY,Nawoschik S,Kowal D,Smith D,Spangler T,Ochalski R,Schechter L,Dunlop J

更新日期：2003-07-04 00:00:00

abstract：:The actions of a purified Helicobacter pylori lipopolysaccharide (3 mg x kg(-1), i.v.) on rat gastric antral and duodenal microvascular integrity (determined as radiolabelled albumin leakage) and the expression of the inducible nitric oxide (NO) synthase (iNOS; assessed by the citrulline assay) were investigated 4 h a...

journal_title：European journal of pharmacology

authors： Kiss J,Lamarque D,Moran AP,Pozsár J,Morschl E,László F,Whittle BJ

更新日期：2001-05-25 00:00:00

abstract：:The effects of adenyl compounds and some of their analogues were examined on atrial and ventricular muscle of Xenopus laevis. In contrast to all heart muscle preparations studied previously, adenosine produced excitation of the ventricle of Xenopus. 2-Chloroadenosine, ATP, beta, gamma-methylene ATP (APPCP) and alpha, ...

journal_title：European journal of pharmacology

authors： Meghji P,Burnstock G

更新日期：1983-05-06 00:00:00

abstract：:Terfenadine, a histamine H(1) receptor antagonist, has been associated with clinical ventricular arrhythmias and in vitro excitation-conduction blocks, whereas anti-ischemic and antiarrhythmic effects have been shown with cicletanine, a prostacyclin generation stimulator. We aimed at determining in vitro if cicletanin...

journal_title：European journal of pharmacology

authors： Criniti A,Picard S,Monti F,Dawodu AA,Ruvolo G,Puddu PE,Campa PP

更新日期：1999-10-15 00:00:00

abstract：:The effect of chronic administration of various monoamine oxidase (MAO) inhibitors on the ability of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) to inhibit forskolin-stimulated adenylate cyclase activity was studied. Groups of 12 rats were given either saline, (E)-beta-fluoromethylene-m-tyrosine (MDL 72394 0.25...

journal_title：European journal of pharmacology

authors： Sleight AJ,Marsden CA,Palfreyman MG,Mir AK,Lovenberg W

更新日期：1988-09-23 00:00:00

abstract：:BAY 38-7271 [(-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate] is a novel, highly potent and selective cannabinoid CB(1)/CB(2) receptor agonist with neuroprotective properties. It was the aim of the present study to further confirm its cannabinoid CB(1) receptor agonist properties in a highly...

journal_title：European journal of pharmacology

authors： De Vry J,Rüdiger Jentzsch K

更新日期：2002-12-20 00:00:00

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

authors： Jonsson JR,Head RJ,Frewin DB

更新日期：1992-02-11 00:00:00

abstract：:One of the best known bioactive triterpenoids is oleanolic acid, a widespread 3-hydroxy-17-carboxy oleanane-type compound. In order to determine whether further oxidation of carbon 3 affects anti-inflammatory activity in mice, different tests were carried out on oleanolic acid and its 3-oxo-analogue oleanonic acid, wh...

journal_title：European journal of pharmacology

authors： Giner-Larza EM,Máñez S,Recio MC,Giner RM,Prieto JM,Cerdá-Nicolás M,Ríos JL

更新日期：2001-09-28 00:00:00

abstract：:The effect of intracutaneous adrenaline and noradrenaline (5 X 10(-12) and 5 X 10(-11) mol) was examined on the oedema (Evans blue dye leakage) response of rats to several inflammatory agents. The catecholamines reduced the oedema response to all agents tested except prostaglandin E1 (PGE1) which was significantly pot...

journal_title：European journal of pharmacology

authors： O'Duffy G,Chahl LA

更新日期：1979-08-15 00:00:00

abstract：:Protective effects of OP-2507 [15-cis-(4-propylcyclohexyl)-16,17,18,19,20-pentanor-9-deoxy -9 alpha, 6-nitrilo-PGF1 methyl ester] against cerebral anoxia and edema were investigated in a variety of experimental models in mice and rats. OP-2507 given s.c. or p.o. led to a consistent and dose-dependent prolongation of s...

journal_title：European journal of pharmacology

authors： Masuda Y,Ochi Y,Ochi Y,Karasawa T,Hatano N,Kadokawa T,Okegawa T

更新日期：1986-04-29 00:00:00

abstract：:The effects of 3-(3-iodo-4-aminobenzyl)-8-(4-oxyacetate)-1-propylxanthine (I-ABOPX; BW-A522), which has nanomolar affinity for the recently cloned human and sheep adenosine A3 receptor, on the putative A3 receptor mediated hypotensive response to N6-2-(4-aminophenyl)ethyl adenosine (APNEA) in the rat have been investi...

journal_title：European journal of pharmacology

authors： Fozard JR,Hannon JP

更新日期：1994-02-03 00:00:00

abstract：:The interaction of phencyclidine, dexoxadrol, their analogs and stereoisomers with phencyclidine receptors was compared to their ability to induce stereotyped behavior and ataxia after i.c.v. administration to rats. The order of potency for binding to phencyclidine receptors revealed that among the stereoisomers of ph...

journal_title：European journal of pharmacology

authors： Contreras PC,Rice KC,Jacobson AE,O'Donohue TL

更新日期：1986-02-11 00:00:00