Convulsant, anticonvulsant and anaesthetic barbiturates. 5-Ethyl-5-(3'-methyl-but-2'-enyl)-barbituric acid and related compounds.

abstract：:Microinjections of substance P (SP, 100 pmol) into the dorsal raphe nucleus (DRN) in conscious rats increased blood pressure and heart rate for 30-40 min. Concomitantly, the extracellular levels of 5-hydroxytryptamine (5-HT) in the ventral hippocampus, monitored by microdialysis, increased by 30% for 20 min compared w...

journal_title：European journal of pharmacology

authors： Gradin K,Qadri F,Nomikos GG,Hillegaart V,Svensson TH

更新日期：1992-08-06 00:00:00

abstract：:We have developed a model of ischaemia-reperfusion injury in C57BL/6 mice involving ischaemia for 0.5 to 2.5 h with an elastic tourniquet on one hind limb and reperfusion for 24 h, analogous to a well-established model of ischaemia-reperfusion injury in the rat. Viability was assessed in tissue homogenates of the gast...

journal_title：European journal of pharmacology

authors： Knight KR,Zhang B,Morrison WA,Stewart AG

更新日期：1997-08-13 00:00:00

abstract：:A deamination product of histidine, urocanic acid, accumulates in the skin of mammals as trans-urocanic acid. Ultraviolet (UV) irradition converts it to the cis-isomer that is an important mediator in UV-induced immunosuppression. We have recently shown that urocanic acid interferes with the agonist binding to GABA(A)...

journal_title：European journal of pharmacology

authors： Uusi-Oukari M,Soini SL,Heikkilä J,Koivisto A,Neuvonen K,Pasanen P,Sinkkonen ST,Laihia JK,Jansén CT,Korpi ER

更新日期：2000-07-14 00:00:00

abstract：:The anti-arrhythmic action of 2,3-cis-1,2,3,4-tetrahydro-5-[(2-hydroxy-3-tert-butylamino)propoxy]2,3-naphthalenediol (nadolol) was evaluated and compared with that of propranolol in several experimental models of cardiac arrhythmias. Both nadolol and propranolol antagonized isoproterenol-induced tachycardia and ouabai...

journal_title：European journal of pharmacology

authors： Evans DB,Peschka MT,Lee RJ,Laffan RJ

更新日期：1976-01-01 00:00:00

abstract：:The responsiveness of the guinea-pig esophageal muscularis mucosae to arachidonic acid (AA) and its cyclooxygenase and lipoxygenase metabolites was examined in vitro. AA (0.1-30 microM) produced a concentration-dependent contraction of the muscularis mucosae (mean EC50 +/- S.E.M. = 5.1 +/- 1.0 microM). The contraction...

journal_title：European journal of pharmacology

authors： Kamikawa Y,Fujinuma S,Shimo Y

更新日期：1985-08-07 00:00:00

abstract：:The contractile responses to capsaicin and anandamide, exogenous and endogenous agonists for transient receptor potential vanilloid receptor 1 (TRPV1), respectively, were investigated in muscle strips isolated from the rat urinary bladder. Capsaicin and anandamide produced concentration-dependent contractions of the m...

journal_title：European journal of pharmacology

authors： Saitoh C,Kitada C,Uchida W,Chancellor MB,de Groat WC,Yoshimura N

更新日期：2007-09-10 00:00:00

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

authors： Stone TW,Addae JI

更新日期：2002-07-05 00:00:00

abstract：:Insulin resistance in skeletal muscle is a major risk factor for the development of type 2 diabetes (T2D). In this study, we investigated the effect of icariin on insulin resistance in C2C12 mouse skeletal muscle cells. C2C12 myoblasts were differentiated into myotubes for five days, then treated with icariin (50 and ...

journal_title：European journal of pharmacology

authors： Han Y,Jung HW,Park YK

更新日期：2015-07-05 00:00:00

abstract：:The effect of chronic treatment (21 days s.c.) with SCH 23390 and haloperidol on spontaneously active DA neurones in substantia nigra pars compacta (SNC) and ventral tegmental area (VTA) was studied in rats by means of single unit recording techniques. The specific DA D-1 receptor antagonist SCH 23390 was injected twi...

journal_title：European journal of pharmacology

authors： Skarsfeldt T

更新日期：1988-01-12 00:00:00

abstract：:We investigated the effect of probucol, a lipid-lowering agent with antioxidant properties, on HCl plus ethanol-induced gastric mucosal injury and on the healing of acetic acid-induced gastric ulcers in rats. When the free radical-scavenging activity of probucol was measured by an electron spin resonance technique, th...

journal_title：European journal of pharmacology

authors： Ito M,Suzuki Y,Ishihara M,Suzuki Y

更新日期：1998-08-07 00:00:00

abstract：:Acute (-)-nicotine administration (0.4 and 0.8 mg/kg s.c.) produced a regionally specific increase in the rate of catecholamine synthesis in the rat nucleus accumbens, hypothalamus and hippocampus but not elsewhere, including the caudate-putamen. In all regions rates of 5-hydroxytryptamine synthesis were unaffected. (...

journal_title：European journal of pharmacology

authors： Mitchell SN,Brazell MP,Joseph MH,Alavijeh MS,Gray JA

更新日期：1989-08-29 00:00:00

abstract：:The novel dopaminergic agents (+)- and (-)-3-PPP were evaluated for their effects upon thermoregulation in rats maintained at room temperature (approximately 22 degrees C). Although approximately 30 times less potent than apomorphine, (+)-3-PPP induced a clearcut, dose-dependent and haloperidol/pimozide-reversible hyp...

journal_title：European journal of pharmacology

authors： Hjorth S,Carlsson A,Clark D,Svensson K,Sanchez D

更新日期：1985-01-08 00:00:00

abstract：:In slices of rat occipital cortex preincubated with 3H-noradrenaline, methioine-enkephalin diminished the overflow of tritium evoked by electrical field stimulation or by 20 mM potassium. The effect was not modified by phentolamine, but was antagonized by naloxone. Giver alone, naloxone slightly increased the potassiu...

journal_title：European journal of pharmacology

authors： Taube HD,Borowski E,Endo T,Starke K

更新日期：1976-08-01 00:00:00

abstract：:The aim of the study was to assess which tachykinin receptors mediate the contractile response in the guinea-pig isolated bronchi. Experiments with natural tachykinins and receptor-selective tachykinin agonists were performed in the absence or presence of peptidase inhibitors and in bronchi pretreated with phenoxybenz...

journal_title：European journal of pharmacology

authors： Maggi CA,Patacchini R,Quartara L,Rovero P,Santicioli P

更新日期：1991-05-17 00:00:00

abstract：:The effects of capsaicin pretreatment on withdrawal responses of guinea-pig isolated ileum to [Met5]enkephalin (ME) and morphine and on the locomotor withdrawal response of guinea-pigs following a single dose of morphine, were investigated. In vitro treatment of ileum with capsaicin, 1.5 mumol/l for 1 h, did not signi...

journal_title：European journal of pharmacology

authors： Chahl LA

更新日期：1988-12-06 00:00:00

abstract：:Large doses of dexamphetamine, methylamphetamine and MPTP failed to induce the formation of 6-hydroxydopamine (6-OHDA) in rat striatum. The potent dopamine (DA) releasing actions of these drugs and of the MPTP metabolite MPP+ were shown by intracerebral dialysis of DA in conscious rats but 6-OHDA was not detectable in...

journal_title：European journal of pharmacology

authors： Rollema H,De Vries JB,Westerink BH,Van Putten FM,Horn AS

更新日期：1986-12-02 00:00:00

abstract：:Urinary obstruction from benign prostatic hyperplasia is a common clinical problem possibly associated with excessive prostatic constriction around the urethra. These studies compared adrenergic and serotonergic functional activity to specific alpha 1 and serotonin (5-hydroxytryptamine; 5-HT) binding sites in the rat ...

journal_title：European journal of pharmacology

authors： Killam AL,Watts SW,Cohen ML

更新日期：1995-01-24 00:00:00

abstract：:In order to identify new atypical antipsychotic drugs which are more selective for the human dopamine D4 receptor than for the human dopamine D2 (long) receptor, we tested enantiomer pairs of dopamine agonists and dopamine antagonists on the expressed proteins of these cloned receptors. The (+)-aporphines ((+)-N-propy...

journal_title：European journal of pharmacology

authors： Seeman P,Van Tol HH

更新日期：1993-03-16 00:00:00

abstract：:We investigated the mechanism of antithrombin III-induced vascular release of endothelins in rat isolated lung. The antithrombin III-stimulated release of big endothelin-1 and endothelin-1 (1.7-fold and 1.3-fold over baseline) was abolished by nicardipine (L-type Ca2+ channel blocker), heparin, and N-acetyl heparin (a...

journal_title：European journal of pharmacology

authors： Stangl K,Dschietzig T,Alexiou K,Brunner F

更新日期：1999-04-01 00:00:00

abstract：:The activation of eosinophils with the lipid mediator, leukotriene B(4), induces their homotypic aggregation. Upon activation with leukotriene B(4), eosinophils release a significant amount of arachidonic acid, a process dependent on the activation of phospholipase A(2). Here, we have evaluated whether arachidonic aci...

journal_title：European journal of pharmacology

authors： Teixeira MM,Lindsay MA,Giembycz MA,Hellewell PG

更新日期：1999-11-19 00:00:00

abstract：:The stable gastric pentadecapeptide BPC 157 (GEPPPGKPADDAGLV, M.W.1419), which was promising in inflammatory bowel disease (PL-10, PLD-116, PL-14736, Pliva) trials, protects against both acute and chronic alcohol-induced lesions in stomach and liver, but also, given peripherally, affects various centrally mediated dis...

journal_title：European journal of pharmacology

authors： Blagaic AB,Blagaic V,Romic Z,Sikiric P

更新日期：2004-09-24 00:00:00

abstract：:Drugs belonging to different chemical classes having the ability to improve behavioral performance in animal learning and memory tests may share the common ability to stimulate protein kinase C activity in rat brain cortex. In vitro acetyl-L-carnitine (100 nM) promoted in rat brain cortex slices a significant increase...

journal_title：European journal of pharmacology

authors： Pascale A,Milano S,Corsico N,Lucchi L,Battaini F,Martelli EA,Trabucchi M,Govoni S

更新日期：1994-11-14 00:00:00

abstract：:Here we investigated the effect of naloxone-precipitated morphine withdrawal on the release of noradrenaline in hippocampus of the anaesthetised rat. Naloxone (1 mg/kg i.p.) injected 3 and 24 h, but not 3 weeks, after eight daily injections of morphine, induced an immediate increase in hippocampal noradrenaline releas...

journal_title：European journal of pharmacology

authors： Done C,Silverstone P,Sharp T

更新日期：1992-05-14 00:00:00

abstract：:Mitochondrial DNA mutations promote hypertensive renal dysfunction, but the molecular mechanism remains unclear. This study compared renal damage between spontaneously hypertensive rats (SHR) and SHR with mitochondrial transfer (t)RNA mutations. To investigate the role of mitochondrial outer membrane voltage-dependent...

journal_title：European journal of pharmacology

authors： Zhu C,Tian L,Yang H,Chen P,Li Y,Liu Y

更新日期：2019-12-15 00:00:00

abstract：:The intracerebroventricularly (i.c.v.) injected presynaptic alpha2-adrenoceptor agonists, clonidine and oxymetazoline, exerted a dose-dependent inhibition on the gastric acid secretion in pylorus-ligated rats; the ED50 values were 20 and 7.5 nmol/rat, respectively. Moreover, beta-endorphin, given i.c.v., also decrease...

journal_title：European journal of pharmacology

authors： Müllner K,Rónai AZ,Fülöp K,Fürst S,Gyires K

更新日期：2002-01-25 00:00:00

abstract：:We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Wh...

journal_title：European journal of pharmacology

authors： Bräuner-Osborne H,Hermit MB,Nielsen B,Krogsgaard-Larsen P,Johansen TN

更新日期：2000-10-06 00:00:00

abstract：:Substance-related and addictive disorders (SRADs) are characterized by compulsive drug use and recurrent relapse. The persistence of pathological drug-related memories indisputably contributes to a high propensity to relapse. Hence, strategies to disrupt reconsolidation of drug reward memory are currently being pursue...

journal_title：European journal of pharmacology

authors： Rulan D,Zhenbang Y,Yipu Z,Yuan G,Galaj E,Xiaorui S,Wenshuya L,Jiaqi L,Yan Z,Chang Y,Xi Y,Li S,Yixiao L,Haishui S

更新日期：2021-01-24 00:00:00

abstract：:Stimulation of muscarinic M1-receptors in isolated rabbit vas deferens by McN-A-343 inhibited electrically induced twitch contractions susceptible to competitive blockade by (+)-, (+/-), (-)-telenzepine and pirenzepine (pA2 = 9.12, 8.86, 6.98 and 7.79, respectively). The inhibition of twitch contractions by 10(-6) M M...

journal_title：European journal of pharmacology

authors： Eltze M

更新日期：1990-05-03 00:00:00

abstract：:Existing antimuscarinic drugs for overactive bladder have high affinity for M(3)/M(1) muscarinic receptors and consequently produce M(3)/M(1)-mediated adverse effects including dry mouth, constipation, mydriasis and somnolence. TD-6301 is a M(2/4) muscarinic receptor-selective antagonist developed for the treatment of...

journal_title：European journal of pharmacology

authors： McNamara A,Pulido-Rios MT,Sweazey S,Obedencio GP,Thibodeaux H,Renner T,Armstrong SR,Steinfeld T,Hughes AD,Wilson RD,Jasper JR,Mammen M,Hegde SS

更新日期：2009-03-01 00:00:00

abstract：:Clomipramine is a tricyclic antidepressant for psychiatric disorders that can induce QT prolongation, which may lead to torsades de pointes. Since blockade of cardiac human ether-a-go-go-related gene (hERG) channels is an important cause of acquired long QT syndrome, we investigated the acute effects of clomipramine o...

journal_title：European journal of pharmacology

authors： Jo SH,Hong HK,Chong SH,Won KH,Jung SJ,Choe H

更新日期：2008-09-11 00:00:00