Pitrazepin: a central glycine and GABA antagonist.

Abstract:

:In the spinal cord of the pentobarbitone-anaesthetised cat, microelectrophoretic pitrazepin reduced the inhibitory effects on neuronal firing of both glycine and GABA.

journal_name

Eur J Pharmacol

authors

Curtis DR,Gynther BD

doi

10.1016/0014-2999(86)90590-x

subject

Has Abstract

pub_date

1986-11-19 00:00:00

pages

311-3

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(86)90590-X

journal_volume

131

pub_type

杂志文章
  • Mode of action of gingerols and shogaols on 5-HT3 receptors: binding studies, cation uptake by the receptor channel and contraction of isolated guinea-pig ileum.

    abstract::Ginger (rhizomes of Zingiber officinale) has been shown to exert potent anti-emetic properties, but its mode of action has not yet been elucidated. Among its active constituents, [6]-, [8]- and [10]-gingerol as well as [6]-shogaol were shown in different in vivo studies to be at least partly responsible for the drug's...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.10.049

    authors: Abdel-Aziz H,Windeck T,Ploch M,Verspohl EJ

    更新日期:2006-01-13 00:00:00

  • Potentiation by neuropeptide Y of 5HT2A receptor-mediated contraction in porcine coronary artery.

    abstract::Potentiation by neuropeptide Y of serotonin (5-HT)-induced vasoconstriction was investigated in porcine coronary artery. 5-HT caused concentration-dependent contraction through 5-HT2A receptors. Neuropeptide Y (30 nM) significantly increased the 5HT-induced contraction by 16+/-5% in arteries with intact endothelium. R...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.036

    authors: Tsurumaki T,Nagai S,Bo X,Toyosato A,Higuchi H

    更新日期:2006-08-21 00:00:00

  • Methamphetamine selectively alters brain glutathione.

    abstract::As methamphetamine-induced neurotoxicity has been proposed to involve oxidative stress, reduced and oxidized glutathione (GSH and GSSG, respectively), vitamin E and ascorbate were measured in the striata of rats killed 2 or 24 h after a neurotoxic regimen of methamphetamine. At 2 h, methamphetamine increased GSH and G...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00392-7

    authors: Harold C,Wallace T,Friedman R,Gudelsky G,Yamamoto B

    更新日期:2000-07-14 00:00:00

  • Is digitalis compound-induced cardiotoxicity, mediated through guinea-pig cardiomyocytes apoptosis?

    abstract::Our aim in performing this study was to analyze in vivo the cell death mechanism induced by toxic doses of digitalis compounds on guinea-pig cardiomyocytes. We analyzed three study groups of five male guinea pigs each. Guinea pigs were intoxicated under anesthesia with ouabain or digoxin (at a 50-60% lethal dose); the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.03.033

    authors: Ramirez-Ortega M,Zarco G,Maldonado V,Carrillo JF,Ramos P,Ceballos G,Melendez-Zajgla J,Garcia N,Zazueta C,Chanona J,Suarez J,Pastelin G

    更新日期:2007-07-02 00:00:00

  • Apoptosis, 5-fluorouracil sensitivity and expression of apoptotic proteins in a human ectocervical cell carcinogenesis model using different media.

    abstract::Apoptosis has received widespread attention for its essential roles in biology, medicine and cancer. We previously found that normal, human papillomavirus (HPV) 16-immortalized and their transformed endocervical cells were increasingly resistant to apoptosis induced by a cancer therapeutic drug. Here, analogously, ano...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01561-9

    authors: Mo B,Pater A

    更新日期:2003-04-25 00:00:00

  • A reduction of epidermal growth factor receptor is involved in brefelamide-induced inhibition of phosphorylation of ERK in human astrocytoma cells.

    abstract::Brefelamide is an aromatic amide isolated from Dictyostelium cellular slime molds. We found that brefelamide has a potent inhibitory growth effect measured by MTT assay in 1321N1 human astrocytoma cells. The inhibition was associated with reduced phosphorylation of extracellular signal-regulated kinase (ERK). Brefelam...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.06.030

    authors: Honma S,Saito M,Kikuchi H,Saito Y,Oshima Y,Nakahata N,Yoshida M

    更新日期:2009-08-15 00:00:00

  • Altered binding properties of beta-adrenergic receptors and lack of coupling to adenylate cyclase in P815 mastocytoma cells.

    abstract::P815, a murine mastocytoma cell line, possesses beta-adrenergic binding sites as assessed by using [3H]dihydroalprenolol (antagonist) and [3H]hydroxybenzylisoproterenol (agonist). The number of binding sites per cell was 29 000 for the agonist and 75 000 for the antagonist, as determined by direct binding assays and i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90717-4

    authors: Durieu-Trautmann O,Delavier-Klutchko C,Hoebeke J,Strosberg AD

    更新日期:1985-01-22 00:00:00

  • Neurotoxic effect of prenatal exposure to MPTP on the dopaminergic systems of the marmoset brain.

    abstract::MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) was incidentally administered to pregnant marmosets during the whole gestational period, except for the last 15 days before term. The infant monkeys were killed 5 months after birth, and dopamine and its metabolites were measured in the striatum and the nucleus accum...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90873-3

    authors: Pérez-Otaño I,Oset C,Trinidad Herrero M,Luquin MR,Kupsch A,Oertel W,Obeso JA,Del Río J

    更新日期:1992-07-07 00:00:00

  • Pharmacological evidence for selective inhibition of gastric acid secretion by telenzepine, a new antimuscarinic drug.

    abstract::The new antisecretory drug, telenzepine (4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno-[3,4 - b][1,5]benzodiazepin-10-one), was investigated for its inhibition of functionally intact muscarinic receptors involved in gastric acid secretion in rabbit fundic glands, perfused mouse stomach in vitro, p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90498-4

    authors: Eltze M,Gönne S,Riedel R,Schlotke B,Schudt C,Simon WA

    更新日期:1985-06-07 00:00:00

  • Cadherins as novel targets for anti-cancer therapy.

    abstract::The cell adhesion molecules N-, VE- and OB-cadherin have been implicated as regulators of tumor growth and metastasis. We discuss evidence that N- and VE-cadherin play a key role in promoting blood vessel formation and stability, processes which are essential for tumor growth. Secondly, we describe the potential invol...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2009.05.033

    authors: Blaschuk OW,Devemy E

    更新日期:2009-12-25 00:00:00

  • GABA-mediated potentiation of amine release from nigrostriatal dopamine neurones in vitro.

    abstract::The uptake and release of 3H-dopamine was studied in slices of corpus striatum and substantia nigra in the presence of nialamide. High potassium triggered the outflow of tritium in both brain structures and this release was potentiated by GABA in a dose related fashion, whereas the spontaneous overflow of radioactivit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(79)90127-4

    authors: Starr MS

    更新日期:1979-01-15 00:00:00

  • Influence of pharmacologically-induced experimental anxiety on nociception and antinociception in rats.

    abstract::Animal studies reveal that diverse environmental stimuli that generate anxiety-like behaviors also induce antinociception; conversely, clinical data show that pain perception is reduced under anxiolysis. This study was conducted to investigate the influence of pharmacologically induced-anxiety on nociception and antin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.060

    authors: Jiménez-Velázquez G,Fernández-Guasti A,López-Muñoz FJ

    更新日期:2006-10-10 00:00:00

  • Platycodin D-induced apoptosis through nuclear factor-kappaB activation in immortalized keratinocytes.

    abstract::Platycodi Radix is the root of Platycodon grandiflorum and it is widely used in the traditional Oriental medicine as an expectorant for pulmonary diseases and a remedy for respiratory disorders. Platycodin D is the major constituent of triterpene saponins in the root. This study investigates apoptosis by platycodin D ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.03.012

    authors: Ahn KS,Hahn BS,Kwack K,Lee EB,Kim YS

    更新日期:2006-05-10 00:00:00

  • A novel Pseudolaric acid B derivative, Hexahydropseudolaric acid B, exterts an immunomodulatory effect in vitro/in vivo evaluation.

    abstract::Identification of immunosuppressants from natural sources has a proven track record in immune mediated disorders. Pseudolaric acid B is a diterpenoid isolated from the roots of Pseudolarix amabilis, possessing potent immunomodulatory effect. However, the cytotoxicity limits its future clinical application. The purpose...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.10.009

    authors: Li T,Chen H,Yang Z,Wang W,Wang YT,Zhang LM,Zhao JH,Zhou X,Li YM

    更新日期:2014-12-15 00:00:00

  • A pharmacological profile of the high-affinity GluK5 kainate receptor.

    abstract::Mouse GluK5 was expressed in Sf9 insect cells and radiolabelled with [(3)H]-kainate in receptor binding assays (Kd=6.9nM). Western immunoblotting indicated an Sf9 GluK5 band doublet corresponding to the glycosylated (128kDa) and deglycosylated (111kDa) protein, which was identical to the band pattern of native rat bra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.06.049

    authors: Møllerud S,Kastrup JS,Pickering DS

    更新日期:2016-10-05 00:00:00

  • Effects of paxilline on K+ channels in rat mesenteric arterial cells.

    abstract::The effects of paxilline, a mycotoxin, on whole-cell outward currents from freshly isolated cells of the rat mesenteric artery were studied. Paxilline inhibited a component of the outward current that was also sensitive to iberiotoxin. Inhibition could be observed at a concentration of 10 nM and complete inhibition of...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00188-0

    authors: Li G,Cheung DW

    更新日期:1999-05-07 00:00:00

  • The antinociceptive effect of leukotriene D(4) receptor antagonist, MK-571, in mice: possible involvement of opioidergic mechanism.

    abstract::The effect of a leukotriene D(4) receptor antagonist, (3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl(3-dimethyl amino-3-oxo propyl)thio)methyl)thio) propanoic acid (L-660,711; MK-571), was investigated on nociceptive responses in mice using three different assays: acetic-acid-induced abdominal constrictions, formalin ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00756-6

    authors: Gök S,Onal A,Cinar MG,Evinç A

    更新日期:1999-12-15 00:00:00

  • Antiarrhythmic action and protection of ischaemia myocardium after beta-blockade with bevantolol.

    abstract::In the present study 12 of 13 untreated pigs died of ventricular fibrillation during three 10 min episodes of left anterior descending coronary artery occlusion interrupted by 20 min of reperfusion. The selective beta-adrenoceptor antagonist bevantolol in a dose of 1.5 mg X kg-1, but not 0.5 mg X kg-1, offered nearly ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90645-4

    authors: Verdouw PD,Van Bremen RH,Verkeste CM,Van der Giessen WJ

    更新日期:1985-05-20 00:00:00

  • The effect of 5-hydroxytryptamine on the chick biventer cervicis muscle.

    abstract::The actions of 5-hydroxytryptamine have been studied in the chick biventer cervicis nerve--muscle preparation. At concentrations between 2.5 X 10(-3) and 3.7 X 10(-3) M, 5HT produced a transient increase in responses to indirect stimulation, but not to direct stimulation. At higher concentrations, 5HT produced a rever...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90095-4

    authors: Teerapong P,Harvey AL

    更新日期:1977-07-15 00:00:00

  • Differences in G-protein activation by mu- and delta-opioid, and cannabinoid, receptors in rat striatum.

    abstract::Receptor activation of G-proteins can be measured by agonist-stimulated [35S]GTP gamma S binding in the presence of excess guanosine diphosphate (GDP). To determine whether opioid and cannabinoid receptor-mediated G-protein activation correlate with their receptor densities, this study compared opioid- and cannabinoid...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00211-7

    authors: Sim LJ,Selley DE,Xiao R,Childers SR

    更新日期:1996-06-20 00:00:00

  • Temperature dependence of angiotensin II-mediated depolarisation of the rat isolated nodose ganglion.

    abstract::The ability of angiotensin II (A II) and 5-hydroxytryptamine (5-HT) to depolarise the rat isolated nodose ganglion preparation was examined. 5-HT depolarised the nodose ganglion, both at room temperature (20-24 degrees C) and at 35-37 degrees C. However, A II depolarised the nodose ganglion only under the latter condi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90217-t

    authors: Widdop RE,Krstew E,Jarrott B

    更新日期:1990-08-21 00:00:00

  • Vasopressin inhibition of human platelet adenylate cyclase: variable responsiveness between donors and involvement of a G-protein different from Gi.

    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

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90020-9

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

    更新日期:1988-06-10 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

    doi:10.1016/j.ejphar.2009.03.031

    authors: Deka DK,Mishra SK,Raviprakash V

    更新日期:2009-05-01 00:00:00

  • Arachidonyl-2'-chloroethylamide, a highly selective cannabinoid CB1 receptor agonist, enhances the anticonvulsant action of valproate in the mouse maximal electroshock-induced seizure model.

    abstract::Endogenous cannabinoid ligands and cannabinoid CB(1) receptor agonists have been shown to exert potent anticonvulsant effects in various experimental models of epilepsy. The purpose of this study was to determine the effects of arachidonyl-2'-chloroethylamide (ACEA; N-(2-chloroethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.07.037

    authors: Luszczki JJ,Czuczwar P,Cioczek-Czuczwar A,Czuczwar SJ

    更新日期:2006-10-10 00:00:00

  • Possible involvement of S-nitrosylation of brain cyclooxygenase-1 in bombesin-induced central activation of adrenomedullary outflow in rats.

    abstract::We previously reported that both nitric oxide (NO) generated from NO synthase by bombesin and NO generated from SIN-1 (NO donor) activate the brain cyclooxygenase (COX) (COX-1 for bombesin), thereby eliciting the secretion of both catecholamines (CA) from the adrenal medulla by brain thromboxane A(2)-mediated mechanis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.01.005

    authors: Tanaka K,Shimizu T,Lu L,Yokotani K

    更新日期:2012-03-15 00:00:00

  • Role of hydrogen sulfide in the formalin-induced orofacial pain in rats.

    abstract::Hydrogen sulfide (H2S) is a gasotransmitter synthesized in peripheral tissues by the enzyme cystathionine gamma-lyase (CSE). This gas has been documented to be involved in a wide variety of processes including inflammation and nociception. The aim of the present study was to investigate the role of the peripheral H2S ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.05.023

    authors: Donatti AF,Araujo RM,Soriano RN,Azevedo LU,Leite-Panissi CA,Branco LG

    更新日期:2014-09-05 00:00:00

  • Human saphenous vein contains both endothelin ETA and ETB contractile receptors.

    abstract::We have investigated the endothelin receptor subtypes mediating contraction in isolated preparations of human saphenous vein. Endothelin-1 (EC50: 17.8 nM), endothelin-3 (EC50: 82.3 nM) and the endothelin ETB receptor-selective agonists, [Ala1,3,11,15]endothelin-1 (EC50: 63 nM) and sarafotoxin S6c (EC50: 0.75 nM) all p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90144-9

    authors: White DG,Garratt H,Mundin JW,Sumner MJ,Vallance PJ,Watts IS

    更新日期:1994-05-23 00:00:00

  • Rotigotine protects against glutamate toxicity in primary dopaminergic cell culture.

    abstract::In Parkinson disease the degeneration of dopaminergic neurones is believed to lead to a disinhibition of the subthalamic nucleus thus increasing the firing rate of the glutamatergic excitatory projections to the substantia nigra. In consequence, excessive glutamatergic activity will cause excitotoxicity and oxidative ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.12.014

    authors: Oster S,Radad K,Scheller D,Hesse M,Balanzew W,Reichmann H,Gille G

    更新日期:2014-02-05 00:00:00

  • Chlorimipramine--but not imipramine--rapidly reduces [3H]imipramine binding in human platelet membranes.

    abstract::A single dose of 50 mg chlorimipramine was followed by a rapid and pronounced decrease in [3H]imipramine binding to platelet membranes. Incubation of human platelets or platelet membranes with 25 nM chlorimipramine similarly reduced [3H]imipramine binding. Imipramine, desmethylchlorimipramine, chlorpromazine and some ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90753-3

    authors: Mellerup ET,Plenge P

    更新日期:1986-07-15 00:00:00

  • Hsp70 promotes synaptic transmission in brain slices damaged by contact with blood clot.

    abstract::Neurotrophic and neuroprotective properties of Hsp70 were studied in olfactory cortex slices of hypertensive rats under normal conditions and under influence of autologous blood (blood clot). Under normal conditions, synaptic response in slices depended on Hsp70 amount in medium. Incubation of slices with Hsp70 showed...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.12.004

    authors: Mokrushin AA,Pavlinova LI

    更新日期:2012-02-29 00:00:00