Effects of baclofen on amino acid release.

Abstract:

:This study showed the effects of baclofen on endogenous excitatory (Glu and Asp) and non-excitatory (Tau, Gly and Ala) amino acid release. (A) Release was stimulated by K+ 30 mM in rat frontal cortex slices in vitro (evoked release in ng/g tissue per 5 min): 3739 +/- 215 (Asp), 3429 +/- 357 (Glu), 763 +/- 181 (Tau), 945 +/- 71 (Ala), 468 +/- 44 (Gly). (B) Release was largely Ca(2+)-dependent for all amino acids but Ca(2+)-independent release was observed for Asp and Glu (29 and 32%, of total evoked release respectively). (C) Ca(2+)-dependent release was inhibited by baclofen 100 microM (% of inhibition taking as 100%, the Ca(2+)-dependent release in the absence of baclofen): 46 (Asp), 96 (Glu) (85% inhibition by baclofen 10 microM), 100 (Tau), 77 (Ala). Ca(2+)-independent release was inhibited: 87 and 88% (Asp), 85 and 95% (Glu) by baclofen 10 and 100 microM respectively. It is concluded that baclofen at a high concentration inhibits the evoked release of Glu, Asp, Tau and Ala due to inhibition of the Ca(2+)-dependent fraction and also of the Ca(2+)-independent component in the case of Glu and Asp. Baclofen at a low concentration inhibits only Glu- and Asp-evoked release (total release) due to inhibition of both Ca(2+)-dependent and -independent fractions in the case of Glu and to inhibition of the Ca(2+)-independent fraction in the case of Asp. The possibility that baclofen might affect the Ca(2+)-independent carrier-mediated release of Glu-Asp is discussed.

journal_name

Eur J Pharmacol

authors

Losada ME,Acosta GB

doi

10.1016/0014-2999(92)94813-b

keywords:

subject

Has Abstract

pub_date

1992-11-24 00:00:00

pages

21-5

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(92)94813-B

journal_volume

224

pub_type

杂志文章
  • Substance P suppresses stress-induced eating.

    abstract::Parenterally administered substance P suppressed stress-induced eating (resulting from mild tail pinch) in a dose-related manner, whereas at similar or higher doses of substance P starvation-induced eating was uneffected. This specific effect of substance P on stress-induced eating is possibly associated with alterati...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90514-2

    authors: Morley JE,Levine AS

    更新日期:1980-10-17 00:00:00

  • Chronic high dose P2X7 receptor inhibition exacerbates cancer-induced bone pain.

    abstract::The functional role of P2X7 receptor (P2X7R) inhibition in cancer-induced bone pain has been highly contradictory. Whereas knockout studies have suggested pro-nociceptive effects, pharmacological studies suggest anti-nociceptive or no effect. The discrepancy is likely linked to the highly polymorphic nature of the P2X...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.12.032

    authors: Falk S,Appel CK,Bennedbæk HB,Al-Dihaissy T,Unger A,Dinkel K,Heegaard AM

    更新日期:2019-02-15 00:00:00

  • Activation of central muscarinic receptor type 1 prevents development of endotoxin tolerance in rat liver.

    abstract::Endotoxin tolerance is a mechanism in which cells receiving low doses of endotoxin, enter a transient phase with less inflammatory response to the next endotoxin challenges. Central nervous system is known to modulate systemic inflammation through activation of the cholinergic system; however, the role of central anti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.06.050

    authors: Eftekhari G,Hajiasgharzadeh K,Ahmadi-Soleimani SM,Dehpour AR,Semnanian S,Mani AR

    更新日期:2014-10-05 00:00:00

  • The actions of benzophenanthridine alkaloids, piperonyl butoxide and (S)-methoprene at the G-protein coupled cannabinoid CB₁ receptor in vitro.

    abstract::This investigation focused primarily on the interaction of two benzophenanthridine alkaloids (chelerythrine and sanguinarine), piperonyl butoxide and (S)-methoprene with G-protein-coupled cannabinoid CB(1) receptors of mouse brain in vitro. Chelerythrine and sanguinarine inhibited the binding of the CB(1) receptor ago...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.11.033

    authors: Dhopeshwarkar AS,Jain S,Liao C,Ghose SK,Bisset KM,Nicholson RA

    更新日期:2011-03-01 00:00:00

  • The actions of receptor-selective substance P analogs on myenteric neurons: an electrophysiological investigation.

    abstract::Intracellular recordings were made from myenteric neurons of the guinea-pig duodenum and the responses to local ejection of several substance P (SP) analogs were examined. It was found that senktide (succinyl-[Asp6,Me-Phe8]SP-(6-11)), a selective analog for the NK-3 (SP-N) receptor, was particularly effective in depol...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90612-7

    authors: Hanani M,Chorev M,Gilon C,Selinger Z

    更新日期:1988-08-24 00:00:00

  • AMP-activated kinase relaxes agonist induced contractions in the mouse aorta via effects on PKC signaling and inhibits NO-induced relaxation.

    abstract::Adenosine monophosphate activated kinase (AMPK), a regulator of cellular metabolism, has been shown to relax arterial smooth muscle via endothelium-dependent and independent mechanisms. We have examined the role of AMPK in different smooth muscles using the activating compound, 5-amino-4-imidazolecarboxamide riboside-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.07.025

    authors: Davis B,Rahman A,Arner A

    更新日期:2012-11-15 00:00:00

  • Dopamine D3 receptor density elevation in aged Fischer-344 x Brown-Norway (F1) rats.

    abstract::The density of dopamine D3 receptors was determined in young (4-month-old) and aged (37-month-old) Fischer-344 x Brown-Norway (F1) male rats using the putative D3 receptor-preferring agonist, [3H](+)-7.hydroxy-2-(N,N-di-n-propylamino)tetralin ([3H](+)-7-OH-DPAT). In the presence of the non-hydrolyzable GTP analog, 5'-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00354-8

    authors: Wallace DR,Booze RM

    更新日期:1996-07-25 00:00:00

  • Control of c-fos expression in STC-1 cells by peptidomimetic stimuli.

    abstract::Enteroendocrine cells respond to nutrient and non-nutrient stimuli in the gut lumen. The intestinal hormone cholecystokinin (CCK) is secreted in response to luminal fatty acids, amino acids, peptides and proteins. The peptidomimetic cephalosporins have been reported to provide model, stable, compounds with similar sec...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00076-5

    authors: Murai A,Noble PM,Deavall DG,Dockray GJ

    更新日期:2000-04-07 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

  • Interactions between regulatory proteins that bind to the nicotinic receptor beta4 subunit gene promoter.

    abstract::The genes encoding the alpha3, alpha5 and beta4 subunits of nicotinic acetylcholine receptors are tightly clustered within the genome. As these three subunits constitute the predominant acetylcholine receptor subtype expressed in the peripheral nervous system, their genomic proximity suggests a regulatory mechanism en...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00884-5

    authors: Melnikova IN,Yang Y,Gardner PD

    更新日期:2000-03-30 00:00:00

  • Systemic administration of lithium chloride and tacrine but not kainic acid augments citrulline content of rat brain.

    abstract::The effects of tacrine (5 mg/kg i.p.) in lithium chloride (LiCl; 12 mEq/kg i.p.)-pretreated (24 h beforehand) animals and of kainate (10 mg/kg i.p.) on brain citrulline, the co-product of nitric oxide (NO) synthesis, were studied in rats. High performance liquid chromatography analysis of whole brain tissue homogenate...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00689-3

    authors: Bagetta G,Rodinò P,Paoletti AM,Arabia A,Massoud R,Nisticò G

    更新日期:1995-12-27 00:00:00

  • Is NAN-190 an effective antagonist of the hypothermia and hyperglycemia induced by the 5-HT1A receptor agonist, 8-OH-DPAT?

    abstract::The putative 5-HT1A receptor antagonist properties of 1-(2-methoxyphenyl)-4-[4-(2-phtalimmido)butyl] piperazine (NAN-190) were studied in mice. The responses studied were hypothermia- and hyperglycemia-induced by the 5-HT1A agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). NAN-190 (0.3-3 mg/kg) did not anta...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90044-q

    authors: Wozniak KM,Durcan MJ,Linnoila M

    更新日期:1991-02-07 00:00:00

  • Tetranactin inhibits interleukin 1 beta and cAMP induction of group II phospholipase A2 in rat renal mesangial cells.

    abstract::Renal mesangial cells express secretory phospholipase A2 in response to two principal classes of activating signals that may interact in a synergistic fashion. These two groups of activators comprise inflammatory cytokines, such as interleukin 1 beta, and agents that elevate cellular levels of cAMP. Treatment of mesan...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00203-8

    authors: Walker G,Kunz D,Pignat W,Wiesenberg I,Van den Bosch H,Pfeilschifter J

    更新日期:1996-06-13 00:00:00

  • Iron deficiency-induced circadian rhythm reversal of dopaminergic-mediated behaviours and thermoregulation in rats.

    abstract::An iron-free diet for 28 days caused a reduced level of iron in the blood. Iron deficient rats exhibited a lower level of motor activity and reversed circadian rhythms of thermoregulation and motor activity. The hypothermic effect of d-amphetamine was significantly reduced in iron deficient rats, and the magnitude of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90048-0

    authors: Youdim MB,Yehuda S,Ben-Uriah Y

    更新日期:1981-09-24 00:00:00

  • Ziprasidone suppresses olanzapine-induced increases in ingestive behaviour in the rat.

    abstract::Many atypical antipsychotic drugs, such as olanzapine, induce significant weight gain. However, ziprasidone produces minimal weight gain, the mechanism of which remains unclear. The aim of the present study was to investigate whether ziprasidone would reduce the acute effect of olanzapine on feeding behaviour. The res...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.10.015

    authors: Kirk SL,Neill JC,Jones DN,Reynolds GP

    更新日期:2004-11-28 00:00:00

  • Infliximab reduces CD147, MMP-3, and MMP-9 expression in peripheral blood monocytes in patients with active rheumatoid arthritis.

    abstract::Recent studies have reported elevated expression levels in active rheumatoid arthritis patients of the cluster of differentiation (CD) 147 on CD14(+) peripheral blood monocytes and as a result, CD147 may be a target for the development of a novel rheumatoid arthritis therapy. This report describes the inhibitory effec...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1016/j.ejphar.2012.10.030

    authors: Huang J,Xie B,Li Q,Xie X,Zhu S,Wang M,Peng W,Gu J

    更新日期:2013-01-05 00:00:00

  • Derivatives of gecko cathelicidin-related antioxidant peptide facilitate skin wound healing.

    abstract::Cathelicidins are a class of gene-encoded multifunctional factors in host defence systems. They have recently attracted a great deal of attention as promising drug candidates. Cathelicidins are well studied in vertebrates, yet no studies have been reported concerning gecko cathelicidin. Recently, we identified a novel...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173649

    authors: Cai S,Lu C,Liu Z,Wang W,Lu S,Sun Z,Wang G

    更新日期:2021-01-05 00:00:00

  • Relationship between morphine and etonitazene-induced working memory impairment and analgesia.

    abstract::An 8-arm radial maze task was used to assess the possible role of the opiate system in the spatial memory of the rat. Increasing doses of etonitazene (0.005-0.06 mg/kg i.p.) and morphine (2.5-100 mg/kg i.p.) significantly impaired performance in the working memory components of the task. For both drugs this impairment...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90811-7

    authors: Braida D,Gori E,Sala M

    更新日期:1994-12-27 00:00:00

  • Desensitization of endogenous angiotensin II receptors in Xenopus oocytes: a role of protein kinase C.

    abstract::The inward chloride current induced by angiotensin II (AII) in Xenopus oocytes shows strong and homologous desensitization, and was suggested to be mediated by phosphatidylinositol (PI) hydrolysis (Sakuta et al., 1991, Eur. J. Pharmacol. Mol. Pharmacol. 208, 31). As a model of agonist-induced desensitization of recept...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(91)90049-n

    authors: Sakuta H,Sekiguchi M,Okamoto K,Sakai Y

    更新日期:1991-09-12 00:00:00

  • Discriminative stimulus effects of BAY 38-7271, a novel cannabinoid receptor agonist.

    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

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02697-3

    authors: De Vry J,Rüdiger Jentzsch K

    更新日期:2002-12-20 00:00:00

  • Antagonism of the anxiolytic action of diazepam and chlordiazepoxide by the novel imidazopyridines, EMD 39593 and EMD 41717.

    abstract::The imidazopyridines EMD 35993 and EMD 41717 antagonized the anticonflict actions of diazepam and chlordiazepoxide in rodent models which are predictive for anxiolytic action in man. In contrast to other described benzodiazepine antagonists, these compounds did not antagonize either the anticonvulsant or muscle relaxa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90582-4

    authors: Skolnick P,Paul S,Crawley J,Lewin E,Lippa A,Clody D,Irmscher K,Saiko O,Minck KO

    更新日期:1983-04-08 00:00:00

  • Role of cell-cell interactions in high mobility group box 1 cytokine activity in human peripheral blood mononuclear cells and mouse splenocytes.

    abstract::Cell-cell interaction through binding of intercellular adhesion molecule (ICAM), B7.1, B7.2 and CD40 on monocytes to their ligands on T-cells plays a number of roles in cytokine . High mobility group box 1 (HMGB1), an abundant and conserved nuclproduction and lymphocyte proliferationear protein, acts in the extracellu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.11.058

    authors: Kohka Takahashi H,Sadamori H,Liu K,Wake H,Mori S,Yoshino T,Yamamoto Y,Yamamoto H,Nishibori M

    更新日期:2013-02-15 00:00:00

  • Targeting different angiogenic pathways with combination of curcumin, leflunomide and perindopril inhibits diethylnitrosamine-induced hepatocellular carcinoma in mice.

    abstract::No effective chemopreventive agent has been approved against hepatocellular carcinoma (HCC) to date. Since HCC is one of the hypervascular solid tumors, blocking angiogenesis represents an intriguing approach to HCC chemoprevention. The aim of the current study was to examine the combined effect of the anti-angiogenic...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.11.022

    authors: Nasr M,Selima E,Hamed O,Kazem A

    更新日期:2014-01-15 00:00:00

  • Pleiotropic protective effects of Vitamin D against high fat diet-induced metabolic syndrome in rats: One for all.

    abstract::Several lines of evidence point to the association of vitamin D deficiency with the different components of metabolic syndrome. Yet, the effect of vitamin D supplementation on metabolic syndrome is not clearly elucidated. Herein, we tested the hypothesis that administration of vitamin D, either alone or in combination...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.10.031

    authors: Mostafa DK,Nasra RA,Zahran N,Ghoneim MT

    更新日期:2016-12-05 00:00:00

  • Lack of effect of atrial natriuretic factor on the tone induced in rat portal vein by platelet-activating factor.

    abstract::The spontaneous myogenic activity of the isolated rat portal vein was inhibited by atrial natriuretic factor or by sodium nitroprusside. These compounds were not effective on the tone induced by PAF-acether or carbachol. 8-Bromo cyclic GMP and dibutyryl cyclic AMP inhibited myogenic activity and reduced the agonist-in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90239-7

    authors: Hellegouarch A,Auguet M,Guillon JM,Baranes J,Pirotzky E,Braquet P

    更新日期:1988-01-12 00:00:00

  • Propofol facilitates climbing fiber-Purkinje cell synaptic transmission via NMDA receptor in vitro in mice.

    abstract::Propofol is generally used for the induction and maintenance of anesthesia in clinical procedures via activation of γ -aminobutyric acid A (GABAA) receptors. When administered at the clinical dose, propofol use is associated with movement disorders, including dystonia and ataxia, suggesting that propofol administratio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173474

    authors: Zhang XY,Zhang YD,Cui BR,Jin R,Chu CP,Jin XH,Qiu DL

    更新日期:2020-11-15 00:00:00

  • Bimoclomol elevates heat shock protein 70 and cytoprotects rat neonatal cardiomyocytes.

    abstract::Bimoclomol is a new compound that improves cell survival under experimental stress conditions partly by increasing intracellular heat shock proteins (HSPs). HSPs, especially HSP70, play a cytoprotective role in the rat heart. Rat neonatal cardiomyocytes were used to determine the ability of bimoclomol to induce HSP70 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01551-5

    authors: Polakowski JS,Wegner CD,Cox BF

    更新日期:2002-01-18 00:00:00

  • Repeated systemic administration of the mixed inhibitor of enkephalin-degrading enzymes, RB101, does not induce either antinociceptive tolerance or cross-tolerance with morphine.

    abstract::The potent analgesic responses elicited by systemic administration of RB101, N-[(R,S)-2-benzyl-3[(S)(2-amino-4-methylthio)butyldithio]-1-oxopro pyl]- 1-oxopropyl]-L-phenylalanine benzyl ester, a prodrug able to inhibit enkephalin-degrading enzymes completely after in vivo bioactivation, has made it possible to investi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90821-k

    authors: Noble F,Turcaud S,Fournié-Zaluski MC,Roques BP

    更新日期:1992-11-13 00:00:00

  • Capsaicin pretreatment does not inhibit the opioid withdrawal response in guinea-pigs.

    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

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90257-9

    authors: Chahl LA

    更新日期:1988-12-06 00:00:00

  • Role of Ca2+ in the vascular contraction caused by a thrombin receptor activating peptide.

    abstract::Thrombin receptor activating peptide (TRAP) caused a slowly developing, sustained contraction of endothelium denuded rat aortic rings. Both nifedipine (10 microM) and removal of Ca2+ from the physiological salt solution (PSS) caused significant (60-75%) reductions in the contractile response to TRAP. In Ca(2+)-free PS...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90613-0

    authors: Antonaccio MJ,Normandin D

    更新日期:1994-04-11 00:00:00