The metabotropic glutamate receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) blocks fear conditioning in rats.

Abstract:

:Glutamate receptors play an essential role in fear-related learning and memory. The present study was designed to assess the role of the group I metabotropic glutamate receptor (mGluR) subtype 5 in the acquisition and retrieval of conditioned fear in rats. The selective mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) was applied systemically (0.0, 0.3, 3.0, 30.0 mg/kg per os) 60 min before the acquisition training and before the expression of conditioned fear, respectively, in the fear-potentiated startle paradigm. MPEP dose-dependently blocked the acquisition of fear. This effect was not due to state-dependent learning. MPEP also prevented the expression of fear at a dose of 30.0 mg/kg. As a positive control for these effects, we showed that the benzodiazepine anxiolytic compound diazepam (1.25 mg/kg intraperitoneally) also blocked acquisition and expression of fear potentiated startle. MPEP did not affect the baseline startle magnitude, short-term habituation of startle, sensitisation of startle by footshocks or prepulse inhibition of startle. These data indicate a crucial role for mGluR5 in the regulation of fear conditioning. In the highest dose MPEP might exert anxiolytic properties.

journal_name

Neuropharmacology

journal_title

Neuropharmacology

authors

Schulz B,Fendt M,Gasparini F,Lingenhöhl K,Kuhn R,Koch M

doi

10.1016/s0028-3908(01)00036-3

subject

Has Abstract

pub_date

2001-07-01 00:00:00

pages

1-7

issue

1

eissn

0028-3908

issn

1873-7064

pii

S0028390801000363

journal_volume

41

pub_type

杂志文章
  • Depletion of nucleus accumbens dopamine leads to impaired reward and aversion processing in mice: Relevance to motivation pathologies.

    abstract::Dopamine (DA) neurotransmission, particularly the ventral tegmental area-nucleus accumbens (VTA-NAcc) projection, underlies reward and aversion processing, and deficient DA function could underlie motivational impairments in psychiatric disorders. 6-hydroxydopamine (6-OHDA) injection is an established method for chron...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2016.03.048

    authors: Bergamini G,Sigrist H,Ferger B,Singewald N,Seifritz E,Pryce CR

    更新日期:2016-10-01 00:00:00

  • Cannabinoid CB(1) receptor activation stimulates neurite outgrowth and inhibits capsaicin-induced Ca(2+) influx in an in vitro model of diabetic neuropathy.

    abstract::Cannabinoid CB(1) receptors mediate, in part, the neuroprotectant properties of endocannabinoids, and altered signalling via the CB(1) receptor may contribute to the pathogenesis of diabetic neuropathy. We investigated CB(1) receptor function in PC12 cells differentiated into a neuronal phenotype with nerve growth fac...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2009.04.017

    authors: Zhang F,Challapalli SC,Smith PJ

    更新日期:2009-08-01 00:00:00

  • Surface expression and metabolic half-life of AMPA receptors in cultured rat cerebellar granule cells.

    abstract::The surface expression and metabolic turnover time of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) receptors are important factors in determining the involvement of these proteins in synaptic function. We used the membrane-impermeant chemical crosslinking reagent BS3 and subsequent immunoblot analysis t...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(98)00135-x

    authors: Archibald K,Perry MJ,Molnár E,Henley JM

    更新日期:1998-10-01 00:00:00

  • Posterior hypothalamic receptors involved in the cardiovascular changes elicited by electrical stimulation of the rostral ventrolateral medulla.

    abstract::The posterior hypothalamic receptors involved in the cardiovascular responses to electrical stimulation of the rostral ventrolateral medulla were investigated in urethane-anaesthetized rats. Electrical stimulation of the rostral ventrolateral medulla produced a significant increase in systolic blood pressure. This res...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(91)90183-c

    authors: Bachelard H,Rivest R,Marsden CA

    更新日期:1991-07-01 00:00:00

  • Behavioural phenotype of histamine H4 receptor knockout mice: Focus on central neuronal functions.

    abstract::The functional expression of H4 receptors (H4R) within neurons of the central nervous system has been recently reported, but their role is poorly understood. The present study aims to elucidate the role of neuronal H4R by providing the first description of the behavioural phenotype of H4R-deficient (H4R knockout, H4R-...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2016.11.023

    authors: Sanna MD,Ghelardini C,Thurmond RL,Masini E,Galeotti N

    更新日期:2017-03-01 00:00:00

  • Is ganglionic transmission through nicotinic receptors essential for the peristaltic reflex in the guinea-pig ileum?

    abstract::Peristaltic reflex activity in the guinea-pig isolated ileum was elicited by slow intraluminal infusion of Tyrode solution. The reflex was abolished by the ganglionic blocking drug hexamethonium. However, in more than half of the preparations, the peristaltic reflex was restored by the opioid antagonist naloxone. Hexa...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(87)90018-9

    authors: Barthó L,Holzer P,Lembeck F

    更新日期:1987-11-01 00:00:00

  • Intracerebroventricular administration of ethylcholine mustard aziridinium ion (AF64A) reduces release of acetylcholine from rat hippocampal slices.

    abstract::Ethylcholine mustard aziridinium ion (AF64A), or vehicle, was infused bilaterally (3 nmol/3 microliter per side) into the lateral ventricles of rats. The effect of such treatment on various cholinergic responses was measured in the hippocampus, cortex and striatum. Potassium-stimulated release of acetylcholine from su...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(85)90031-0

    authors: Leventer S,McKeag D,Clancy M,Wulfert E,Hanin I

    更新日期:1985-05-01 00:00:00

  • Pharmacological characterization of serotonin 5-HT3 receptor-mediated electrical response in cultured mouse neuroblastoma cells.

    abstract::The aim of this study was to investigate the pharmacological characteristics of the 5-hydroxytryptamine-(5-HT)-induced electrical response in cultured neuroblastoma N1E-115 cells of the mouse. In these cells 5-HT induces a transient membrane depolarization, which is associated with a transient inward current, that has...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(88)90048-2

    authors: Neijt HC,te Duits IJ,Vijverberg HP

    更新日期:1988-03-01 00:00:00

  • Changes in metabotropic glutamate receptor 1-8 gene expression in the rodent basal ganglia motor loop following lesion of the nigrostriatal tract.

    abstract::Metabotropic glutamate (mGlu) receptors in the basal ganglia motor loop may increase cell excitability (Group I) or modulate neurotransmitter release (Group I, II and III). Nigrostriatal tract degeneration in Parkinson's disease (PD) produces downstream pathological disturbances in glutamate and GABA transmission. The...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(02)00090-4

    authors: Messenger MJ,Dawson LG,Duty S

    更新日期:2002-08-01 00:00:00

  • Chronic alcohol exposure reduces acetylated histones in the sleep-wake regulatory brain regions to cause insomnia during withdrawal.

    abstract:BACKGROUND:Alcohol use disorder (AUD) develops after chronic and heavy use of alcohol. Insomnia, a hallmark of AUD, plays a crucial role in the development of AUD. However, the causal mechanisms are unknown. Since chronic alcohol reduces acetylated histones and disrupts the epigenome, we hypothesized that chronic alcoh...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2020.108332

    authors: Sharma R,Sahota P,Thakkar MM

    更新日期:2020-12-01 00:00:00

  • Regional differences in the effects of isoflurane on neurotransmitter release.

    abstract::Stimulus evoked neurotransmitter release requires that Na(+) channel-dependent nerve terminal depolarization be transduced into synaptic vesicle exocytosis. Inhaled anesthetics block presynaptic Na(+) channels and selectively inhibit glutamate over GABA release from isolated nerve terminals, indicating mechanistic dif...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2011.05.013

    authors: Westphalen RI,Kwak NB,Daniels K,Hemmings HC Jr

    更新日期:2011-09-01 00:00:00

  • GABA(B) receptor activation inhibits dopamine D1 receptor-mediated facilitation of [(3)H]GABA release in substantia nigra pars reticulata.

    abstract::GABA(B) receptors inhibit and dopamine D1 receptors stimulate the release of GABA from striatal terminals in the pars reticulata of the substantia nigra. Here we have studied the interaction between both classes of receptors by exploring the effect of GABA(B) receptors upon the stimulation of depolarization-induced [(...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2007.07.014

    authors: Nava-Asbell C,Paz-Bermudez F,Erlij D,Aceves J,Florán B

    更新日期:2007-10-01 00:00:00

  • Prenatal exposure to the cannabinoid receptor agonist WIN 55,212-2 increases glutamate uptake through overexpression of GLT1 and EAAC1 glutamate transporter subtypes in rat frontal cerebral cortex.

    abstract::Prenatal exposure to the CB1 receptor agonist (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl)-pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone) mesylate (WIN) at a daily dose of 0.5 mg/kg, and Delta9-tetrahydrocannabinol (Delta9-THC) at a daily dose of 5 mg/kg, reduced dialysate glutamate levels in ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2007.05.019

    authors: Castaldo P,Magi S,Gaetani S,Cassano T,Ferraro L,Antonelli T,Amoroso S,Cuomo V

    更新日期:2007-09-01 00:00:00

  • Anticonvulsant action and long-term effects of gabapentin in the immature brain.

    abstract::The anticonvulsant action and the long-term effects on learning, memory and behavior of the new generation antiepileptic drug gabapentin (GBP) were investigated in immature animals. Kainic acid (KA) was administered to rats on postnatal day (P) 35. Animals were treated with GBP or saline from P36 to P75 and spontaneou...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(00)00103-9

    authors: Cilio MR,Bolanos AR,Liu Z,Schmid R,Yang Y,Stafstrom CE,Mikati MA,Holmes GL

    更新日期:2001-01-01 00:00:00

  • Sub-efficacious doses of phosphodiesterase 4 and 5 inhibitors improve memory in a mouse model of Alzheimer's disease.

    abstract::Cyclic nucleotides cAMP and cGMP cooperate to ensure memory acquisition and consolidation. Increasing their levels by phosphodiesterase inhibitors (PDE-Is) enhanced cognitive functions and rescued memory loss in different models of aging and Alzheimer's disease (AD). However, side effects due to the high doses used li...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2018.06.002

    authors: Gulisano W,Tropea MR,Arancio O,Palmeri A,Puzzo D

    更新日期:2018-08-01 00:00:00

  • Disrupting GluA2 phosphorylation potentiates reinstatement of cocaine seeking.

    abstract::Addiction is associated with changes in synaptic plasticity mediated, in part, by alterations in the trafficking and stabilization of AMPA receptors at synapses within the nucleus accumbens. Exposure to cocaine can lead to protein kinase C-mediated phosphorylation of GluA2 AMPA subunits and this phosphorylation event ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2016.09.010

    authors: Briand LA,Deutschmann AU,Ellis AS,Fosnocht AQ

    更新日期:2016-12-01 00:00:00

  • The hypothermic response of mice to delta-9-tetrahydrocannabinol is enhanced by chlorpromazine, thioxanthenes, alpha-adrenoceptor antagonists and pentolinium but not by SCH 23390 or sulpiride.

    abstract::Chlorpromazine, given either subcutaneously (0.375 mg/kg) or unilaterally into the preoptic/anterior hypothalamic area through a chronically implanted cannula (20 micrograms), was found to enhance the hypothermic response to delta-9-tetrahydrocannabinol (THC; 5 mg/kg i.p.) in unrestrained adult male MF1 mice, kept at ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(88)90164-5

    authors: Pertwee RG,Hedley D,McQueen AS,Gentleman SM

    更新日期:1988-02-01 00:00:00

  • Effects of apomorphine and methamphetamine on a quickly-learned conditioned-suppression response in rats.

    abstract::Rats exhibited a marked suppression of motor activity when placed in the same chamber where they had been given electric shocks. Administration of apomorphine-HCl (0.1, 0.5 and 1.0 mg/kg, i.p.) attenuated the conditioned suppression, dose-dependently, but did not facilitate motor activity of control (i.e. non-shocked)...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(83)90125-9

    authors: Kameyama T,Nagasaka M

    更新日期:1983-07-01 00:00:00

  • Behavioral and serotonergic consequences of decreasing or increasing hippocampus brain-derived neurotrophic factor protein levels in mice.

    abstract::Antidepressants such as Selective Serotonin Reuptake Inhibitors (SSRI) act as indirect agonists of serotonin (5-HT) receptors. Although these drugs produce a rapid blockade of serotonin transporters (SERTs) in vitro, several weeks of treatment are necessary to observe clinical benefits. This paradox has not been solve...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2008.08.001

    authors: Deltheil T,Guiard BP,Cerdan J,David DJ,Tanaka KF,Repérant C,Guilloux JP,Coudoré F,Hen R,Gardier AM

    更新日期:2008-11-01 00:00:00

  • A bradycardiac agent ZD7288 blocks the hyperpolarization-activated current (I(h)) in retinal rod photoreceptors.

    abstract::Recently it has been reported that "I(f) channel blockers", which block the hyperpolarization-activated inward current (I(f)) in heart sino atrial node cells, also block the hyperpolarization-activated inward current (I(h)) in other tissues. Here we compared the effects of one of these agents, ZD7288 [4-(N-ethyl-N-phe...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(99)00207-5

    authors: Satoh TO,Yamada M

    更新日期:2000-04-27 00:00:00

  • Pharmacological characterization of mGlu1 receptors in cerebellar granule cells reveals biased agonism.

    abstract::The majority of existing research on the function of metabotropic glutamate (mGlu) receptor 1 focuses on G protein-mediated outcomes. However, similar to other G protein-coupled receptors (GPCR), it is becoming apparent that mGlu1 receptor signaling is multi-dimensional and does not always involve G protein activation...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2015.02.007

    authors: Hathaway HA,Pshenichkin S,Grajkowska E,Gelb T,Emery AC,Wolfe BB,Wroblewski JT

    更新日期:2015-06-01 00:00:00

  • In vivo assessment of release and metabolism of dopamine in the ventrolateral striatum of awake rats following administration of dopamine D1 and D2 receptor agonists and antagonists.

    abstract::The ability of specific dopamine (DA) receptor agonists and antagonists to modify the release and metabolism of DA in the ventrolateral striatum of awake rats was assessed using in vivo microdialysis. The specific DA D2 receptor antagonist, raclopride (0.1, 0.5 and 2.0 mg/kg, i.p.), dose-dependently increased release ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(91)90022-4

    authors: See RE,Sorg BA,Chapman MA,Kalivas PW

    更新日期:1991-12-01 00:00:00

  • Neurochemical and behavioral effects of acute and chronic treatment with apomorphine in rats.

    abstract::In three experiments, rats were injected once daily with 5.0 mg/kg apomorphine or vehicle and tested for locomotor activity for 10-14 days. In each experiment, apomorphine produced behavioral sensitization, characterized by a progressively greater increase in locomotor activity with each succeeding injection. On day 1...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(91)90203-n

    authors: Rowlett JK,Mattingly BA,Bardo MT

    更新日期:1991-02-01 00:00:00

  • Enhanced spontaneous transmitter release at murine motor nerve terminals with cyclosporine.

    abstract::Cyclosporine, a calcineurin inhibitor, significantly enhances spontaneous acetylcholine release after a brief tetanus and potentiates the effect of phorbol 12,13-dibutyrate. Both actions are prevented by the protein kinase C inhibitor, bisindolylmaleimide iodide. Protein kinase C and calcineurin thus play important ro...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(98)00178-6

    authors: Lin MJ,Lin-Shiau SY

    更新日期:1999-01-01 00:00:00

  • Interplay between PACAP and NO in mouse ileum.

    abstract::We investigated the possibility that pituitary adenylate cyclase activating peptide (PACAP) has a role in the control of contractility in the mouse ileum. PACAP-(1-27) produced tetrodotoxin (TTX)-insensitive, concentration-dependent reduction of the amplitude of the spontaneous contractions of longitudinal muscle up t...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2003.09.011

    authors: Zizzo MG,Mulè F,Serio R

    更新日期:2004-03-01 00:00:00

  • Depression-related behavior and mechanical allodynia are blocked by 3-(4-fluorophenylselenyl)-2,5-diphenylselenophene in a mouse model of neuropathic pain induced by partial sciatic nerve ligation.

    abstract::Clinically, it is suggested that chronic pain might induce mood disorders like depression and anxiety. Based on this antidepressant drugs have emerged as a new therapy for pain. In this study, the effect of acute and subchronic treatments with 3-(4-fluorophenylselenyl)-2,5-diphenylselenophene (F-DPS) on behavioral cha...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2014.01.020

    authors: Gai BM,Bortolatto CF,Brüning CA,Zborowski VA,Stein AL,Zeni G,Nogueira CW

    更新日期:2014-04-01 00:00:00

  • Binding characteristics of kappa opioids in rat brain. A comparison of in vitro binding paradigms.

    abstract::Putative kappa binding was investigated in homogenates of the brain of the rat using [3H]ethylketocylazocine and [3H]diprenorphine under conditions where mu and delta sites were blocked. Under blocked conditions, the binding of [3H]ethylketocyclazocine labelled a single site, as defined by kinetic and equilibrium anal...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(85)90169-8

    authors: Weyhenmeyer JA,Mack KJ

    更新日期:1985-02-01 00:00:00

  • Tolerance to nicotine-induced sympathoadrenal stimulation and cross-tolerance to stress: differential central and peripheral mechanisms in rats.

    abstract::Nicotine stimulates the secretion of catecholamines from sympathetic nerve endings and adrenal medulla by acting on peripheral nicotinic cholinergic receptors. Nicotine is also a potent stimulant in the central nervous system but the significance of nicotinic receptors in brain in mediating cardiovascular and sympatho...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(90)90071-x

    authors: Kiritsy-Roy JA,Mousa SA,Appel NM,Van Loon GR

    更新日期:1990-06-01 00:00:00

  • Okadaic acid blocks the effects of 5-aza-2-deoxycytidine on consolidation, acquisition and retrieval of morphine-induced place preference in rats.

    abstract::Recent studies indicated that epigenetic modification, especially DNA methylation, play an important role in the persistence of addiction-related memory. 5-aza-2-deoxycytidine (5-aza), an inhibitor of DNA methyltransferases, was approved for clinical treatment. However, it is not clear whether 5-aza is involved in opi...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2014.08.005

    authors: Zhang JJ,Han J,Sui N

    更新日期:2014-11-01 00:00:00

  • Interactions between CAP70 and actinfilin are important for integrity of actin cytoskeleton structures in neurons.

    abstract::The integrity of dynamic actin structures is coupled to a variety of neurological processes. Actin-binding proteins play a critical role in regulating actin structure dynamics. A link between actin-binding proteins and receptor interacting scaffolding proteins may provide a conduit for transmitting signaling events to...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2005.05.022

    authors: Chen Y,Li M

    更新日期:2005-12-01 00:00:00