Molecular cloning, functional expression and pharmacological characterization of the human metabotropic glutamate receptor type 4.


:A cDNA encoding the human metabotropic glutamate receptor type 4 (hmGluR4) was isolated from human brain cDNA libraries by cross-hybridization with rat mGluR4 probes. The deduced amino acid sequence of human mGluR4 consists of 912 residues and shows a sequence identity of 96% to the amino acid sequence of rat mGluR4. Northern blot analyses indicate that hmGluR4 is strongly expressed in the cerebellum of the adult human brain but also at low levels in hippocampus, hypothalamus and thalamus. Stimulation of hmGluR4 with L-2-amino-4-phosphonobutyrate (L-AP4), L-serine-O-phosphate (L-SOP), L-glutamate or (1S,3R)-1-aminocyclo-pentane-1,3-dicarboxylic acid ((1S,3R)-ACPD) in stably transfected Chinese hamster ovary (CHO) cells depressed forskolin-induced cAMP accumulation, whereas quisqualate (0.5 mM) was ineffective. The rank order of agonist potencies is: L-AP4 > L-SOP > L-glutamate > (1S,3R)-ACPD > quisqualate. (R,S)-alpha-methyl-4-carboxyphenylglycine (1 mM), a reported antagonist at some mGluR subtypes, did not reduce the depression of forskolin-induced cAMP accumulation by L-AP4.






Flor PJ,Lukic S,Rüegg D,Leonhardt T,Knöpfel T,Kuhn R




Has Abstract


1995-02-01 00:00:00














  • Zaltoprofen inhibits bradykinin-induced responses by blocking the activation of second messenger signaling cascades in rat dorsal root ganglion cells.

    abstract::Bradykinin interacts with the bradykinin B2 receptor on dorsal root ganglion (DRG) neurons, setting off a series of reactions inside the cells that ultimately make the vanilloid receptor 1 more sensitive to a normal stimulus by activating various enzymes coupled with second messenger signaling cascades. Zaltoprofen, a...


    pub_type: 杂志文章


    authors: Tang HB,Inoue A,Oshita K,Hirate K,Nakata Y

    更新日期:2005-06-01 00:00:00

  • The kynurenine pathway and parasitic infections that affect CNS function.

    abstract::The kynurenine pathway of tryptophan metabolism has been implicated in brain function, immunoregulation, anti-microbial mechanisms and pregnancy. Some of these actions are due to depletion of tryptophan and others to the formation of biologically active metabolites. This review focuses on the roles of the kynurenine p...


    pub_type: 杂志文章,评审


    authors: Hunt NH,Too LK,Khaw LT,Guo J,Hee L,Mitchell AJ,Grau GE,Ball HJ

    更新日期:2017-01-01 00:00:00

  • Protein kinase C modulates the release of [3H]5-hydroxytryptamine in the spinal cord of the rat: the role of L-type voltage-dependent calcium channels.

    abstract::The present studies examined the relationship between protein kinase C (PKC) and L-type voltage-dependent calcium channels in modulating the release of neurotransmitter from K(+)-depolarized rat spinal cord synaptosomes. Activators of PKC, such as phorbol 12-myristate 13-acetate (PMA), mezerein and oleoyl acetylglycer...


    pub_type: 杂志文章


    authors: Gandhi VC,Jones DJ

    更新日期:1992-11-01 00:00:00

  • Introduction of the 5-HT3B subunit alters the functional properties of 5-HT3 receptors native to neuroblastoma cells.

    abstract::The identification of a second 5-HT(3) (5-HT(3B)) subunit provides an explanation for 5-HT(3) receptor heterogeneity. We investigated whether introduction of recombinant 5-HT(3B) subunits would alter the functional properties of mouse neuroblastoma 5-HT(3) receptors. RT-PCR analysis revealed that NB41A3 cells contain ...


    pub_type: 杂志文章


    authors: Stewart A,Davies PA,Kirkness EF,Safa P,Hales TG

    更新日期:2003-02-01 00:00:00

  • An in vitro mature spinal cord preparation from the rat.

    abstract::The preparation of an isolated hemisected spinal cord preparation, maintained in vitro, from mature (180-300 g body weight) rats is described. Sacral and coccygeal segments (S2-Co1) gave consistent ventral root reflexes (DR-VRP) from electrical stimulation of dorsal roots. The mean latency and amplitude of the fastest...


    pub_type: 杂志文章


    authors: Long SK,Evans RH,Cull L,Krijzer F,Bevan P

    更新日期:1988-05-01 00:00:00

  • The effect of a glycine derivative (CP 1552-S) on kindled seizures in rats.

    abstract::The effects of the glycine derivative, CP 1552-S (2-N-pentylaminoacetamide hydrochloride) were evaluated for potential anticonvulsant activity in rats which were cortically- or amygdaloid-kindled. Large doses (300-600 mg/kg, i.p.) of CP 1552 given 30 min before stimulation resulted in significant reductions in duratio...


    pub_type: 杂志文章


    authors: Albertson TE,Stark LG,Joy RM

    更新日期:1984-08-01 00:00:00

  • Activation of peroxisome proliferator-activated receptor gamma in brain inhibits inflammatory pain, dorsal horn expression of Fos, and local edema.

    abstract::Systemic administration of thiazolidinediones reduces peripheral inflammation in vivo, presumably by acting at peroxisome proliferator-activated receptor gamma (PPARgamma) in peripheral tissues. Based on a rapidly growing body of literature indicating the CNS as a functional target of PPARgamma actions, we postulated ...


    pub_type: 杂志文章


    authors: Morgenweck J,Abdel-Aleem OS,McNamara KC,Donahue RR,Badr MZ,Taylor BK

    更新日期:2010-02-01 00:00:00

  • Increased serotonin axons (immunoreactive to 5-HT transporter) in postmortem brains from young autism donors.

    abstract::Imaging studies of serotonin transporter binding or tryptophan retention in autistic patients suggest that the brain serotonin system is decreased. However, treatment with drugs which increase serotonin (5-HT) levels, specific serotonin reuptake inhibitors (SSRIs), commonly produce a worsening of the symptoms. In this...


    pub_type: 杂志文章


    authors: Azmitia EC,Singh JS,Whitaker-Azmitia PM

    更新日期:2011-06-01 00:00:00

  • Pre-training administration of anesthetic ketamine differentially affects rats' spatial and non-spatial recognition memory.

    abstract::There is poor experimental evidence concerning the effects of anesthetic doses of the non-competitive NMDA receptor antagonist ketamine on rodents' memory abilities. The present study was designed to investigate a) the long-term consequences of anesthetic ketamine on rats' non-spatial and spatial recognition memory; b...


    pub_type: 杂志文章


    authors: Pitsikas N,Boultadakis A

    更新日期:2009-07-01 00:00:00

  • Transitions near the open state in Shaker K(+)-channel: probing with temperature.

    abstract::Ionic currents from non-inactivating Shaker K(+)-channels were expressed in Xenopus oocytes and recorded with the cut-open oocyte voltage clamp technique. Kinetic properties of ionic currents were studied between 1.4 and 19 degrees C. The forward step of the last transition (...C --> O) of the activation pathway, just...


    pub_type: 杂志文章


    authors: Rodríguez BM,Bezanilla F

    更新日期:1996-01-01 00:00:00

  • Blockade of alcohol's amnestic activity in humans by an alpha5 subtype benzodiazepine receptor inverse agonist.

    abstract::Alcohol produces many subjective and objective effects in man including pleasure, sedation, anxiolysis, plus impaired eye movements and memory. In human volunteers we have used a newly available GABA-A/benzodiazepine receptor inverse agonist that is selective for the alpha5 subtype (a5IA) to evaluate the role of this ...


    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Nutt DJ,Besson M,Wilson SJ,Dawson GR,Lingford-Hughes AR

    更新日期:2007-12-01 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...


    pub_type: 杂志文章


    authors: Messenger MJ,Dawson LG,Duty S

    更新日期:2002-08-01 00:00:00

  • Dopamine reuptake transporter (DAT) "inverse agonism"--a novel hypothesis to explain the enigmatic pharmacology of cocaine.

    abstract::The long held view is cocaine's pharmacological effects are mediated by monoamine reuptake inhibition. However, drugs with rapid brain penetration like sibutramine, bupropion, mazindol and tesofensine, which are equal to or more potent than cocaine as dopamine reuptake inhibitors, produce no discernable subjective eff...


    pub_type: 杂志文章,评审


    authors: Heal DJ,Gosden J,Smith SL

    更新日期:2014-12-01 00:00:00

  • A somatic marker theory of addiction.

    abstract::Similar to patients with ventromedial prefrontal cortex (VMPC) lesions, substance abusers show altered decision-making, characterized by a tendency to choose the immediate reward, at the expense of negative future consequences. The somatic marker model proposes that decision-making depends on neural substrates that re...


    pub_type: 杂志文章,评审


    authors: Verdejo-García A,Bechara A

    更新日期:2009-01-01 00:00:00

  • Differential effects of the novel antidepressant agomelatine (S 20098) versus fluoxetine on 5-HT1A receptors in the rat brain.

    abstract::Agomelatine (S 20098) is a novel antidepressant drug with melatonin receptor agonist and 5-HT(2C) receptor antagonist properties, but actual mechanisms underlying its antidepressant action are unknown. Because functional desensitization of 5-HT(1A) autoreceptors in the dorsal raphe nucleus (DRN) occurs after chronic a...


    pub_type: 杂志文章


    authors: Hanoun N,Mocaër E,Boyer PA,Hamon M,Lanfumey L

    更新日期:2004-09-01 00:00:00

  • Receptor-mediated internalization of [3H]-neurotensin in synaptosomal preparations from rat neostriatum.

    abstract::Following its binding to somatodendritic receptors, the neuropeptide neurotensin (NT) internalizes via a clathrin-mediated process. In the present study, we investigated whether NT also internalizes presynaptically using synaptosomes from rat neostriatum, a region in which NT1 receptors are virtually all presynaptic. ...


    pub_type: 杂志文章


    authors: Nguyen HM,Cahill CM,McPherson PS,Beaudet A

    更新日期:2002-06-01 00:00:00

  • Dizocilpine-like discriminative stimulus effects of low-affinity uncompetitive NMDA antagonists.

    abstract::The dizocilpine-like discriminative stimulus effects of a variety of channel blocking (uncompetitive) N-methyl-D-aspartate (NMDA) receptor antagonists were examined in rats trained to discriminate dizocilpine (0.17 mg/kg, i.p) from saline in a two-lever operant procedure. The dissociative anesthetic-type NMDA antagoni...


    pub_type: 杂志文章


    authors: Grant KA,Colombo G,Grant J,Rogawski MA

    更新日期:1996-01-01 00:00:00

  • Receptor mediation of exaggerated responses to serotonin-enhancing drugs in serotonin transporter (SERT)-deficient mice.

    abstract::Administration of serotonin-enhancing drugs induces a distinctive behavioral syndrome in rodents. We previously reported that mice with a targeted disruption of the serotonin transporter (SERT) display some of these behaviors spontaneously, in the absence of drug. In the current studies, we assessed the drug-induced s...


    pub_type: 杂志文章


    authors: Fox MA,Jensen CL,Gallagher PS,Murphy DL

    更新日期:2007-10-01 00:00:00

  • Effects of phencyclidine in combination with morphine on the levels of met-enkephalin, dopamine, DOPAC and HVA in discrete brain areas of mice.

    abstract::The study investigated the interaction between phencyclidine (PCP) and morphine in affecting the levels of met-enkephalin, dopamine, DOPAC and HVA in mice. Morphine 5 mg/kg alone and PCP 10 mg/kg alone failed to change the levels of met-enkephalin in the midbrain and striatum. However, PCP in combination with morphine...


    pub_type: 杂志文章


    authors: Nabeshima T,Hiramatsu M,Furukawa H,Kameyama T

    更新日期:1985-08-01 00:00:00

  • Adenosine A(2A) Receptors as novel upstream regulators of BDNF-mediated attenuation of hippocampal Long-Term Depression (LTD).

    abstract::Hippocampal Long-Term Potentiation (LTP) is facilitated by BDNF, through the activation of tropomyosin-related kinase B (TrkB) receptors. However, an influence of BDNF upon Long-Term Depression (LTD) was also shown. The present work aimed to further evaluate the effect of BDNF and TrkB receptors upon CA1 hippocampal L...


    pub_type: 杂志文章


    authors: Rodrigues TM,Jerónimo-Santos A,Sebastião AM,Diógenes MJ

    更新日期:2014-04-01 00:00:00

  • Stimulation of P2 receptors in the ventral tegmental area enhances dopaminergic mechanisms in vivo.

    abstract::It has been shown that endogenous adenosine 5'-triphosphate (ATP) as well as its exogenously applied structural analogue, 2-methylthio ATP (2-MeSATP), facilitate the release of dopamine from axon terminals in the rat nucleus accumbens (NAc) by activating ATP-sensitive P2 receptors. In the present study, reversed micro...


    pub_type: 杂志文章


    authors: Krügel U,Kittner H,Franke H,Illes P

    更新日期:2001-06-01 00:00:00

  • Altered nocifensive behavior in animal models of autism spectrum disorder: The role of the nicotinic cholinergic system.

    abstract::Caretakers and clinicians alike have long recognized that individuals with autism spectrum disorder (ASD) can have altered sensory processing, which can contribute to its core symptoms. However, the pathobiology of sensory alterations in ASD is poorly understood. Here we examined nocifensive behavior in ASD mouse mode...


    pub_type: 杂志文章


    authors: Wang L,Almeida LE,Nettleton M,Khaibullina A,Albani S,Kamimura S,Nouraie M,Quezado ZM

    更新日期:2016-12-01 00:00:00

  • 24S-Hydroxycholesterol enhances synaptic vesicle cycling in the mouse neuromuscular junction: Implication of glutamate NMDA receptors and nitric oxide.

    abstract::24S-hydroxycholesterol (24S-HC) is a brain-derived product of lipid metabolism present in the systemic circulation, where its level can change significantly in response to physiological and pathophysiological conditions. Here, using electrophysiological and optical approaches, we have found a high sensitivity to 24S-H...


    pub_type: 杂志文章


    authors: Kasimov MR,Fatkhrakhmanova MR,Mukhutdinova KA,Petrov AM

    更新日期:2017-05-01 00:00:00

  • Endocannabinoid modulation of dopamine neurotransmission.

    abstract::Dopamine (DA) is a major catecholamine neurotransmitter in the mammalian brain that controls neural circuits involved in the cognitive, emotional, and motor aspects of goal-directed behavior. Accordingly, perturbations in DA neurotransmission play a central role in several neuropsychiatric disorders. Somewhat surprisi...


    pub_type: 杂志文章,评审


    authors: Covey DP,Mateo Y,Sulzer D,Cheer JF,Lovinger DM

    更新日期:2017-09-15 00:00:00

  • Diversity in the lateral hypothalamic input to the ventral tegmental area.

    abstract::The obesity epidemic is one of the biggest health challenges globally and rates have tripled since 1975. Overeating is the largest determinant of obesity, yet little is understood of the neural mechanisms underlying why individuals consume food regardless of satiety. The lateral hypothalamic (LH) input to the ventral ...


    pub_type: 杂志文章,评审


    authors: Godfrey N,Borgland SL

    更新日期:2019-08-01 00:00:00

  • Nitric oxide, superoxide and peroxynitrite: putative mediators of NMDA-induced cell death in cerebellar granule cells.

    abstract::In this study, we analysed the implication of superoxide (O2-.) and nitric oxide (NO.) free radicals and their resulting product peroxynitrite (ONOO-) in the neuronal death induced by the activation of the glutamatergic receptor of the N-methyl-D-aspartate (NMDA) subtype using cultured cerebellar granule cells. The NO...


    pub_type: 杂志文章


    authors: Lafon-Cazal M,Culcasi M,Gaven F,Pietri S,Bockaert J

    更新日期:1993-11-01 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...


    pub_type: 杂志文章


    authors: Zhang JJ,Han J,Sui N

    更新日期:2014-11-01 00:00:00

  • Dynamic changes in NADPH-diaphorase staining reflect activity of nitric oxide synthase: evidence for a dopaminergic regulation of striatal nitric oxide release.

    abstract::In fixed tissue, neuronal NADPH-diaphorase staining results from nitric oxide synthase (NOS) activity. Neuronal NOS only synthesizes nitric oxide once activated by the binding of Ca2+/calmodulin. We show here that neuronal NADPH-diaphorase staining is also dependent on Ca2+/calmodulin, implying that only activated NOS...


    pub_type: 杂志文章


    authors: Morris BJ,Simpson CS,Mundell S,Maceachern K,Johnston HM,Nolan AM

    更新日期:1997-11-01 00:00:00

  • Electroconvulsive seizures activate anorexigenic signals in the ventromedial nuclei of the hypothalamus.

    abstract::The ventromedial nucleus of the hypothalamus (VMH) plays an important role in feeding and energy homeostasis. Electroconvulsive seizure (ECS) therapy is highly effective in the treatment of several psychiatric diseases, including depression, but may also have beneficial effects in other neurological diseases. Although...


    pub_type: 杂志文章


    authors: Segi-Nishida E,Sukeno M,Imoto Y,Kira T,Sakaida M,Tsuchiya S,Sugimoto Y,Okuno Y

    更新日期:2013-08-01 00:00:00

  • Transient increase in alcohol self-administration following a period of chronic exposure to corticosterone.

    abstract::Stressful life events and chronic stressors have been associated with escalations in alcohol drinking. Stress exposure leads to the secretion of glucocorticoids (cortisol in the human; corticosterone (CORT) in the rodent). To model a period of heightened elevations in CORT, the present work assessed the effects of chr...


    pub_type: 杂志文章


    authors: Besheer J,Fisher KR,Lindsay TG,Cannady R

    更新日期:2013-09-01 00:00:00