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Submit Review(RS)-3,5-DHPG is a selective group I metabotropic glutamate receptor agonist which activates both mGlu1 and mGlu5. Also reported to be an antagonist at metabotropic glutamate receptors linked to phospholipase D.
S-enantiomer also available.
分子量 | 183.16 |
公式 | C8H9NO4 |
储存 | Desiccate at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 146255-66-5 |
PubChem ID | 108001 |
InChI Key | HOOWCUZPEFNHDT-UHFFFAOYSA-N |
Smiles | NC(C(O)=O)C1=CC(O)=CC(O)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 1.83 | 10 |
以下数据基于产品分子量 183.16。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 54.6 mL | 272.99 mL | 545.97 mL |
0.5 mM | 10.92 mL | 54.6 mL | 109.19 mL |
1 mM | 5.46 mL | 27.3 mL | 54.6 mL |
5 mM | 1.09 mL | 5.46 mL | 10.92 mL |
参考文献是支持产品生物活性的出版物。
Ito et al (1992) 3,5-Dihydroxyphenylglycine: a potent agonist of metabotropic glutamate receptors. NeuroReport 3 1013 PMID: 1362358
Mistry et al (1998) Regulation of phosphoinositide turnover in neonatal rat cerebral cortex by group I- and II-selective metabotropic glutamate receptor agonists. Br.J.Pharmacol. 123 581 PMID: 9504400
Pellegrini-Giampietro et al (1996) Pharmacological characterization of metabotropic glutamate recpetors coupled to phopholipase D in the rat hippocampus. Br.J.Pharmacol. 118 1035 PMID: 8799579
Palmer et al (1997) The group I mGlu receptor agonist DHPG induces a novel form of LTD in the CA1 region of the hippocampus. Neuropharmacology 36 1517 PMID: 9517422
If you know of a relevant reference for (RS)-3,5-DHPG, please let us know.
关键词: (RS)-3,5-DHPG, (RS)-3,5-DHPG supplier, Selective, group, I, mGlur, agonists, Group, Receptors, mGlu1, mGlu5, mGluR1, mGluR5, Glutamate, Metabotropic, 19641-83-9, (Metabotropic), 0342, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (RS)-3,5-DHPG 的部分引用包括:
Guo et al (2016) Selective Disruption of Metabotropic Glutamate Receptor 5-Homer Interactions Mimics Phenotypes of Fragile X Syndrome in Mice. J Neurosci 36 2131 PMID: 26888925
Sethna et al (2016) Calmodulin activity regulates group I metabotropic glutamate receptor-mediated signal transduction and synaptic depression. J Neurosci Res 94 401 PMID: 26864654
Rojas et al (2013) Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors. Mol Pharmacol 83 106 PMID: 23066089
Ramiro-Cortés (2013) Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression. PLoS One 8 e71155 PMID: 23951097
Jiang et al (2006) Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism. J Neurosci 26 4318 PMID: 16624952
Hsieh et al (2006) AMPAR removal underlies Abeta-induced synaptic depression and dendritic spine loss. Neuron 52 831 PMID: 17145504
Calò et al (2005) Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons. J Neurosci 25 2245 PMID: 15745950
Lin et al (2016) Neuronal splicing regulator RBFOX3(NeuN) regulates adult hippocampal neurogenesis and synaptogenesis PLoS One 11 e0164164 PMID: 27701470
Romei et al (2016) Colocalization of neurotransmitter transporters on the plasma membrane of the same nerve terminal may reflect cotransmission. Brain Research Bulletin 127 100 PMID: 27565422
Ziskin et al (2007) Vesicular release of glutamate from unmyelinated axons in white matter. Proc Natl Acad Sci U S A 10 321 PMID: 17293857
Rancillac et al (2006) Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum. J Neurosci 26 6997 PMID: 16807329
Keuren-Jensen and Cline (2006) Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction. J Neurosci 26 7575 PMID: 16855085
Etkin et al (2006) A role in learning for SRF: deletion in the adult forebrain disrupts LTD and the formation of an immediate memory of a novel context. Neuron 50 127 PMID: 16600861
Bateup et al (2011) Loss of Tsc1 in vivo impairs hippocampal mGluR-LTD and increases excitatory synaptic function. Neurosci Lett 31 8862 PMID: 21677170
Kim et al (2010) Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid(β)42 from isolated intact nerve terminals. J Neurosci 30 3870 PMID: 20237257
Schapitz et al (2010) Neuroligin 1 is dynamically exchanged at postsynaptic sites. J Neurosci 30 12733 PMID: 20861378
Kolber et al (2010) Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior. Sci Rep 30 8203 PMID: 20554871
Muddashetty et al (2007) Dysregulated metabotropic glutamate receptor-dependent translation of AMPA receptor and postsynaptic density-95 mRNAs at synapses in a mouse model of fragile X syndrome. J Neurosci 27 5338 PMID: 17507556
Jan and Westbrook (2007) Disynaptic amplification of metabotropic glutamate receptor 1 responses in the olfactory bulb. J Neurosci 27 132 PMID: 17202480
Sakuragi et al (2013) Involvement of TrkB- and p75(NTR)-signaling pathways in two contrasting forms of long-lasting synaptic plasticity. J Vis Exp 3 3185 PMID: 24212565
Crock et al (2012) Central amygdala metabotropic glutamate receptor 5 in the modulation of visceral pain. Eur J Neurosci 32 14217 PMID: 23055491
Zhong et al (2012) MeCP2 phosphorylation is required for modulating synaptic scaling through mGluR5. Stem Cell Reports 32 12841 PMID: 22973007
Coulon et al (2011) Activity Modes in Thalamocortical Relay Neurons are Modulated by G(q)/G(11) Family G-proteins - Serotonergic and Glutamatergic Signaling. Front Cell Neurosci 4 132 PMID: 21267426
Hays et al (2011) Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry. J Neurosci 31 14223 PMID: 21976507
Chiu and Castillo (2008) Input-specific plasticity at excitatory synapses mediated by endocannabinoids in the dentate gyrus. Neuropharmacology 54 68 PMID: 17706254
Grueter et al (2008) In vivo metabotropic glutamate receptor 5 (mGluR5) antagonism prevents cocaine-induced disruption of postsynaptically maintained mGluR5-dependent long-term depression. J Neurosci 28 9261 PMID: 18784306
Dai et al (2008) A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients. Neurosignals 16 112 PMID: 18253052
McElligott (2008) Alpha1-adrenergic receptor-induced heterosynaptic long-term depression in the bed nucleus of the stria terminalis is disrupted in mouse models of affective disorders. Neuropsychopharmacology 33 2313 PMID: 18046308
Li et al (2007) The different roles of cyclinD1-CDK4 in STP and mGluR-LTD during the postnatal development in mice hippocampus area CA1. BMC Dev Biol 7 57 PMID: 17535444
Brager and Johnston (2007) Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons. J Neurosci 27 13926 PMID: 18094230
Takano et al (2014) Rapid manifestation of reactive astrogliosis in acute hippocampal brain slices. Glia 62 78 PMID: 24272704
Lee et al (2014) Long-term depression-inducing stimuli promote cleavage of the synaptic adhesion molecule NGL-3 through NMDA receptors, matrix metalloproteinases and presenilin/γ-secretase. Philos Trans R Soc Lond B Biol Sci 369 20130158 PMID: 24298159
Zhang et al (2008) The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation. J Neurosci 28 10561 PMID: 18923032
Marchaland et al (2008) Fast subplasma membrane Ca2+ transients control exo-endocytosis of synaptic-like microvesicles in astrocytes. J Neurosci 28 9122 PMID: 18784293
Wall et al (2018) The Temporal Dynamics of Arc Expression Regulate Cognitive Flexibility. Neuron 98 1124 PMID: 29861284
Lim et al (2018) Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures. Int J Mol Sci 19 PMID: 30274399
Yasuda et al (2018) Drebrin Isoforms Critically Regulate NMDAR- and mGluR-Dependent LTD Induction. Front Cell Neurosci 12 330 PMID: 30349460
Vergassola et al (2018) Presynaptic mGlu1 Receptors Control GABAB Receptors in an Antagonist-Like Manner in Mouse Cortical GABAergic and Glutamatergic Nerve Endings. Front Mol Neurosci 11 324 PMID: 30279647
Iliff et al (2013) Impaired activity-dependent FMRP translation and enhanced mGluR-dependent LTD in Fragile X premutation mice. Hum Mol Genet 22 1180 PMID: 23250915
Chen and Shen (2013) Modulation of mGluR-dependent MAP1B translation and AMPA receptor endocytosis by microRNA miR-146a-5p. J Neurosci 33 9013 PMID: 23699512
Xu et al (2013) Simultaneous monitoring of presynaptic transmitter release and postsynaptic receptor trafficking reveals an enhancement of presynaptic activity in metabotropic glutamate receptor-mediated long-term depression. J Neurosci 33 5867 PMID: 23536098
Thompson and Perkel (2011) Endocannabinoids mediate synaptic plasticity at glutamatergic synapses on spiny neurons within a basal ganglia nucleus necessary for song learning. J Neurophysiol 105 1159 PMID: 21177997
Wang et al (2009) Converging signal on ERK1/2 activity regulates group I mGluR-mediated Arc transcription. J Neurosci 460 36 PMID: 19446601
Citri et al (2009) N-MthD.-aspartate receptor- and metabotropic glutamate receptor-dependent long-term depression are differentially regulated by the ubiquitin-proteasome system. J Neurosci 30 1443 PMID: 19821836
Kim et al (2008) Aberrant early-phase ERK inactivation impedes neuronal function in fragile X syndrome. J Neurosci 105 4429 PMID: 18332424
Schmidt et al (2015) Group I metabotropic glutamate receptor-mediated activation of PKC gamma in the nucleus accumbens core promotes the reinstatement of cocaine seeking. Addict Biol 20 285 PMID: 24506432
Nishi et al (2003) Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. J Neurosci 100 1322 PMID: 12538871
Collard et al (2002) Neutrophil-derived glutamate regulates vascular endothelial barrier function. J Biol Chem 277 14801 PMID: 11847215
Huber et al (2002) Altered synaptic plasticity in a mouse model of fragile X mental retardation. Proc Natl Acad Sci U S A 99 7746 PMID: 12032354
Job and Eberwine (2001) Identification of sites for exponential translation in living dendrites. Proc Natl Acad Sci U S A 98 13037 PMID: 11606784
Nonobe et al (2016) Application of surface plasmon resonance imaging to monitoring G protein-coupled receptor signaling and its modulation in a heterologous expression system. BMC Biotechnol 16 36 PMID: 27068216
Zhong et al (2015) BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain DA neurons. Sci Rep 35 4469 PMID: 25762688
Hasegawa et al (2015) Dendritic spine dynamics leading to spine elimination after repeated inductions of LTD. J Neurosci 5 7707 PMID: 25573377
Choi et al (2015) PDE-4 inhibition rescues aberrant synaptic plasticity in Drosophila and mouse models of fragile X syndrome. Proc Natl Acad Sci U S A 35 396 PMID: 25568131
Pasquale and Sherman (2013) A modulatory effect of the feedback from higher visual areas to V1 in the mouse. J Neurophysiol 109 2618 PMID: 23446698
Oh et al (2013) Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening. Proc Natl Acad Sci U S A 110 E305 PMID: 23269840
Sherkhane and Kapfhammer (2013) The plasma membrane Ca2+-ATPase2 (PMCA2) is involved in the regulation of Purkinje cell dendritic growth in cerebellar organotypic slice cultures. J Neurosci 2013 321685 PMID: 24288624
Kapfhammer and Gugger (2012) The analysis of purkinje cell dendritic morphology in organotypic slice cultures. J Neurosci NULL PMID: 22473312
Hoffman et al (2010) Control of cannabinoid CB1 receptor function on glutamate axon terminals by endogenous adenosine acting at A1 receptors. J Neurosci 30 545 PMID: 20071517
Citri et al (2010) Calcium binding to PICK1 is essential for the intracellular retention of AMPA receptors underlying long-term depression. J Neurosci 30 16437 PMID: 21147983
Glitsch (2010) Activation of native TRPC3 cation channels by phospholipase D. FASEB J 24 318 PMID: 19741172
Patel et al (2009) Mobilization of calcium from intracellular stores facilitates somatodendritic DA release. J Neurosci 29 6568 PMID: 19458227
Bagayogo and Dreyfus (2009) Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway. ASN Neuro 1 PMID: 19570026
Gallagher et al (2004) Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1. Neural Plast 24 4859 PMID: 15152046
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
Levenga et al (2017) AKT isoforms have distinct hippocampal expression and roles in synaptic plasticity. Elife 6 PMID: 29173281
Xi (2017) Metabotropic glutamate receptor 5 mediates the suppressive effect of 6-OHDA-induced model of Parkinson's disease on liver cancer. Pharmacol Res 121 145 PMID: 28455267
Wang et al (2017) Striatopallidal dysfunction underlies repetitive behavior in Shank3-deficient model of autism. J Clin Invest 127 1978 PMID: 28414301
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(RS)-3,5-DHPG was used to test a (potential) impact of metabotropic glutamate receptors on the effect of 5HT-1B receptors on neurotransmitter vesicle release in interneuronal synapse. Picture: membrane capacitance fluctuation of living neuron after series of electrical stimuli delivered to acute neural tissue. Left: control. Right: activation of metabotropic glutamate receptors (with 1 μM CHPG, 1 μM (RS)-3,5-DHPG and 1 μM AMN 082), GABA-B receptors and ACh receptors does not show a significant effect. Grey traces: individual recordings; red: averaged trace.
I used (RS)-3,5-DHPG (Cat. No. 0342) in slice ephys recordings. Worked as expected.
Dissolved in MilliQ H2O, and used at a concentration of 0.1 mM.
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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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