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Submit ReviewL-AP4
说明： Selective group III mGlu agonist
化学名： L-(+)-2-Amino-4-phosphonobutyric acid
纯度： ≥99% (HPLC)
生物活性 for L-AP4
L-AP4 is a selective group III metabotropic glutamate receptor agonist that acts at mGlu4, mGlu8, mGlu6 and mGlu7 receptors (EC50 values = 0.1-0.13 μM, 0.29 μM, 1.0-2.4 μM and 249-337 μM, respectively). L-AP4 is a synaptic depressant and inhibits excitatory post-synaptic currents. L-AP4 is also an agonist at the quisqualate-sensitized AP6 site in hippocampus.
DL Mixture and D-isomer also available.
技术数据 for L-AP4
| 分子量 | 183.1 |
| 公式 | C4H10NO5P |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 23052-81-5 |
| PubChem ID | 179394 |
| InChI Key | DDOQBQRIEWHWBT-VKHMYHEASA-N |
| Smiles | [H][C@@](CCP(O)(O)=O)(N)C(O)=O |
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.
溶解性数据 for L-AP4
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 0.92 | 5 | |
| 1eq. NaOH | 18.31 | 100 |
制备储备液 for L-AP4
以下数据基于产品分子量 183.1。 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 |
|---|---|---|---|
| 1 mM | 5.46 mL | 27.31 mL | 54.61 mL |
| 5 mM | 1.09 mL | 5.46 mL | 10.92 mL |
| 10 mM | 0.55 mL | 2.73 mL | 5.46 mL |
| 50 mM | 0.11 mL | 0.55 mL | 1.09 mL |
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产品说明书 for L-AP4
参考文献 for L-AP4
参考文献是支持产品生物活性的出版物。
Bushell et al (1995) Antagonism of the synaptic depressant actions of L-AP4 in the lateral perforant path by MAP4. Neuropharmacology 34 239 PMID: 7617150
Evans et al (1982) The effect of a series of ω-phosphonic-α-carboxylic amino acids on electrically evoked and amino acid induced responses in isolated spinal cord preparations. Br.J.Pharmacol. 75 65 PMID: 7042024
Nakanishi (1992) Molecular diversity of glutamate receptors and implications for brain functions. Science 258 597 PMID: 1329206
Tones et al (1995) The agonist selectivity of a class III metabotropic glutamate receptor, human mGluR4a, is determined by the N-terminal extracellular domain. NeuroReport 7 117 PMID: 8742431
Selvam et al (2018) Increased potency and selectivity for group III metabotropic glutamate receptor agonists binding at dual sites. J.Med.Chem. 61 1969 PMID: 29397723
If you know of a relevant reference for L-AP4, please let us know.
关键词: L-AP4, L-AP4 supplier, Selective, group, III, mGlur, agonists, Group, Receptors, mGlu4, mGlu6, mGlu7, mGlu8, mGluR4, mGluR6, mGluR7, mGluR8, Glutamate, Metabotropic, (Metabotropic), 0103, Tocris Bioscience
56 篇 L-AP4 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-AP4 的部分引用包括：
Hellmer et al (2018) A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina. Physiol Rep 6 e13885 PMID: 30338673
Macé et al (2015) Targeting channelrhodopsin-2 to ON-bipolar cells with vitreally administered AAV Restores ON and OFF visual responses in blind mice. Mol Ther 23 7 PMID: 25095892
Taman and Ribeiro (2011) Characterization of a truncated metabotropic glutamate receptor in a primitive metazoan, the parasitic flatworm Schistosoma mansoni. PLoS One 6 e27119 PMID: 22069494
Chaffiol et al (2017) A New Promoter Allows Optogenetic Vision Restoration with Enhanced Sensitivity in Macaque Retina. Mol Ther 25 2546 PMID: 28807567
Mills et al (2014) Three distinct blue-green color pathways in a mammalian retina. J Neurosci 34 1760 PMID: 24478358
De-May and Ali (2013) Cell type-specific regulation of inhibition via cannabinoid type 1 receptors in rat neocortex. J Neurophysiol 109 216 PMID: 23054605
Klatte et al (2013) Impaired D-serine-mediated cotransmission mediates cognitive dysfunction in epilepsy. J Neurosci 33 13066 PMID: 23926260
Romo-Parra et al (2008) GABA actions in hippocampal area CA3 during postnatal development: differential shift from depolarizing to hyperpolarizing in somatic and dendritic compartments. J Neurophysiol 99 1523 PMID: 18216229
Suh et al (2008) Corequirement of PICK1 binding and PKC phosphorylation for stable surface expression of the metabotropic glutamate receptor mGluR7. Neuron 58 736 PMID: 18549785
Sabater et al (2021) Voltage-gated potassium channels ensure action potential shape fidelity in distal axons. J Neurosci 41 5372 PMID: 34001627
Maldonado et al (2021) Oxytocin shapes spontaneous activity patterns in the developing visual cortex by activating somatostatin interneurons. Curr Biol 31 322 PMID: 33157028
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236
Murphy-Baum and Taylor (2015) The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina. J Neurosci 35 13336 PMID: 26424882
Kammermeier (2015) Constitutive activity of metabotropic glutamate receptor 7. BMC Neurosci 16 17 PMID: 25881041
Schmidt and Kofuji (2011) Structure and function of bistratified intrinsically photosensitive retinal ganglion cells in the mouse. J Comp Neurol 519 1492 PMID: 21452206
Krock et al (2009) Retrograde intraflagellar transport by cytoplasmic dynein-2 is required for outer segment extension in vertebrate photoreceptors but not arrestin translocation. Invest Ophthalmol Vis Sci 50 5463 PMID: 19474410
Pickard et al (2009) Light-induced fos expression in intrinsically photosensitive retinal ganglion cells in melanopsin knockout (opn4) mice. PLoS One 4 e4984 PMID: 19319185
Montesano et al (2015) Effects of the Concomitant Activation of ON and OFF Retinal Ganglion Cells on the Visual Thalamus: Evidence for an Enhanced Recruitment of GABAergic Cells. Front Neural Circuits 9 77 PMID: 26635537
Reifler et al (2015) The rat retina has five types of ganglion-cell photoreceptors. Exp Eye Res 130 17 PMID: 25450063
Jacoby et al (2015) An Amacrine Cell Circuit for Signaling Steady Illumination in the Retina. Cell Rep 13 2663 PMID: 26711334
Xiong et al (2015) Voriconazole, an antifungal triazol that causes visual side effects, is an inhibitor of TRPM1 and TRPM3 channels. Invest Ophthalmol Vis Sci 56 1367 PMID: 25650413
Spampinato et al (2015) Glial metabotropic glutamate receptor-4 increases maturation and survival of oligodendrocytes. Front Cell Neurosci 8 462 PMID: 25642169
Tse et al (2014) Possible roles of glutamate transporter EAAT5 in mouse cone depolarizing bipolar cell light responses. Vision Res 103 63 PMID: 24972005
Tse et al (2014) Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses. Vision Res 103 49 PMID: 25152321
Bennett et al (2014) Examination of VLC-PUFA-deficient photoreceptor terminals. Invest Ophthalmol Vis Sci 55 4063 PMID: 24764063
Kiyama et al (2019) Essential Roles of Tbr1 in the Formation and Maintenance of the Orientation-Selective J-RGCs and a Group of OFF-Sustained RGCs in Mouse. Cell Rep 27 900 PMID: 30995485
Caiati et al (2013) PrPC controls via protein kinase A the direction of synaptic plasticity in the immature hippocampus. J Neurosci 33 2973 PMID: 23407955
Ichinose and Lukasiewicz (2012) The mode of retinal presynaptic inhibition switches with light intensity. J Neurosci 32 4360 PMID: 22457487
Bonezzi et al (2018) The Development of Mid-Wavelength Photoresponsivity in the Mouse Retina. Curr Eye Res 43 666 PMID: 29447486
Manookin et al (2018) Neural Mechanisms Mediating Motion Sensitivity in Parasol Ganglion Cells of the Primate Retina. Neuron 97 1327 PMID: 29503188
Lee et al (2022) Inhibition, but not excitation, recovers from partial cone loss with greater spatiotemporal integration, synapse density, and frequency. Cell Rep. 38 110317 PMID: 35108533
Broadstock et al (2012) Antiparkinsonian potential of targeting group III metabotropic glutamate receptor subtypes in the rodent substantia nigra pars reticulata. Br J Pharmacol 165 1034 PMID: 21627638
Sher and DeVries (2012) A non-canonical pathway for mammalian blue-green color vision. Nat Neurosci 15 952 PMID: 22634728
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777
Maier et al (2010) Sustained glutamate receptor activation down-regulates GABAB receptors by shifting the balance from recycling to lysosomal degradation. J Biol Chem 285 35606 PMID: 20826795
Maurer et al (2010) Distinct retinal deficits in a zebrafish pyruvate dehydrogenase-deficient mutant. J Neurosci 30 11962 PMID: 20826660
Prigge et al (2016) M1 ipRGCs Influence Visual Function through Retrograde Signaling in the Retina The Journal of Neuroscience 6 7184 PMID: 27383593
Zhang et al (2012) Melanopsin mediates retrograde visual signaling in the retina. PLoS One 7 e42647 PMID: 22880066
Govea et al (2012) Group III metabotropic glutamate receptors and transient receptor potential vanilloid 1 co-localize and interact on nociceptors. Neuroscience 217 130 PMID: 22609935
Peachey et al (2012) Depolarizing bipolar cell dysfunction due to a Trpm1 point mutation. J Neurophysiol 108 2442 PMID: 22896717
Hook et al (2012) DArgic modulation of ganglion-cell photoreceptors in rat. Eur J Neurosci 35 507 PMID: 22304466
Pearring et al (2011) A role for nyctalopin, a small leucine-rich repeat protein, in localizing the TRP melastatin 1 channel to retinal depolarizing bipolar cell dendrites. J Neurosci 31 10060 PMID: 21734298
Zhang et al (2010) RGS7 and -11 complexes accelerate the ON-bipolar cell light response. Invest Ophthalmol Vis Sci 51 1121 PMID: 19797214
El-Kouhen et al (2006) Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. Br J Pharmacol 149 761 PMID: 17016515
Galici et al (2006) Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J Pharmacol Exp Ther 318 173 PMID: 16608916
Maruyama et al (2006) Umami responses in mouse taste cells indicate more than one receptor. J Neurosci 26 2227 PMID: 16495449
Alberdi et al (2006) Activation of kainate receptors sensitizes oligodendrocytes to complement attack. J Neurosci 26 3220 PMID: 16554473
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
Newman (2005) Calcium increases in retinal glial cells evoked by light-induced neuronal activity. J Neurosci 25 5502 PMID: 15944378
Bender et al (2007) Localization of HCN1 channels to presynaptic compartments: novel plasticity that may contribute to hippocampal maturation. J Neurosci 27 4697 PMID: 17460082
Matsui et al (2006) Effects of ethanol on photoreceptors and visual function in developing zebrafish. Invest Ophthalmol Vis Sci 47 4589 PMID: 17003456
Fujino and Oertel (2003) Bidirectional synaptic plasticity in the cerebellum-like mammalian dorsal cochlear nucleus. Proc Natl Acad Sci U S A 100 265 PMID: 12486245
Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br J Pharmacol 138 1026 PMID: 12684257
Nishi et al (2003) Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. Proc Natl Acad Sci U S A 100 1322 PMID: 12538871
Collard et al (2002) Neutrophil-derived glutamate regulates vascular endothelial barrier function. J Biol Chem 277 14801 PMID: 11847215
Sekaran et al (2005) Melanopsin-dependent photoreception provides earliest light detection in the mammalian retina. Curr Biol 15 1099 PMID: 15964274
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Used in inhibitor cocktail.
By
Anonymous on 12/03/2019
分析类型： In Vitro
种属： Rat
细胞系/组织： Retinal rod bipolar cells
Retinal dissections were performed in HEPES-buffered extracellular solution containing inhibitor cocktail4 umol/L
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