MW 801 Da, Purity >99%. Non-competitive NMDA receptor antagonist acting at the polyamine site. Displays GluN2B (formerly NR2B) subunit selectivity. IC50 values are 0.15 μM at NR1/NR2B and >30 μM for NR1/NR2A, NR1/NR2C and NR1/NR2D receptors.
Also available in simple stock solutions (ab146675) - add 1 ml of water to get an exact, ready-to-use concentration.
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- American journal of hypertension 34:840-8502021Chronic Blockade of NMDAR Subunit 2A in the Hypothalamic Paraventricular Nucleus Alleviates Hypertension Through Suppression of MEK/ERK/CREB Pathway.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYing Li,Yu-Xin Lu,Hong-Li Chi,Tong Xiao,Yan-Mei Chen,Li-Yan Fu,Abdoulaye Issotina Zibrila,Jie Qi,Hong-Bao Li,Qing Su,Hong-Li Gao,Yan Zhang,Xiao-Lian Shi,Xiao-Jing Yu,Yu-Ming KangPubMed 33856436
- Journal of neuroinflammation 15:362018Hyperammonemia alters membrane expression of GluA1 and GluA2 subunits of AMPA receptors in hippocampus by enhancing activation of the IL-1 receptor: underlying mechanisms.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLucas Taoro-Gonzalez et. al.PubMed 29422059
- Learning & memory (Cold Spring Harbor, N.Y.) 23:486-932016Involvement of protein phosphatases in the destabilization of methamphetamine-associated contextual memory.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYang-Jung Yu et. al.PubMed 27531839
- Journal of neurophysiology 113:3634-452015Different pools of glutamate receptors mediate sensitivity to ambient glutamate in the cochlear nucleus.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYang Yang et. al.PubMed 25855696
- The Journal of neuroscience : the official journal of the Society for Neuroscience 33:9150-602013Triheteromeric NMDA receptors at hippocampal synapses.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKenneth R Tovar,Matthew J McGinley,Gary L WestbrookPubMed 23699525
- Proceedings of the National Academy of Sciences of 110:9124-92013Reinstatement of nicotine seeking is mediated by glutamatergic plasticity.Applications:Unspecified applicationReactive species:Unspecified reactive speciesCassandra D Gipson et. al.PubMed 23671067
- The Journal of neuroscience : the official journal of the Society for Neuroscience 33:1109-152013Double dissociation of the requirement for GluN2B- and GluN2A-containing NMDA receptors in the destabilization and restabilization of a reconsolidating memory.Applications:Unspecified applicationReactive species:Unspecified reactive speciesAmy L Milton,Emiliano Merlo,Patrizia Ratano,Ben L Gregory,Jessica K Dumbreck,Barry J EverittPubMed 23325248
- PloS one 7:e460122012Chronic zinc exposure decreases the surface expression of NR2A-containing NMDA receptors in cultured hippocampal neurons.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJia Zhu,Chong-Yu Shao,Wei Yang,Xiao-Min Zhang,Zhen-Yong Wu,Liang Zhou,Xin-Xin Wang,Yun-Hong Li,Jun Xia,Jian-Hong Luo,Ying ShenPubMed 23049922
- The Journal of neuroscience : the official journal of the Society for Neuroscience 32:8065-732012Amino-terminal ligands prolong NMDA Receptor-mediated EPSCs.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKenneth R Tovar,Gary L WestbrookPubMed 22674281
- Proceedings of the National Academy of Sciences of the United States of America 108:19407-122011Heroin relapse requires long-term potentiation-like plasticity mediated by NMDA2b-containing receptors.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHaowei Shen,Khaled Moussawi,Wenhua Zhou,Shigenobu Toda,Peter W KalivasPubMed 22084102
Key facts
- CAS number
- 23210-58-4
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 801 Da
- Molecular formula
- C46H60N2O10
- PubChem identifier
- 656586
- Nature
- Synthetic
Alternative names
AMPA 1, AMPA-selective glutamate receptor 1, GLUH1, GRIA1_HUMAN, GluA1, GluR-1, GluR-A, GluR-K1, Glutamate receptor 1, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, HBGR1, MGC133252, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243
Recommended products
MW 801 Da, Purity >99%. Non-competitive NMDA receptor antagonist acting at the polyamine site. Displays GluN2B (formerly NR2B) subunit selectivity. IC50 values are 0.15 μM at NR1/NR2B and >30 μM for NR1/NR2A, NR1/NR2C and NR1/NR2D receptors.
Also available in simple stock solutions (ab146675) - add 1 ml of water to get an exact, ready-to-use concentration.
Key facts
- CAS number
- 23210-58-4
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 801 Da
- Molecular formula
- C46H60N2O10
- PubChem identifier
- 656586
- Nature
- Synthetic
- Solubility
Soluble in water to 15 mM.
Soluble in DMSO to 100 mM.
- Biochemical name
- Ifenprodil (tartrate)
- Biological description
Non-competitive NMDA receptor antagonist acting at the polyamine site. Displays GluN2B (formerly NR2B) subunit selectivity. IC50 values are 0.15 μM at NR1/NR2B and >30 μM for NR1/NR2A, NR1/NR2C and NR1/NR2D receptors.
Also available in simple stock solutions (ab146675) - add 1 ml of water to get an exact, ready-to-use concentration.- Canonical SMILES
- CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.C(C(C(=O)O)O)(C(=O)O)O
- Isomeric SMILES
- CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
- InChI
- InChI=1S/2C21H27NO2.C4H6O6/c2*1-16(21(24)19-7-9-20(23)10-8-19)22-13-11-18(12-14-22)15-17-5-3-2-4-6-17;5-1(3(7)8)2(6)4(9)10/h2*2-10,16,18,21,23-24H,11-15H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t;;1-,2-/m..1/s1
- InChIKey
- DMPRDSPPYMZQBT-CEAXSRTFSA-N
- IUPAC name
- 4-[2-(4-benzylpiperidin-1-yl)-1-hydroxypropyl]phenol;(2R,3R)-2,3-dihydroxybutanedioic acid
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Glutamate Receptor 1 (AMPA subtype) also known as GluR1 is a subunit of the AMPA receptor complex which mediates fast synaptic transmission in the central nervous system. It is an ionotropic receptor for glutamate functioning by opening ion channels to allow the flow of Na+ and Ca2+ ions across the cell membrane contributing to excitatory neurotransmission. The GluR1 subunit has a molecular mass of approximately 100 kDa. This receptor is commonly expressed in the brain regions such as the hippocampus and the cerebral cortex playing an important role in synaptic plasticity and memory formation.
- Biological function summary
The GluR1 subunit is an essential component of the AMPA receptor complex which typically forms as a tetramer. This complex modulates synaptic strength and plasticity processes critical for learning and memory. The activity of AMPA receptors including those containing GluR1 is regulated by several auxiliary proteins and is essential for post-synaptic responses. The GluR1 subunit also interacts with other proteins such as TARPs which modulate its trafficking and channel properties.
- Pathways
The GluR1-containing AMPA receptors participate significantly in the glutamatergic signaling pathway which is vital for fast excitatory synaptic transmission in the brain. This pathway also involves the NMDA receptors which work together with AMPA receptors to regulate synaptic plasticity and neuronal communication. Additionally the GluR1 interacts within the long-term potentiation (LTP) pathway contributing to the strengthening of synapses an essential mechanism underlying learning and memory.
- Associated diseases and disorders
Dysfunction in GluR1 and associated AMPA receptors has been implicated in conditions like Alzheimer's disease and epilepsy. Alzheimer's disease exhibits decreased synaptic transmission and plasticity linked to impaired GluR1 function and its interactions with NMDA receptors. In epilepsy abnormal GluR1 activity may contribute to heightened neuronal excitability and seizure propagation. Targeting GluR1 or associated pathways offers potential for therapeutic interventions in these disorders possibly through drugs such as memantine and NBQX which modulate receptor activity.
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2 product images
Chemical Structure - Ifenprodil hemitartrate, GluN2B (formerly NR2B)-preferring NMDA antagonist (ab120111)
2D chemical structure image of ab120111, Ifenprodil hemitartrate, GluN2B (formerly NR2B)-preferring NMDA antagonist
Image from Case DT et al., PLoS One. 2011;6(6):e20756. Fig 4(D).; doi: 10.1371/journal.pone.0020756. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/Functional Studies - Ifenprodil hemitartrate, GluN2B (formerly NR2B)-preferring NMDA antagonist (ab120111)
Median ifenprodil sensitivity from a rat postnatal day 2 (P2) and day 12 (P12) neuron; NMDAR-mediated responses in control (black) and in presence of the GluN2B-preferring antagonist ifenprodil (ab120111, grey).
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