MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit
Publication Date
February 01, 2016
Journal
PLOS ONE
Authors
Robert A. Volkmann, Christopher M. Fanger, David R. Anderson, Venkata Ramana Sirivolu, et al
Volume
11
Issue
2
Pages
e0148129
DOI
https://dx.plos.org/10.1371/journal.pone.0148129
Publisher URL
http://journals.plos.org/plosone/article?id=10.1371%2Fjournal.pone.0148129
PubMed
http://www.ncbi.nlm.nih.gov/pubmed/26829109
PubMed Central
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4734667
Europe PMC
http://europepmc.org/abstract/MED/26829109
Web of Science
000369548200068
Scopus
84958817607
Mendeley
http://www.mendeley.com/research/mpx004-mpx007-new-pharmacological-tools-study-physiology-nmda-receptors-containing-glun2a-subunit
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Mendeley | Further Information

{"title"=>"MPX-004 and MPX-007: New pharmacological tools to study the physiology of nmda receptors containing the GluN2A Subunit", "type"=>"journal", "authors"=>[{"first_name"=>"Robert A.", "last_name"=>"Volkmann", "scopus_author_id"=>"7006553380"}, {"first_name"=>"Christopher M.", "last_name"=>"Fanger", "scopus_author_id"=>"57130787300"}, {"first_name"=>"David R.", "last_name"=>"Anderson", "scopus_author_id"=>"57129450900"}, {"first_name"=>"Venkata Ramana", "last_name"=>"Sirivolu", "scopus_author_id"=>"57194483866"}, {"first_name"=>"Kathy", "last_name"=>"Paschetto", "scopus_author_id"=>"6506969525"}, {"first_name"=>"Earl", "last_name"=>"Gordon", "scopus_author_id"=>"57129912900"}, {"first_name"=>"Caterina", "last_name"=>"Virginio", "scopus_author_id"=>"6701381312"}, {"first_name"=>"Melanie", "last_name"=>"Gleyzes", "scopus_author_id"=>"55653064300"}, {"first_name"=>"Bruno", "last_name"=>"Buisson", "scopus_author_id"=>"7003496735"}, {"first_name"=>"Esther", "last_name"=>"Steidl", "scopus_author_id"=>"14062637500"}, {"first_name"=>"Susanna B.", "last_name"=>"Mierau", "scopus_author_id"=>"6505469552"}, {"first_name"=>"Michela", "last_name"=>"Fagiolini", "scopus_author_id"=>"56719404700"}, {"first_name"=>"Frank S.", "last_name"=>"Menniti", "scopus_author_id"=>"7003918109"}], "year"=>2016, "source"=>"PLoS ONE", "identifiers"=>{"issn"=>"19326203", "scopus"=>"2-s2.0-84958817607", "pui"=>"608335388", "doi"=>"10.1371/journal.pone.0148129", "sgr"=>"84958817607", "pmid"=>"26829109"}, "id"=>"ea3e73a6-6f0c-3de5-bd67-7ab432713208", "abstract"=>"GluN2A is themost abundant of theGluN2NMDA receptor subunits in the mammalianCNS. Physiological and genetic evidence implicate GluN2A-containing receptors in susceptibility to autism, schizophrenia, childhood epilepsy and neurodevelopmental disorders such as Rett Syndrome.However,GluN2A-selective pharmacological probes to explore the therapeutic potential of targeting these receptors have been lacking. Here we disclose a novel series of pyrazine-containingGluN2A antagonists exemplified byMPX-004 (5-(((3-chloro-4-fluorophe- nyl)sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl)pyrazine-2-carboxamide) andMPX- 007 (5-(((3-fluoro-4-fluorophenyl)sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl) methylpyrazine-2-carboxamide).MPX-004 andMPX-007 inhibit GluN2A-containingNMDA receptors expressed inHEK cells with IC50s of 79 nMand 27nM, respectively. In contrast, at concentrations that completely inhibitedGluN2A activity these compounds have no inhibitory effect onGluN2B or GluN2D receptor-mediated responses in similarHEK cell-based assays. Potency and selectivitywere confirmed in electrophysiology assays in Xenopus oocytes expressingGluN2A-Dreceptor subtypes.Maximal concentrations ofMPX-004 andMPX-007 inhibited ~30%of the whole-cell current in rat pyramidal neurons in primary culture andMPX- 004 inhibited ~60%of the totalNMDAreceptor-mediated EPSP in rat hippocampal slices. GluN2A-selectivity at native receptorswas confirmed by the finding thatMPX-004 had no inhibitory effect onNMDAreceptor mediated synaptic currents in cortical slices fromGRIN2A knock out mice. Thus,MPX-004 andMPX-007 offer highly selective pharmacological tools to probeGluN2A physiology and involvement in neuropsychiatric and developmental disorders.", "link"=>"http://www.mendeley.com/research/mpx004-mpx007-new-pharmacological-tools-study-physiology-nmda-receptors-containing-glun2a-subunit", "reader_count"=>40, "reader_count_by_academic_status"=>{"Unspecified"=>2, "Researcher"=>8, "Student > Doctoral Student"=>4, "Student > Ph. D. Student"=>9, "Student > Postgraduate"=>3, "Student > Master"=>4, "Other"=>3, "Student > Bachelor"=>5, "Lecturer"=>1, "Lecturer > Senior Lecturer"=>1}, "reader_count_by_user_role"=>{"Unspecified"=>2, "Researcher"=>8, "Student > Doctoral Student"=>4, "Student > Ph. D. Student"=>9, "Student > Postgraduate"=>3, "Student > Master"=>4, "Other"=>3, "Student > Bachelor"=>5, "Lecturer"=>1, "Lecturer > Senior Lecturer"=>1}, "reader_count_by_subject_area"=>{"Unspecified"=>3, "Biochemistry, Genetics and Molecular Biology"=>4, "Agricultural and Biological Sciences"=>10, "Medicine and Dentistry"=>1, "Neuroscience"=>11, "Psychology"=>5, "Chemistry"=>5, "Pharmacology, Toxicology and Pharmaceutical Science"=>1}, "reader_count_by_subdiscipline"=>{"Medicine and Dentistry"=>{"Medicine and Dentistry"=>1}, "Neuroscience"=>{"Neuroscience"=>11}, "Chemistry"=>{"Chemistry"=>5}, "Psychology"=>{"Psychology"=>5}, "Agricultural and Biological Sciences"=>{"Agricultural and Biological Sciences"=>10}, "Biochemistry, Genetics and Molecular Biology"=>{"Biochemistry, Genetics and Molecular Biology"=>4}, "Unspecified"=>{"Unspecified"=>3}, "Pharmacology, Toxicology and Pharmaceutical Science"=>{"Pharmacology, Toxicology and Pharmaceutical Science"=>1}}, "reader_count_by_country"=>{"Colombia"=>1, "United States"=>2}, "group_count"=>1}

Scopus | Further Information

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Figshare

  • {"files"=>["https://ndownloader.figshare.com/files/4222798"], "description"=>"<p>Slices were exposed to MPX-004 from 100 nM to 30 μM in half log concentration increments as well as to 50 μM. Right panel- Time course for inhibition of fEPSPs after application of different concentrations of MPX-004. Left panel- Percent inhibition at 40 min after application for each MPX-004 concentration. Maximum inhibition was approximately 60% of the fEPSPs at 30 or 50 μM. The IC<sub>50</sub> of MPX-004 for inhibition of fEPSPs was 3.4 μM. Curves in the right panel and data point in the left panel are a mean (± SEM) of 4, 5, 6, 8, 6, 5 and 2 slices obtained from 2, 2, 3, 3, 2, 2 and 1 rats exposed to 0.1, 0.3, 1, 3, 10, 30 and 50 μM MPX-004, respectively. In separate experiments, a highly selective GluN2B NAM inhibited approximately 40% of the fEPSP (data not shown).</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578756, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g006", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Effect_of_MPX_004_on_isolated_NMDA_receptor_mediated_fEPSPs_in_rat_hippocampal_CA1_stratum_radiatum_in_response_to_stimulation_of_Schaffer_collateral_input_/2578756", "title"=>"Effect of MPX-004 on isolated NMDA receptor-mediated fEPSPs in rat hippocampal CA1 stratum radiatum in response to stimulation of Schaffer collateral input.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222828"], "description"=>"<p>Physical/Chemical and <i>in vitro</i> ADME properties of TCN-201, MPX-004 and MPX-007.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578789, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.t002", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Physical_Chemical_and_i_in_vitro_i_ADME_properties_of_TCN_201_MPX_004_and_MPX_007_/2578789", "title"=>"Physical/Chemical and <i>in vitro</i> ADME properties of TCN-201, MPX-004 and MPX-007.", "pos_in_sequence"=>0, "defined_type"=>3, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222675"], "description"=>"<p><b>C</b>ells were stimulated with glutamate and glycine (3 μM each) in the presence of compounds at a range of concentrations. IC<sub>50</sub> for inhibition of the Ca<sup>2+</sup> response in GluN2A-expressing cells was fitted to the Hill equation using CDD Vault. For GluN2B or GluN2D no IC<sub>50</sub> could be determined, so the effect of each compound at 10 μM is shown as the % inhibition of the Ca<sup>2+</sup> response (note that negative % inhibition represents an increase in Ca<sup>2+</sup> response over glutamate plus glycine alone). Values are the mean IC<sub>50</sub> or % ± SEM with the number of replicate curves indicated in parentheses. ND- not determined.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578630, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g003", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Potency_or_efficacy_of_TCN_201_and_selected_analogs_for_inhibition_of_Ca_sup_2_sup_responses_mediated_by_GluN2A_GluN2B_and_GluN2D_expressed_in_HEK_cells_/2578630", "title"=>"Potency or efficacy of TCN-201 and selected analogs for inhibition of Ca<sup>2+</sup> responses mediated by GluN2A, GluN2B and GluN2D expressed in HEK cells.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222834"], "description"=>"<p>Effect of MPX-004 on the ratio of NMDA receptor- to AMPA receptor-mediated synaptic currents (NMDAR/AMPAR ratio) at layer 4-to-2/3 synapses in mouse visual cortex.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578792, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.t003", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Effect_of_MPX_004_on_the_ratio_of_NMDA_receptor_to_AMPA_receptor_mediated_synaptic_currents_NMDAR_AMPAR_ratio_at_layer_4_to_2_3_synapses_in_mouse_visual_cortex_/2578792", "title"=>"Effect of MPX-004 on the ratio of NMDA receptor- to AMPA receptor-mediated synaptic currents (NMDAR/AMPAR ratio) at layer 4-to-2/3 synapses in mouse visual cortex.", "pos_in_sequence"=>0, "defined_type"=>3, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222723"], "description"=>"<p>Oocytes were exposed to MPX-004 or MPX-007 at concentrations from 10 nM to 10 μM as indicated. Inhibition curves were generated using GraphPad Prism and IC<sub>50</sub> values were generated using CCD Vault. The IC<sub>50</sub>s for inhibition of GluN2A-mediated currents were 198 ± 17 and 143 ± 10 nM for MPX-004 and MPX-007, respectively. Each data point is a mean (± standard deviation) of data from 4–12 oocytes.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578669, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g004", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Effect_of_MPX_004_and_MPX_007_on_glutamate_glycine_induced_currents_in_i_Xenopus_i_oocytes_expressing_GluN1_and_GluN2A_B_C_or_D_/2578669", "title"=>"Effect of MPX-004 and MPX-007 on glutamate/glycine-induced currents in <i>Xenopus</i> oocytes expressing GluN1 and GluN2A, B, C, or D.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222570"], "description"=>"<p>The values are IC<sub>50</sub>s for inhibition of Ca<sup>2+</sup> responses mediated by GluN2A receptors expressed in HEK cells.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578573, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g001", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/The_structures_of_TCN_201_MPX_004_and_MPX_007_/2578573", "title"=>"The structures of TCN-201, MPX-004 and MPX-007.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222816"], "description"=>"<p>Synthetic schemes for compounds 2–10.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578777, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g007", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Synthetic_schemes_for_compounds_2_10_/2578777", "title"=>"Synthetic schemes for compounds 2–10.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222819"], "description"=>"<p>Potency of standard NMDA antagonists for inhibition of Ca<sup>2+</sup> responses mediated by GluN2A, GluN2B and GluN2D expressed in HEK cells.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578780, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.t001", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Potency_of_standard_NMDA_antagonists_for_inhibition_of_Ca_sup_2_sup_responses_mediated_by_GluN2A_GluN2B_and_GluN2D_expressed_in_HEK_cells_/2578780", "title"=>"Potency of standard NMDA antagonists for inhibition of Ca<sup>2+</sup> responses mediated by GluN2A, GluN2B and GluN2D expressed in HEK cells.", "pos_in_sequence"=>0, "defined_type"=>3, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222759"], "description"=>"<p>Cortical neurons were maintained in primary culture for 13–15 days and then examined using whole-cell manual patch clamp for current evoked by NMDA (100 μM) + glycine (10 μM) applied for 4 seconds during 10 second pulses to +20 or +40 mV from a holding potential of -70 mV. Inhibition of NMDA-activated currents was quantified during exposure to 10 μM MPX-007, MPX-004, Ro 25–6981, or a combination of Ro 25–6981 + MPX-004. Currents were blocked ~25–30% by either MPX-007 or MPX-004 alone, ~70% by Ro 25–6981 alone, and ~85% by Ro 25–6981 plus MPX-004.</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578717, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g005", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Effects_of_MPX_004_and_MPX_007_on_NMDA_glycine_induced_currents_of_rat_cortical_neurons_in_primary_culture_/2578717", "title"=>"Effects of MPX-004 and MPX-007 on NMDA/glycine-induced currents of rat cortical neurons in primary culture.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}
  • {"files"=>["https://ndownloader.figshare.com/files/4222621"], "description"=>"<p>Cells were stimulated with glutamate and glycine (3 μM each) in the presence of compounds at a range of concentrations. Curves for inhibition of the Ca<sup>2+</sup> response in GluN2A-expressing cells were derived from fits to the Hill equation using GraphPad Prism (v6.00 for Mac, GraphPad Software, La Jolla California USA). Whereas MPX-004 and MPX-007 achieve full inhibition of the GluN2A Ca<sup>2+</sup> response by ~ 3 μM, TCN-201 never inhibits more than ~40% of the response. Each data point is a mean (± standard deviation) of data from 20–86 experiments).</p>", "links"=>[], "tags"=>["probe GluN 2A physiology", "GluN 2A", "GluN 2A NMDA receptors", "GluN 2 NMDA receptor subunits", "2D", "2B", "GluN 2A receptor subtypes", "GluN 2A Subunit GluN 2A", "rat hippocampal slices", "NMDA Receptors Containing", "MPX", "GRIN", "HEK", "GluN 2A receptors", "GluN 2A activity", "CNS", "IC", "EPSP"], "article_id"=>2578597, "categories"=>["Biochemistry", "Cell Biology", "Molecular Biology", "Neuroscience", "Pharmacology", "Chemical Sciences not elsewhere classified", "Cancer", "Mental Health"], "users"=>["Robert A. Volkmann", "Christopher M. Fanger", "David R. Anderson", "Venkata Ramana Sirivolu", "Kathy Paschetto", "Earl Gordon", "Caterina Virginio", "Melanie Gleyzes", "Bruno Buisson", "Esther Steidl", "Susanna B. Mierau", "Michela Fagiolini", "Frank S. Menniti"], "doi"=>"https://dx.doi.org/10.1371/journal.pone.0148129.g002", "stats"=>{"downloads"=>0, "page_views"=>0, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Concentration_response_of_TCN_201_MPX_004_and_MPX_007_inhibition_of_Ca_sup_2_sup_responses_mediated_by_GluN2A_expressed_in_HEK_cells_/2578597", "title"=>"Concentration-response of TCN-201, MPX-004, and MPX-007 inhibition of Ca<sup>2+</sup> responses mediated by GluN2A expressed in HEK cells.", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2016-02-01 13:00:18"}

PMC Usage Stats | Further Information

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  • {"unique-ip"=>"12", "full-text"=>"18", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2018", "month"=>"11"}
  • {"unique-ip"=>"9", "full-text"=>"11", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"1", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"2"}
  • {"unique-ip"=>"7", "full-text"=>"7", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"3"}
  • {"unique-ip"=>"11", "full-text"=>"12", "pdf"=>"6", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"1", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"4"}
  • {"unique-ip"=>"10", "full-text"=>"16", "pdf"=>"3", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"5"}
  • {"unique-ip"=>"14", "full-text"=>"12", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"7", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"8"}
  • {"unique-ip"=>"8", "full-text"=>"11", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"9"}
  • {"unique-ip"=>"33", "full-text"=>"46", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"10"}
  • {"unique-ip"=>"11", "full-text"=>"7", "pdf"=>"6", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2019", "month"=>"12"}
  • {"unique-ip"=>"6", "full-text"=>"6", "pdf"=>"1", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"0", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2020", "month"=>"2"}
  • {"unique-ip"=>"5", "full-text"=>"2", "pdf"=>"6", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"2", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2020", "month"=>"3"}
  • {"unique-ip"=>"11", "full-text"=>"11", "pdf"=>"2", "scanned-summary"=>"0", "scanned-page-browse"=>"0", "figure"=>"4", "supp-data"=>"0", "cited-by"=>"0", "year"=>"2020", "month"=>"4"}

Relative Metric

{"start_date"=>"2016-01-01T00:00:00Z", "end_date"=>"2016-12-31T00:00:00Z", "subject_areas"=>[]}
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