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Synthetic peptides that modulate the NMDA receptor

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  • Publication Date:
    June 23, 2020
  • Additional Information
    • Patent Number:
      10689,418
    • Appl. No:
      16/065078
    • Application Filed:
      December 22, 2016
    • Abstract:
      The invention provides a series of peptides with N-methyl-D-aspartate (NMDA) receptor modulating activity. Specifically it contains two synthetic peptides acting as ion inflow antagonists through the NMDA receptor with specificity GluN2B and GluN2A NMDA receptor subunits and a peptide having agonist activity regarding the NMDA receptor in rat hippocampal neuron cultures.
    • Inventors:
      UNIVERSIDAD NACIONAL DE COLOMBIA (Bogotá, CO)
    • Assignees:
      Universidad Nacional de Colombia (Bogota, CO)
    • Claim:
      1. An artificially designed 17 amino acid-long peptide, wherein said peptide has the following hydrophilic amino acid sequence: GEDDLQDNQDLIRDKSN (SEQ ID NO: 2); said peptide having a molecular formula of C 78 H 127 N 25 O 35 ; a molecular weight of 1975.03 g/Mol; an isoelectric point of 3.90 and an average hydropathicity (GRAVY) of −1.912.
    • Claim:
      2. The peptide, according to claim 1 , wherein said peptide has selective antagonism towards the NMDA receptor GluN2B subunit.
    • Claim:
      3. The peptide, according to claim 1 , wherein said peptide is a membrane ionic permeability modifier in cell cultures.
    • Claim:
      4. The peptide, according to claim 1 , wherein said peptide is a membrane ionic permeability modifier of neurons in a primary culture.
    • Claim:
      5. A pharmaceutical composition useful for modifying neural membrane permeability wherein the active principle is a peptide according to claim 1 , in an effective amount to modify the neural membrane permeability along with a pharmaceutically acceptable carrier or vehicle.
    • Claim:
      6. The pharmaceutical composition according to claim 5 , wherein said peptide has selective antagonism towards the NMDA receptor GluN2B subunit.
    • Claim:
      7. The pharmaceutical composition according to claim 5 , wherein said peptide is a membrane ionic permeability modifier of neurons in a primary culture.
    • Claim:
      8. An artificially designed 17 amino acid-long peptide, wherein said peptide has the following hydrophilic amino acid sequence: GEDDYQDAQDLIRDKSN (SEQ ID NO: 3); has a molecular formula of C 80 H 124 N 24 O 35 ; a molecular weight of 1981.99 g/Mol; and isoelectric point of 3.90 and an average hydropathicity (GRAVY) of −1.900.
    • Claim:
      9. The peptide according to claim 8 , wherein said peptide has selective antagonism towards the NMDA receptor GluN2B and GluN2A subunits.
    • Claim:
      10. The peptide, according to claim 8 , wherein said peptide is a membrane ionic permeability modifier in cell cultures.
    • Claim:
      11. The peptide, according to claim 8 , wherein said peptide is a membrane ionic permeability modifier of neurons in a primary culture.
    • Claim:
      12. A pharmaceutical composition useful for modifying neural membrane permeability wherein the active principle is a peptide according to claim 8 , in an effective amount to modify the neural membrane permeability along with a pharmaceutically acceptable carrier or vehicle.
    • Claim:
      13. The pharmaceutical composition according to claim 12 , wherein said peptide has selective antagonism towards the NMDA receptor GluN2B and GluN2A subunits.
    • Claim:
      14. The pharmaceutical composition according to claim 12 , wherein said peptide is a membrane ionic permeability modifier in cell cultures.
    • Patent References Cited:
      5830998 November 1998 Maccecchini
      2003/0134799 July 2003 Maccecchini
      2003/0144210 July 2003 Olivera
      2003/0194729 October 2003 Abogadie
    • Primary Examiner:
      Ulm, John D
    • Attorney, Agent or Firm:
      Angres, Isaac
    • Accession Number:
      edspgr.10689418