Allosteric modulators of the NMDA receptor and their use in the treatment of CNS disorders and enhancement of CNS function
AssigneeBearsden Bio, Inc.
InventorMaria-Luisa Maccecchini
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Abstract
Novel compounds and compositions for modulating NMDA receptor function comprising Conantokin-G and derivatives thereof; methods for modulating NMDA receptor function and methods for treating neuropsychopharmacological disorders, using the novel compounds and compositions of the invention; and a method for screening compounds capable of binding to a novel allosteric modulatory site, are described.
Claims6
A composition comprising a compound or pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier, wherein the compound is selected from the group consisting of SEQ ID No:55 GEggLQSNVSQIRAKSN;
- SEQ ID No:56 GEggLQAALALIRAKSN;
- SEQ ID No:57 GEggL-gKSN;
- SEQ ID No:58 GEggL-GG-gKSN;
- SEQ ID No:59 GEggL-GGGG-gKSN;
- SEQ ID No:60 GFggL-AA-gKSN;
- SEQ ID No:61 GEggL-AAA-gKSN;
- SEQ ID No:62 GEggLQ-AAAAA-gSKN;
- SEQ ID No:63 GEggLQ-AAAAAAA-gKSN;
- and SEQ ID No:64 GEggL-BB-gKSN.
A composition comprising a compound or a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier, wherein said compound is an antagonist of the NMDA receptor and has the following formula:
- A1-A2-A3-A4-A5-A6-(A7)xc-[A8-(A9-A10)xd—NH2]n
- wherein
- A1 is glycine, alanine, valine, leucine or isoleucine;
- A2 is glutamic acid, aspartic acid, γ-carboxyglutamate (Gla), 3-carboxyaspartic acid, D-glutamic acid, phosphoserine or phosphothreonine;
- A3 is glutamic acid, aspartic acid, γ-carboxyglutamate (Gla), 3-carboxyaspartic acid, D-glutamic acid, phosphoserine or phosphothreonine;
- A4 is Gla;
- A5 is glycine, alanine, valinc, leucine or isoleucine;
- A6 is a peptide of 7-9 amino acids;
- A7 is an amino acid selected from the group consisting of natural, modified or non-natural amino acids;
- A8 is lysine or arginine;
- A9 is an amino acid selected from the group consisting of natural, modified or non-natural amino acids;
- A10 is an amino acid selected from the group consisting of natural, modified or non-natural amino acids;
- xc and xd are independently 0 or 1;
- and
- n is 0 or 1,
- with the proviso that the compound is not GEggLQgNQgLIRgKSN (SEQ ID NO:1).
Dependencies are inferred from the claim text.