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.
Claims8
A composition comprising a compound selected from the group consisting of partial agonists, agonists and antagonists binding to the NMDA receptor in combination with a pharmaceutical carrier wherein the compound has a formula selected from the group consisting of:
- Asn Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:14);
- Phe Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:16);
- t-BuTyr Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:20);
- Ser Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:21);
- Gly Glu Ser Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2, wherein the serine at position 3 is phosphorylated (SEQ. ID NO:24);
- Gly Glu Ala Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:22);
- Gly Glu Gla Gla Leu Gln Tyr Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:31);
- Gly Glu Gla Gla Leu Gln Ala Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:32);
- Gly Glu Gla Gla Leu Gln Ser Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:33);
- Gly Glu Gla Gla Leu Gln Ser Asn Gln Gla Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 wherein the first serine is phosphorylated (SEQ. ID NO:34);
- Gly Glu Gla Gla Leu Gln Gla Asn Gln Ala Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:35);
- Gly Glu Gla Gla Leu Gln Gla Asn Gln Ser Leu Ile Arg Gla Lys Ser Asn-NH.sub.2 (SEQ. ID NO:36);
- Gly Glu Gla Gla Leu Gln Gla Asn Gln Ser Leu Ile Arg Gla Lys Ser Asn-NH.sub.2, wherein the first serine is phosphorylated (SEQ. ID NO:37);
- Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Ala Lys Ser Asn-NH.sub.2 (SEQ. ID NO:38);
- Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Ser Lys Ser Asn-NH.sub.2 (SEQ. ID NO:39);
- Gly Glu Gla Gla Leu Gln Gla Asn Gln Gla Leu Ile Arg Ser Lys Ser Asn-NH.sub.2, wherein the first serine is phosphorylated (SEQ. ID NO:40);
- Gly Glu Gla Gla Leu Gln Ala Asn Gln Ala Leu Ile Arg Ala Lys Ser Asn-NH.sub.2 (SEQ. ID NO:42);
- and Gla Lys Ser Asn-NH2 (SEQ. ID NO:49).
A composition comprising a compound selected from the group consisting of agonists, partial agonists and antagonists binding to the NMDA receptor in combination with a pharmaceutical carrier, wherein the compound has a formula selected from the group consisting of:
- Tyr Gly Glu Glu Glu Leu Gln Glu Asn Gln Glu Leu Ile Arg Glu Lys Ser Asn-NH.sub.2 (SEQ ID NO:6) and
- Glu Glu Glu Leu Gln Glu Asn Gln Glu Leu Ile Arg Glu Lys Ser Asn-NH2 (SEQ ID NO:10).
Dependencies are inferred from the claim text.