Patent ID: 6511963
Filing Date: 2003-01-28
Classification: A61K,A61P,C07K

Abstract:
A method for treating excitotoxicity resulting from over-stimulation of the NMDA receptor which comprises administering to a patient in need thereof a therapeutically effective amount of an active agent selected from the group consisting of Conantokin-G, a Conantokin-G derivative and pharmaceutically acceptable salts thereof, wherein Conantokin-G has the formula Gly-Glu-Xaa1-Xaa2-Leu-Gln-Xaa1-Asn-Gln-Xaa1-Leu-Ile-Arg-Xaa1-Lys-Ser-Asn (SEQ ID NO:1) where Xaa1 and Xaa2 are each &ggr;-carboxy-glutamic acid and wherein said Conantokin-G derivative is an antagonist of the NMDA receptor and has the following formula:A1â€”A2â€”A3â€”A4â€”A5â€”A6â€”(A7)xcâ€”[A8â€”(A9â€”A10)xdâ€”NH2]n whereinA1 is glycine, alanine, valine, leucine or isoleucine; A2 is glutamic acid, aspartic acid, &ggr;-carboxyglutamate (Gla), 3-carboxyaspartic acid, D-glutamic acid, phosphoserine or phosphothreonine; A3 is glutamic acid, aspartic acid, &ggr;-carboxyglutamate (Gla), 3-carboxyaspartic acid, D-glutamic acid, phosphoserine or phosphothreonine; A4 is Gla; A5 is glycine, alanine, valine, 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.