Contryphan peptides

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/64 (2006.01) C07H 21/00 (2006.01) C07K 7/06 (2006.01) C07K 14/435 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2270284

The present invention is directed to contryphan peptides having 6-12 amino acids, preferably including one or more D-tryptophan residues. More specifically, the present invention is directed to contryphan peptides having the general formula Xaa1-Cys-Xaa2-Xaa3-Glu-Pro-Trp-Cys (SEQ ID NO:1), wherein Xaa1 is Gly or des-Xaa1, Xaa2 is Pro or 4-trans-hydroxyproline and Xaa3 is D- Trp or L-Trp, preferably D-Trp. The present invention is further directed to the peptides contryphan R and des-Gly1 contryphan R. In contryphan R, Xaa1 is Gly and Xaa3 is D-Trp. These contryphans are useful as anticonvulsant or neuroprotective agents.

La présente invention concerne des peptides contryphanes présentant 6 à 12 aminoacides, et comprenant, de préférence, au moins un résidu de D-tryptophane. Plus spécifiquement, la présente invention concerne des peptides contryphanes correspondant à la formule générale Xaa¿1?-Cys-Xaa¿2?-Xaa¿3?-Glu-Pro-Trp-Cys (SEQ ID NO:1), dans laquelle Xaa¿1? représente Gly ou bien des-Xaa¿1?, Xaa¿2? représente Pro ou bien 4-trans-hydroxyproline, et Xaa¿3? représente D-Trp ou bien L-Trp, de préférence D-Trp. La présente invention concerne également les peptides contryphane R et des-Gly?1¿ contryphane R. Dans le peptide contryphane R, Xaa¿1? représente Gly et Xaa¿3? représente D-Trp. Ces contryphanes peuvent être utilisés comme agents anticonvulsivants ou neuroprotecteurs.

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