Novel sodium channel blocking peptides and the use thereof
AssigneePurdue Pharma L.P.
InventorsDonald James Kyle, Jae Hyun Park
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Abstract
The present invention relates to C-terminal modified Protoxin II peptides that selectively inhibit the Nav1.7 sodium channel; the present invention also relates to pharmaceutical compositions useful for prophylactic or therapeutic treatment of a disorder responsive to the blockade of sodium ion channels, especially Nav1.7 sodium ion channels; the present invention further provides methods of treating a disorder responsive to the blockade of sodium channels, and particularly Nav1.7 sodium channels, in a mammal sulfuring from excess activity of said channels.
Claims23
A C-terminal modified Protoxin II peptide of general formula (I):
- wherein:
- Pro is Protoxin II of the amino acid sequence:
- Tyr1-Cys2-Gln3-Lys4-Trp5-Met6-Trp7-Thr8-Cys9-Asp10-Ser11-Glu12-Arg13-Lys14-Cys15-Cys16-Glu17-Gly18-Met19-Val20-Cys21-Arg22-Leu23-Trp24-Cys25-Lys26-Lys27-Lys28-Leu29-Trp30 (SEQ ID NO:
- 1),
- wherein Trp30 is D or L—Trp30,
- X is —O—,
- R1 is C1-C6 alkyl, or C3-C7 cycloalkyl or C5-C10 aryl;
- or a pharmaceutically acceptable salt, prodrug or solvate thereof.
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19-22. (canceled)
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Dependencies are inferred from the claim text.