Conotoxin peptides useful as inhibitors of neuronal amine transporters

Abstract

The invention relates to an isolated, synthetic or recombinant χ-conotoxin peptide having the ability to inhibit a neuronal amine transporter, nucleic acid molecules encoding all or part of such peptides, antibodies to such peptides and uses and methods of treatment involving them.

1 - 6 . (canceled) 
     
     
         7 . An isolated, synthetic or recombinant χ-conotoxin peptide having the activity inhibiting a neuronal amine transporter, wherein said χ-conotoxin peptide comprises MrIA as set forth in SEQ ID NO: 1 (NGVCCGYKLCHOC) or a modified sequence of SEQ ID NO: 1 which has undergone a conservative substitution of an amino acid residue, wherein “◯” represents 4-hydroxyproline, and wherein the first and fourth cysteine residues of SEQ ID NO: 1 are connected to form a disulfide bond and the second and third cysteine residues of SEQ ID NO: 1 are connected to form a disulfide bond. 
     
     
         8 . The χ-conotoxin peptide according to  claim 7  having the ability to inhibit a neuronal noradrenaline transporter. 
     
     
         9 . The χ-conotoxin peptide according to  claim 8  which is a selective inhibitor of neuronal noradrenaline transporter. 
     
     
         10 . The χ-conotoxin peptide according to  claim 8  having negligible or no anticholinergic effect. 
     
     
         11 . The χ-conotoxin peptide according to  claim 8  having negligible or no activity as a sodium channel blocker. 
     
     
         12 . The χ-conotoxin peptide according to  claim 8  having negligible or no activity as an inhibitor of dopamine transporter. 
     
     
         13 . (canceled) 
     
     
         14 . A composition comprising a χ-conotoxin peptide and a pharmaceutically acceptable carrier or diluent, wherein said χ-conotoxin peptide is a peptide according to  claim 7 . 
     
     
         15 . The composition according to  claim 14  which is a pharmaceutical composition. 
     
     
         16 - 17 . (canceled)