Patent ID: 8933020
Filing Date: 2015-01-13
Classification: A61P,C07K

Abstract:
1. A method of increasing permeability of the blood brain barrier for a neuropeptide comprising modifying the neuropeptide, the neuropeptide being derived from an unmodified neuropeptide selected from galanin, somatostatin, delta-sleep inducing peptide, and neuropeptide Y, comprising: generating a first modification relative to the unmodified neuropeptide that increases the lipophilic character of the modified neuropeptide when compared to the unmodified neuropeptide; with the first modification being selected from at least one of: (a) a hydrophobic moiety conjugated to one or more amino acid residues of the modified neuropeptide; and (b) substitution of one or more aromatic amino acid residues with a halogenated aromatic amino acid residue; and generating a second modification relative to the unmodified neuropeptide that increases the basicity of the modified neuropeptide when compared to the unmodified neuropeptide, with the second modification being selected from at least one of: (a) an oligomer of positively charged amino acid residues introduced into the amino acid sequence of the unmodified neuropeptide, wherein the oligomer is selected from the group consisting of homooligomers and heterooligomers comprising Lysine, Arginine, homo-Lysine, homo-Arginine, L-Ornithine, D-Ornithine, 2,3-Diaminopropioic acid, and 2,4-Diaminobutyric acid, and (b) a polyamine-based moiety conjugated to the modified neuropeptide, wherein the polyamine-based moiety is selected from the group consisting of spermine, spermidine, polyamidoamine, dendrimers, and polyamine toxins.