Patent ID: 7214657

Claim:
A method of transporting a pharmacologically active peptide across the blood brain barrier into the central nervous system of a living subject, by administration to said subject conjugate molecule comprising said peptide covalently linked to a non-peptide mu (μ) opioid receptor agonist, comprising: a. Selecting a non-peptide mu (μ) opioid receptor agonist and a cross-linker, such that when the mu (μ) opioid receptor agonist is modified and covalently linked to the cross-linker and the cross-linker is covalently linked via a peptide bond to the pharmacologically active peptide, the cross-clinker will be able to flex such that the mu (μ) opioid opioid receptor agonist and the pharmacologically active peptide contemporaneously active their respective receptors; b. Modifying the mu (μ) opioid receptor agonist such that it can be covalently attached to a flexible cross-linker, the covalent attachment of the modified mu (μ) opioid receptor agonist to the flexible hinge cross-linker, and the covalent attachment of the cross-linker via a peptide bond to the pharmacologically active peptide, to form a conjugate molecule; and c. Administering a pharmaceutical composition of said conjugate molecule to said living subject.