Method of inhibiting opioid tolerance with chimeric hybrid analgesics
OwnerRichard M. Kreaminventor
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Abstract
The present invention provides a method of inhibiting the development of opioid tolerance using novel chimeric hybrid molecules containing an opioid moiety of chemically modified morphine (3) that binds to and activates the human mu (μ) opioid receptor, with the opioid moiety linked through a novel linker-hinge (4) to a substance P peptide fragment moiety (5) that binds to and activates the human substance P receptor. The hybrid alkaloid/peptide analgesics may be administered intrathecally, systemically or orally.
Claims1
A method of inhibiting the development of opioid tolerance by clinically administering a chemically combination of a pharmacologically active form of substance p with morphine in a chimeric hybrid molecule wherein morphine, chemically modified and covalently linked through its 6′OH group, comprises a cyclic alkaloid moiety which binds as an agonist to a mammalian or human (μ) opioid receptor;
- and wherein a pharmacologically active C-mu terminal substance P fragment, chemically modified and covalently linked through its free NH2 group, comprises a peptide moiety which binds as an agonist to a mammalian/human substance p receptor;
- and wherein a compact, but flexible, molecular hinge covalently cross links morphine through its 6′OH group to the free NH2 group of the substance p receptor agonist moiety, so as to allow both the mu (μ) opioid receptor and the substance p receptor agonist moieties to activate their respective receptors simultaneously and independently.
Dependencies are inferred from the claim text.