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US 8,772,308 B2Granted
Non-peptidyl, potent, and selective mu opioid receptor antagonists
AssigneeVirginia Commonwealth University
InventorsYan Zhang, Dana E. Selley, William Dewey
Life of this patent
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Abstract
Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.
Claims5
A selective, non-peptide MOR antagonist represented by formula
- where
- Z is selected from the group consisting of an aliphatic moiety, NH, CO, (NHCO)n where n=1-5, (CONH)n where n=1-5, (NHCO)(CH2)n(NHCO), where n=1-5, (NHCO)(CH2)n where n=1-5, (CH2)n(NHCO), where n=1-5, and O, and
- R is selected from the group consisting of
A method of testing whether or not a candidate compound is a MOR agonist, comprising the step of
- conducting competitive inhibition tests between said candidate compound and a MOR antagonist represented by formula
- where
- Z is selected from the group consisting of an aliphatic moiety, NH, CO, (NHCO)n where n=1-5, (CONH)n where n=1-5, (NHCO)(CH2)n(NHCO), where n=1-5, (NHCO)(CH2)n where n=1-5, (CH2)n(NHCO), where n=1-5, and O, and
- R is selected from the group consisting of
1 more element
A method of treating symptoms of opiate addiction in a patient in need thereof, comprising
- administering to said patient a MOR antagonist represented by formula
- where
- Z is selected from the group consisting of an aliphatic moiety, NH, CO, (NHCO)n where n=1-5, (CONH)n where n=1-5, (NHCO)(CH2)n(NHCO), where n=1-5, (NHCO)(CH2)n where n=1-5, (CH2)n(NHCO), where n=1-5, and O, and
- R is selected from the group consisting of
1 more element
Dependencies are inferred from the claim text.