Sigma 2 Receptor Ligands and Therapeutic Uses Therefor
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Abstract
A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
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10 Claims
- 1. A compound selected from the group consisting of
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4. A method of inducing apoptosis in a tumor cell, the method comprising contacting the cell with at least one σ
- 2 receptor ligand or a salt thereof, wherein the at least one σ
2 receptor ligand is selected from the group consisting of - View Dependent Claims (5)
- 2 receptor ligand or a salt thereof, wherein the at least one σ
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6. A method for treating a cancer, the method comprising administering to a subject in need of cancer therapy a therapeutically effective amount of a σ
- 2 receptor ligand or a salt thereof, wherein the ligand is selected from the group consisting of
- View Dependent Claims (7, 8, 9, 10)
Specification