- Aryl-substituted derivatives of cycloalkyl and branched chain alkyl carboxylic acids useful as antinociceptive drugs for peripheral targets
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Novel peripheral antinociceptive compounds are disclosed having a pharmacophore unit that target small-diameter nerve fibers that transmit signals of pain and discomfort from the soma and viscera. By acting on this target, the pharmacophore unit obtunds pain and diminishes hyper-reflexia from organs such as the skin, the respiratory tract, the corpus, the lower urinary tract, and the bowel. The pharmacophore unit is coupled to substituents that facilitate delivery of the pharmacophore to its target.
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- Radioligands for the TRP-M8 receptor and methods therewith
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One embodiment of the invention is a composition that comprises a radioactive [18F], [123I], [125I], or [131I]—N-radiohaloaryl-alkylcarboxamide molecule. The composition binds to the transient receptor potential-M8 (TRP-M8) receptor of cells. The TRP-M8 receptor is selectively expressed in sensory neurons and in malignant tissues such as prostate cancer cells. The [18F], [123I], [125I], or [131I]—N-radiohaloaryl-alkylcarboxamide ligand may be used for radioreceptor binding studies, for diagnostic studies, and for radiotherapy of cancerous tissues. Affinity of the [125I] or [131I]—N-radiohaloaryl-alkylcarboxamide ligand for the TRP-M8 receptor confers selectivity and specificity in delivering lethal radiation to the diseased cells.
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