2, 3-Dihydro-dithiin and-dithiepine-1, 1, 4, 4-tetroxides: small molecule non-peptide antagonists of the human galanin hGAL-1 receptor

…, CB Davis, JJ Crooke, AC Potocki, AB Reitz

Index: Scott, Malcolm K.; Ross, Tina M.; Lee, Daniel H. S.; Wang, Hoau-Yan; Shank, Richard P.; Wild, Kenneth D.; Davis, Coralie B.; Crooke, Jeffrey J.; Potocki, Alexander C.; Reitz, Allen B. Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 6 p. 1383 - 1391

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Citation Number: 60

Abstract

The neuropeptide galanin modulates several physiological functions such as cognition, learning, feeding behavior, and depression, probably via the galanin 1 receptor (GAL-R1). Using an HTS assay based on 125I-human galanin binding to the human galanin-1 receptor (hGAL-R1), we discovered a series of 1, 4-dithiin and dithiipine-1, 1, 4, 4-tetroxides that exhibited binding affinity IC50's to hGAL-R1 ranging from 190 to 2700nM. Two of the ...