Cooper, Anna G. published the artcileAlkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment, COA of Formula: C6H13NO2, the publication is European Journal of Medicinal Chemistry (2018), 770-789, database is CAplus and MEDLINE.
Cannabinoid type 2 (CB2) receptor continues to emerge as a promising drug target for many diseases and conditions. New tools for studying CB2 receptor are required to further inform how this receptor functions in healthy and diseased states. The alkyl indole scaffold is a well-recognized ligand for cannabinoid receptors, and in this study the indole C5-7 positions were explored for linker and fluorophore attachment. A new high affinity, CB2 receptor selective inverse agonist was identified (16b, 3-(4-methoxybenzoyl)-1-[(oxan-4-yl)methyl]-7-propoxy-1H-indole) along with a general trend of C5-substituted indoles acting as agonists vs. C7-substituted indoles acting as inverse agonists. The indole C7 position was found to be the most tolerant to linker extension and resulted in a high affinity inverse agonist with a medium length linker (19, Me 5-[[3-(4-methoxybenzoyl)-1-[(oxan-4-yl)methyl]-1H-indol-7-yl]oxy]pentanoate). Although a high affinity fluorescent ligand for CB2 receptor was not identified in this study, the indole C7 position shows great promise for fluorophore or probe attachment.
European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, COA of Formula: C6H13NO2.
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