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|Title:||Design, Synthesis, and Pharmacological Characterization of Indole-3-ylacetamides, Indole-3-yloxoacetamides, and Indole-3-ylcarboxamides: Potent and Selective CB2 Cannabinoid Receptor Inverse Agonists||Authors:||Pasquini, Serena
Borea, P. A.
Di Marzo, V.
|Issue Date:||2012||Project:||None||Journal:||JOURNAL OF MEDICINAL CHEMISTRY||Abstract:||
In our search for new cannabinoid receptormodulators, we describe herein the design and synthesis ofthree sets of indole-based ligands characterized by anacetamide, oxalylamide, or carboxamide chain, respectively.Most of the compounds showed affinity for CB2 receptors inthe nanomolar range, with Ki values spanning 3 orders ofmagnitude (377−0.37 nM), and moderate to good selectivityover CB1 receptors. Their in vitro functional activity as inverseagonists was confirmed in vivo in the formalin test of acuteperipheral and inflammatory pain in mice, in whichcompounds 10a and 11e proved to be able to reverse the effect of the CB2 selective agonist COR167
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