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Synthesis and Pharmacological Evaluation of Analogs of Indole‐Based Cannabimimetic Agents
Author(s) -
Mazzoni Orazio,
Diurno Maria V.,
Di Bosco Antonio M.,
Novellino Ettore,
Grieco Paolo,
Esposito Giovanni,
Bertamino Alessia,
Calignano Antonio,
Russo Roberto
Publication year - 2010
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2009.00910.x
Subject(s) - cannabinoid receptor , cannabinoid , indole test , chemistry , cannabinoid receptor agonists , receptor , pharmacology , cannabinoid receptor type 2 , stereochemistry , ligand binding assay , biochemistry , agonist , biology
Aminoalkylindoles (AAIs), although structurally dissimilar from the classical cannabinoids, are known to be capable of binding to cannabinoid receptors and of evoking cannabinomimetic responses. With the aim of investigating the structure–activity relationships (SAR) for the binding of non‐classical agonists to CB1 and CB2 cannabinoid receptors, we designed and synthesized a series of indole derivatives. The compounds were tested for their analgesic action by formalin test and compared to WIN 55212‐2, an AAI acting to the cannabinoid receptors. In receptor binding assay, compound 5 showed affinity for the CB1 receptor comparable to WIN 55212‐2.