期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 75, 期 1, 页码 106-114出版社
WILEY
DOI: 10.1111/j.1747-0285.2009.00910.x
关键词
aminoalkylindole analogs; analgesic agents; cannabimimetic agents; CB1 receptor; SAR study
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.
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