New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists |
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| Authors: | Pagé Daniel Yang Hua Brown William Walpole Christopher Fleurent Manon Fyfe Meredith Gaudreault François St-Onge Stéphane |
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| Institution: | Department of Medicinal Chemistry, AstraZeneca R&D Montreal, St-Laurent, Quebec, Canada. daniel.page@astrazeneca.com |
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| Abstract: | The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo3,4-b]indole moiety are reported. They showed binding affinities up to 4.2 nM toward CB2 with sub-nanomolar EC(50) values. They also showed moderate to good (>350-fold) selectivity over the CB1 receptor. |
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