Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies |
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| Authors: | Lambeng N Lebon F Christophe B Burton M De Ryck M Quéré L |
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| Affiliation: | CNS Molecular and Cellular Biology, Centre for CNS Innovation, UCB S.A., Chemin du Foriest, B-1420 Braine L'Alleud, Belgium. |
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| Abstract: | High-throughput screening of the UCB sample collection identified the piperidinyl-sulfonyl benzoic ester 1 as a novel agonist for CB(1) receptor with nanomolar affinity. We report here the pharmacological profile of compound 1 as well as preliminary biological activities in pain model. Diverse close analogs of 1 were purchased and the structure-affinity relationships among this novel class are discussed. |
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