Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies.
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.
Lambeng
N
N
CNS Molecular and Cellular Biology, Centre for CNS Innovation, UCB S.A., Chemin du Foriest, B-1420 Braine L'Alleud, Belgium.
Lebon
F
F
Christophe
B
B
Burton
M
M
De Ryck
M
M
Quéré
L
L
D000700:Analgesics / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001565:Benzoates / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology*
C519013:8-quinolinyl 4-methyl-3-(1-piperidinylsulfonyl)benzoate; D000700:Analgesics; D001565:Benzoates; D008024:Ligands; D043884:Receptor, Cannabinoid, CB1; D013449:Sulfonamides