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.
MeSH terms
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Analgesics / chemistry*
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Analgesics / pharmacology*
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Animals
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Benzoates / chemistry*
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Benzoates / pharmacology*
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Humans
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Ligands
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Male
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Mice
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Mice, Inbred Strains
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Receptor, Cannabinoid, CB1 / agonists*
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Structure-Activity Relationship
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology*
Substances
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8-quinolinyl 4-methyl-3-(1-piperidinylsulfonyl)benzoate
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Analgesics
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Benzoates
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Ligands
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Receptor, Cannabinoid, CB1
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Sulfonamides