Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Paper

Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Published 2000 · L. Brockunier, E. Parmee, H. Ok

Bioorganic & medicinal chemistry letters

Q2 SJR score

166

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0

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Semantic Scholar

Abstract

Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were prepared and found to be potent and selective human beta3-adrenergic receptor agonists. The most interesting compound, trifluoromethylbenzyl analogue 12e (beta3 EC50 = 3.1 nM with >1500-fold selectivity over binding to both beta1- and beta2 receptors), stimulates lipolysis in the rhesus monkey (ED50 = 0.36 mg/kg) and is 25% orally bioavailable in the dog.

Highly Cited

Study Snapshot

Trifluoromethylbenzyl analogue 12e is a potent and selective human beta3-adrenergic receptor agonist with potential for lipolysis stimulation in rhesus monkeys and 25% oral bioavailability in dogs.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

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