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Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist
Journal article   Peer reviewed

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist

D D Feng, T Biftu, M R Candelore, M A Cascieri, L F Colwell, Jr, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, …
Bioorganic & medicinal chemistry letters, Vol.10(13), pp.1427-1429
07/03/2000
PMID: 10888324

Abstract

Oxadiazoles - administration & dosage Cricetinae Administration, Oral Humans Adrenergic beta-Agonists - pharmacology Rats Adrenergic beta-Agonists - pharmacokinetics Biological Availability Structure-Activity Relationship Adrenergic beta-Agonists - chemistry Animals Oxadiazoles - pharmacology Adrenergic beta-Agonists - administration & dosage Dogs Molecular Structure Oxadiazoles - chemistry Oxadiazoles - pharmacokinetics Adrenergic beta-3 Receptor Agonists CHO Cells Drug Design
5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective beta3 adrenergic receptor agonist (beta3 EC50 = 23 nM, beta1 IC50 = 3000 nM, beta2 IC50 = 3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable beta3 adrenergic receptor agonists reported to date.

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