Abstract
Pyridyloxypropanolamines L-749,372 (8, beta 3 EC50 = 3.6 nM) and L-750,355 (29, beta 3 EC50 = 13 nM) are selective partial agonists of the human receptor, with 33% and 49% activation, respectively. Both stimulate lipolysis in rhesus monkeys (ED50 = 2 and 0.8 mg/kg, respectively), with minimal effects on heart rate. Oral bioavailability in dogs, 41% for L-749,372 and 47% for L-750,355, is improved relative to phenol analogs.
MeSH terms
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Adrenergic beta-Agonists / chemical synthesis*
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Adrenergic beta-Agonists / chemistry
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Adrenergic beta-Agonists / pharmacokinetics
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Animals
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Binding, Competitive
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Biological Availability
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Dogs
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Humans
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Kinetics
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Lipolysis / drug effects
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Macaca mulatta
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Molecular Structure
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Propanolamines / chemical synthesis*
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Propanolamines / chemistry
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Propanolamines / pharmacokinetics*
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Propanolamines / pharmacology
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Pyridines
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Receptors, Adrenergic, beta / drug effects
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Receptors, Adrenergic, beta / physiology*
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Receptors, Adrenergic, beta-3
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacokinetics
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Sulfonamides / pharmacology
Substances
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Adrenergic beta-Agonists
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Propanolamines
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Pyridines
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Receptors, Adrenergic, beta
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Receptors, Adrenergic, beta-3
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Sulfonamides