Abstract
The cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.
MeSH terms
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Adrenergic beta-1 Receptor Agonists
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Adrenergic beta-2 Receptor Agonists
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Adrenergic beta-Agonists / chemical synthesis*
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Adrenergic beta-Agonists / pharmacokinetics
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Adrenergic beta-Agonists / pharmacology
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Animals
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CHO Cells
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Cricetinae
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Cyclopentanes / chemical synthesis*
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Cyclopentanes / pharmacokinetics
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Cyclopentanes / pharmacology
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Dose-Response Relationship, Drug
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Heart Rate / drug effects
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacokinetics
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Imidazoles / pharmacology
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Macaca mulatta
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Receptors, Adrenergic, beta / drug effects
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Receptors, Adrenergic, beta / metabolism*
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Receptors, Adrenergic, beta-3
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Structure-Activity Relationship
Substances
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Adrenergic beta-1 Receptor Agonists
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Adrenergic beta-2 Receptor Agonists
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Adrenergic beta-Agonists
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Cyclopentanes
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Imidazoles
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Receptors, Adrenergic, beta
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Receptors, Adrenergic, beta-3
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cyclopentylpropylimidazolidinone