Abstract
The design and profile of a series of indole containing long acting beta(2)-adrenoceptor agonists is described. Evaluation of these analogues using an in vitro guinea pig trachea tissue model demonstrates that analogues within this series have salmeterol-like duration of action with potential for long duration of action in humans.
MeSH terms
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Adrenergic beta-Agonists / chemistry*
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Adrenergic beta-Agonists / pharmacokinetics
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Adrenergic beta-Agonists / pharmacology*
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Albuterol / analogs & derivatives
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Albuterol / chemistry
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Albuterol / pharmacology
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Animals
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Asthma / drug therapy*
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Biological Availability
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CHO Cells
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Caco-2 Cells
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Cricetinae
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Cricetulus
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Drug Design
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Drug Evaluation, Preclinical
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Guinea Pigs
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Humans
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Indoles / chemistry*
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Indoles / pharmacokinetics
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Indoles / pharmacology*
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Microsomes / drug effects
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Microsomes / metabolism
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Models, Molecular
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Molecular Structure
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Pulmonary Disease, Chronic Obstructive / drug therapy*
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Rats
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Receptors, Adrenergic, beta-2 / drug effects*
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Salmeterol Xinafoate
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Time Factors
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Trachea / drug effects
Substances
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Adrenergic beta-Agonists
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Indoles
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Receptors, Adrenergic, beta-2
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Salmeterol Xinafoate
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Albuterol