Abstract
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be therapeutically useful. The pharmacological and pharmacokinetic SAR of a series of inhaled A(2A) agonists is described leading through to human pharmacokinetic data for a clinical candidate.
MeSH terms
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Adenosine / analogs & derivatives
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Adenosine / chemistry
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Adenosine A2 Receptor Agonists*
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Administration, Inhalation
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Adolescent
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Adult
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Animals
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Chemistry, Pharmaceutical / methods
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Drug Design
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Humans
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Inhibitory Concentration 50
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Lung / drug effects
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Male
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Middle Aged
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Models, Chemical
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Phenethylamines / chemistry
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Pulmonary Disease, Chronic Obstructive / drug therapy*
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Purines / chemistry
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Rats
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Structure-Activity Relationship
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Triazoles / chemistry
Substances
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Adenosine A2 Receptor Agonists
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GW 328267
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Phenethylamines
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Purines
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Triazoles
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2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine
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Adenosine