The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
The design and profile of a series of adamantyl-containing long acting beta(2)-adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a guinea pig trachea tissue model. A focus was then placed on developing a robust synthetic route to ensure rapid delivery of material for clinical trials.
Brown
Alan D
AD
Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
Bunnage
Mark E
ME
Glossop
Paul A
PA
James
Kim
K
Jones
Rhys
R
Lane
Charlotte A L
CA
Lewthwaite
Russell A
RA
Mantell
Simon
S
Perros-Huguet
Christelle
C
Price
David A
DA
Trevethick
Mike
M
Webster
Rob
R
D000218:Adamantane / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000280:Administration, Inhalation; D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D006168:Guinea Pigs; D006801:Humans; D014132:Trachea / Q000187:drug effects
D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists; D000218:Adamantane