title: The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
abstract: 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.
authors.affiliation: Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
authors.forename: Alan D
authors.initials: AD
authors.lastname: Brown
authors.forename: Mark E
authors.initials: ME
authors.lastname: Bunnage
authors.forename: Paul A
authors.initials: PA
authors.lastname: Glossop
authors.forename: Kim
authors.initials: K
authors.lastname: James
authors.forename: Rhys
authors.initials: R
authors.lastname: Jones
authors.forename: Charlotte A L
authors.initials: CA
authors.lastname: Lane
authors.forename: Russell A
authors.initials: RA
authors.lastname: Lewthwaite
authors.forename: Simon
authors.initials: S
authors.lastname: Mantell
authors.forename: Christelle
authors.initials: C
authors.lastname: Perros-Huguet
authors.forename: David A
authors.initials: DA
authors.lastname: Price
authors.forename: Mike
authors.initials: M
authors.lastname: Trevethick
authors.forename: Rob
authors.initials: R
authors.lastname: Webster
mesh_terms: 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
chemical_list: D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists; D000218:Adamantane