Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action.
Beta2-adrenoceptor agonists with basic and acidic groups attached via an alkyl linker to the phenyl ethanolamine core were prepared and investigated in vitro and in vivo. The compounds exhibited a high potency in a functional cellular assay and a bronchoprotective effect in a guinea pig model which lasted over the complete study period of 5h.
Bouyssou
Thierry
T
Department of Pulmonary Diseases Research, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach, Germany.
Rudolf
Klaus
K
Hoenke
Christoph
C
Lustenberger
Philipp
P
Schnapp
Andreas
A
Konetzki
Ingo
I
D058665:Adrenergic beta-1 Receptor Agonists; D058666:Adrenergic beta-2 Receptor Agonists; D000818:Animals; D001249:Asthma / Q000188:drug therapy; D001993:Bronchodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004983:Ethanolamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006168:Guinea Pigs; D006339:Heart Rate; D006801:Humans; D018342:Receptors, Adrenergic, beta-1 / Q000378:metabolism; D018343:Receptors, Adrenergic, beta-2 / Q000378:metabolism
D058665:Adrenergic beta-1 Receptor Agonists; D058666:Adrenergic beta-2 Receptor Agonists; D001993:Bronchodilator Agents; D004983:Ethanolamines; D018342:Receptors, Adrenergic, beta-1; D018343:Receptors, Adrenergic, beta-2