Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5237-40. doi: 10.1016/j.bmcl.2009.06.104. Epub 2009 Jul 4.

Abstract

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.

MeSH terms

  • Adrenergic beta-1 Receptor Agonists
  • Adrenergic beta-2 Receptor Agonists*
  • Animals
  • Asthma / drug therapy
  • Bronchodilator Agents / chemical synthesis
  • Bronchodilator Agents / chemistry*
  • Bronchodilator Agents / pharmacology
  • Ethanolamines / chemical synthesis
  • Ethanolamines / chemistry*
  • Ethanolamines / pharmacology
  • Guinea Pigs
  • Heart Rate
  • Humans
  • Receptors, Adrenergic, beta-1 / metabolism
  • Receptors, Adrenergic, beta-2 / metabolism

Substances

  • Adrenergic beta-1 Receptor Agonists
  • Adrenergic beta-2 Receptor Agonists
  • Bronchodilator Agents
  • Ethanolamines
  • Receptors, Adrenergic, beta-1
  • Receptors, Adrenergic, beta-2