Recent Advances in Identification and Characterization of β-Adrenoceptor Agonists and Antagonists

Title: Recent Advances in Identification and Characterization of β-Adrenoceptor Agonists and Antagonists

Volume: 7 Issue: 2

Author(s): J. Paul Hieble

Affiliation:

Keywords: Phenylethanolamine, phenoxypropanolamine, D2 receptor, phosphodiesterase, calcium channel

Abstract: The three β-adrenoceptor subtypes (β1, β2, β3) represent important therapeutic targets. The use of β2- adrenoceptor agonists as bronchodilators and β1 or β1/β2 antagonists as antihypertensives is well established; research is ongoing in these areas to refine pharmacodynamic properties. It is also feasible to design molecules combining β-adrenoceptor affinity with other pharmacophores. This is facilitated by the ability to confer β- adrenoceptor antagonist activity via attachment of a phenylethanolamine moiety or to incorporate diverse structural elements in the N-alkyl substituent of a β-adrenoceptor agonist or antagonist. β3-Adrenoceptor agonists have not yet been successfully developed as drugs for any therapeutic indication; nevertheless, during the past few years many highly potent and selective β3-agonists have been reported, some with good oral bioavailability. Selective β3-adrenoceptor antagonists have also been identified; useful pharmacological tools are now available for the evaluation of the functional role of each β-adrenoceptor subtype.

Cite this article as:

Hieble J. Paul, Recent Advances in Identification and Characterization of β-Adrenoceptor Agonists and Antagonists, Current Topics in Medicinal Chemistry 2007; 7 (2) . https://dx.doi.org/10.2174/156802607779318208