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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

Author(s): J. Paul Hieble

Volume 7 , Issue 2 , 2007

Page: [207 - 216] Pages: 10

DOI: 10.2174/156802607779318208

Price: $65


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.

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

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