Ligands and therapeutic perspectives of adenosine A(2A) receptors

• Type: Article in International Scientific Journal
• Date: 2008

Authors

Diniz, C (Author) FFUP; Borges, F (Author) FFUP; Santana, L (Author) Other; Uriarte, E (Author) Other; Oliveira, JMA (Author) FFUP; Goncalves, J (Author) FFUP; Fresco, P (Author) FFUP

Journal

Title: Current Pharmaceutical Design

Vol. 14

Pages: 1698-1722

ISSN: 1381-6128

Publisher: Bentham Science

Indexing

ISI Proceedings

ISI Web of Knowledge - 20 Citations

Scopus - 20 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-003-YQ1

DOI: 10.2174/138161208784746842

Abstract (EN): Adenosine A(2A) receptors are members of the G protein-coupled receptor family and mediate multiple physiological effects of adenosine, both at the central nervous system (CNS) and at peripheral tissues, by activating several pathways or interacting with other receptors or proteins. Increasing evidence relate A(2A) receptors with pharmacological stress testing, neurodegenerative disorders (such as Parkinson's disease) and inflammation, renewing the interest in these receptors, increasingly viewed as promising therapeutic targets. Series of agonists and antagonists have been developed by medicinal chemistry artwork either by structure activity relationship (SAR) or quantitative structure activity relationship (QSAR) studies. These studies have allowed identification of the structural and electrostatic requirements for high affinity A(2A) receptor binding and, therefore, contributing to the rational design of A(2A) receptor ligands. Additional rational chemical modifications of the existing A(2A) receptor ligands may further improve their affinity/selectivity. The purpose of this review is to analize and summarize aspects related to the medicinal chemistry of A(2A) receptor ligands, their present and potencial therapeutic applications by exploring the molecular structure and physiological and pathophysiological roles of A(2A) receptors.

Language: English

Type (Professor's evaluation): Scientific