A review. Allosteric modulators of endogenous adenosine represent an alternative to direct acting adenosine agonists and nucleoside uptake blockers. These compds. can selectively enhance the response to adenosine in only those organs or localized areas of a given organ in which prodn. of adenosine is increased. The present article is an overview of the recent patent literature related to allosteric modulators of adenosine function on the A1 receptor. In particular, the compds. with improved potency as enhancers and reduced antagonist properties are mentioned. Among the reported compds., two mols. appear to be of potential therapeutic utility. A synergistic combination of PD-81723 and cyclopentyladenosine, an allosteric enhancer and agonist, resp., of the adenosine A1 receptor, appeared to be effective to induce angiogenesis. Moreover, (2-amino-4,5,6,7-tetrahydro-benzo[b]thiophen-3-yl)-(4-chloro-phenyl)methanone appears to be active for the treatment of neuropathic pain without co-administration of adenosine.
Allosteric modulators for the A1-adenosine receptor
BARALDI, Pier Giovanni;AGHAZADEH TABRIZI, Mojgan;PAVANI, Maria Giovanna;ROMAGNOLI, Romeo
2004
Abstract
A review. Allosteric modulators of endogenous adenosine represent an alternative to direct acting adenosine agonists and nucleoside uptake blockers. These compds. can selectively enhance the response to adenosine in only those organs or localized areas of a given organ in which prodn. of adenosine is increased. The present article is an overview of the recent patent literature related to allosteric modulators of adenosine function on the A1 receptor. In particular, the compds. with improved potency as enhancers and reduced antagonist properties are mentioned. Among the reported compds., two mols. appear to be of potential therapeutic utility. A synergistic combination of PD-81723 and cyclopentyladenosine, an allosteric enhancer and agonist, resp., of the adenosine A1 receptor, appeared to be effective to induce angiogenesis. Moreover, (2-amino-4,5,6,7-tetrahydro-benzo[b]thiophen-3-yl)-(4-chloro-phenyl)methanone appears to be active for the treatment of neuropathic pain without co-administration of adenosine.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
