New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 microM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor. Compounds 4e and 4o appeared to be allosteric enhancers at a low concentration and antagonists at a higher concentration, whereas compounds 3c, 3g, 3s and 4l appeared to be weak antagonists that are also allosteric enhancers at the higher concentration of 10 microM.

Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor

BARALDI, Pier Giovanni;LAMPRONTI, Ilaria;FRUTTAROLO, Francesca;PAVANI, Maria Giovanna;AGHAZADEH TABRIZI, Mojgan;ROMAGNOLI, Romeo
2000

Abstract

New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 microM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor. Compounds 4e and 4o appeared to be allosteric enhancers at a low concentration and antagonists at a higher concentration, whereas compounds 3c, 3g, 3s and 4l appeared to be weak antagonists that are also allosteric enhancers at the higher concentration of 10 microM.
2000
Baraldi, Pier Giovanni; Zaid, A. N.; Lampronti, Ilaria; Fruttarolo, Francesca; Pavani, Maria Giovanna; AGHAZADEH TABRIZI, Mojgan; Shryock, J. C.; Leung, E.; Romagnoli, Romeo
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1685232
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