This work reports the design, synthesis, and preliminary biol. evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine (I), the first potent radioligand antagonist of P2X7 receptor. I, bound to human P2X7 receptors expressed in HEK 293 cells, transfected cells with KD and Bmax values of 3.46 0.1 nM and 727 73 fmol/mg of protein, resp. The high affinity and facile labeling of I make it a promising radioligand for a further characterization of P2X7 receptor subtype.

Synthesis, radiolabeling, and preliminary biological evaluation of [H-3]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl )-piperazine, a potent antagonist radioligand for the P2X(7) receptor

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;AGHAZADEH TABRIZI, Mojgan;DI VIRGILIO F;CATTABRIGA, Elena;PANCALDI, Cecilia;GESSI, Stefania;BOREA, Pier Andrea
2004

Abstract

This work reports the design, synthesis, and preliminary biol. evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine (I), the first potent radioligand antagonist of P2X7 receptor. I, bound to human P2X7 receptors expressed in HEK 293 cells, transfected cells with KD and Bmax values of 3.46 0.1 nM and 727 73 fmol/mg of protein, resp. The high affinity and facile labeling of I make it a promising radioligand for a further characterization of P2X7 receptor subtype.
2004
Romagnoli, Romeo; Baraldi, Pier Giovanni; Pavani, Mg; AGHAZADEH TABRIZI, Mojgan; Moorman, Ar; DI VIRGILIO, F; Cattabriga, Elena; Pancaldi, Cecilia; Ge...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/517051
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