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.File in questo prodotto:
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