Title of article :
Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor
Author/Authors :
Romeo Romagnoli، نويسنده , , Pier Giovanni Baraldi، نويسنده , , Maria Giovanna Pavani، نويسنده , , Mojgan Aghazadeh Tabrizi، نويسنده , , Allan R. Moorman، نويسنده , , Francesco Di Virgilio، نويسنده , , Elena Cattabriga، نويسنده , , Cecilia Pancaldi، نويسنده , , Stefania Gessi، نويسنده , , Pier Andrea Borea، نويسنده ,
Abstract :
The design, synthesis, and preliminary biological evaluation of the first potent radioligand antagonist for the P2X7 receptor, named [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine (compound 13), are reported. This compound bound to human P2X7 receptors expressed in HEK transfected cells with KD and Bmax value of 3.46 ± 0.1 nM and 727 ± 73 fmol/mg of protein, respectively. The high affinity and facile labeling makes it a promising radioligand for a further characterization of P2X7 receptor subtype.
