Uses
(S)-Draflazine ((-)-Draflazine) is the (S)-configuration of Draflazine (HY-106841). (S)-Draflazine is a potent blocker of nucleoside transport[1].
Biological Activity
Draflazine (R88021; (-)-R75231)is a potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2). R88021 exhibits 30- and 40-times higher affinity as (+)-R75231 (R88016) using calf lung membrane preparation (by [3H]R75231 & [3H]NBI displacement) and intact human erythrocytes (by [3H]NBMPR displacement)respectively. Draflazine is 20-times more potent as R88016 in enhancing adenosine potency against ADP-induced aggregation in human whole blood (IC50 = 0.5 μM vs 10 μM with 1 μM respective inhibitor)Draflazine and R75231but not R88016show cardioprotective efficacy against catecholamines infusion in rabbits in vivo.
References
[1] M. A. Bruce, et al. Kinetic Resolution of Piperazine-2-Carboxamide by Leucine Aminopeptidase. An Application in the Synthesis of the Nucleoside Transport Blocker (-) Draflazine. An International Journal for Rapid Communication of Synthetic Organic Chemistry Volume 25, 1995 - Issue 17
