Synonyms: (-)-1-[2-(4-Amino-2,6-dichloro-anilino)-2-oxo-ethyl]-4-[5,5-bis(4-fluorophenyl)pentyl]piperazine-2-carboxamide; (-)-R 75,231; (-)-R 75231; (-)-R-75231; (-)-R75231; (S)-2-(Aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis(4-fluorophenyl)pentyl]-1-piperazineacetamide; (S)-R 75,231; (S)-R 75231; (S)-R-75231; (S)-R75231; R 88,021; R 88021; R-88021; R88021
Molecular Formula: C30H33Cl2F2N5O2
Molecular Weight: 604.52
Linear Structural Formula: C30H33Cl2F2N5O2
Purity: >=98% (HPLC)
Storage: room temp
Biochem Physiol Actions: 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 muM vs 10 muM with 1 muM respective inhibitor), Draflazine and R75231, but not R88016, show cardioprotective efficacy against catecholamines infusion in rabbits in vivo.