TABLE 3

Ki values for inhibition of uridine transport into TLCT1 and ARAC/D2 stable transfectants by analogs of adenine and adenosine

IC50 values were determined from concentration-effect relationships of Figs. 4 and 5 or from similar experiments (data not shown) as described in Table 1.

TLCT1 (hCNT1) ARAC/D2 (hCNT2)
Test Compounds IC50Ki IC50Ki
μM μM
Adenosine 49 39 30 25
2′-Deoxyadenosine 57 44 35 29
5′-Deoxyadenosine 88 68 288 237
2′-3′-Dideoxyadenosine >500a >386 >500a >411
l-Adenosine >250 >193 >300 >246
2-Chloroadenosine 131 101 45 37
8-Chloroadenosine >300 >232 >300 >246
N6-(p-Aminobenzyl)adenosine 36 28 43 35
Caffeine 59 46 125 103
Nicotine 81 63 276 227
  • a No inhibition observed at 500 μM.