INHIBITION OF ADENOSINE KINASE AND ADENOSINE UPTAKE IN GUINEA-PIG CNSTISSUE BY HALOGENATED TUBERCIDIN ANALOGS

Two halogenated analogues of tubercidin (7-deazaadenosine) viz. 5-iodo tubercidin and 5'-deoxy-5-iodotubercidin, previously were shown to be potent inhibitors of guinea-pig brain adenosine kinase activity and ad enosine uptake in guinea-pig cerebral cortex slices. A further series of halogenated tubercidin analogues have been investigated; of the 9 c ompounds tested, 5'-deoxy-5-iodotubericidin was the most potent adenos ine kinase inhibitor while 5-iodotubercidin was the most potent in inh ibiting the facilitated uptake of adenosine. These compounds may be us eful for elucidating the involvement of adenosine kinase in adenosine uptake, the maintenance of intracellular adenosine levels and in the n euromodulatory actions of adenosine in the CNS.