Journal of labelled compounds and radiopharmaceuticals p. 415 - 427 (2004)
Update date:2022-08-30
Topics:
Blum, Till
Ermert, Johannes
Wutz, Walter
Bier, Dirk
Coenen, Heinz H.
The precursor synthesis and the no-carrier-added (n.c.a.) radiosynthesis of the adenosine-A1 receptor ligand 5′-(methyl[ 75Se]seleno)-N6-cyclopentyladenosine ([75Se]1) are described in this report. A method was developed starting from elemental n.c.a. selenium-75, followed by a three-step polymer-supported radioselenation and deprotection which gave the radioligand with a radiochemical yield of 30%, a radiochemical purity of > 99% and a specific radioactivity of > 300 GBq/mmol (8 Ci/mmol). Preparation time was 40 min. The nonradioactive compound 5′-(methylseleno)-N6-cyclopentyladenosine (1) was pharmacologically evaluated in vitro and showed high affinity and selectivity for the adenosine-A1 receptor. These preliminary results suggest that this compound could be a useful radioligand for the noninvasive imaging of the brain adenosine-A1 receptors using positron emission tomography (PET) when labelled with the positron emitter selenium-73 (half-life: 7.1 h). Copyright
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