Evaluation of radioiodinated 8-Cyclopentyl-3-[(E)-3-iodoprop-2-en-1-yl]-1-propylxanthine (cas 104285-82-7) ([*I]CPIPX) as a new potential A1 adenosine receptor antagonist for SPECT

Add time:08/04/2019    Source:sciencedirect.com

8-Cyclopentyl-3-[(E)-3-[131I]iodoprop-2-en-1-yl]-1-propylxanthine (2*) was generated by iododestannylation of the tributyl-stannyl-precursor with [131I]NaI and chloramine T. The radiochemical yield of 2* was 82 ± 4%, and the purity exceeded 98%. The specific activity was 33 ± 19 GBq/μmol. Affinities for rat, pig and human A1 adenosine receptors (A1ARs) were in the low nanomolar range, but poor selectivity for the human A1AR over the A2AAR was found. Additionally, in vitro and ex vivo autoradiographic studies revealed high unspecific binding which makes this ligand unsuitable for SPECT imaging.

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