Characterization of the Adenosine Pharmacology of Ticagrelor Reveals Therapeutically Relevant Inhibition of Equilibrative Nucleoside Transporter 1

Conclusions:
Ticagrelor inhibits cellular adenosine uptake selectively via ENT1 inhibition at concentrations of clinical relevance. However, the low-binding affinity and functional inhibition of adenosine receptors observed with ticagrelor or its metabolites indicate that they possess a negligible adenosine-like activity at clinically relevant concentrations.

Source: Journal of Cardiovascular Pharmacology and Therapeutics - February 17, 2014 Category: Cardiology Authors: Armstrong, D., Summers, C., Ewart, L., Nylander, S., Sidaway, J. E., van Giezen, J. J. J. Tags: Experimental Studies Source Type: research