High‐Grade Nucleoside Transport Inhibition Stimulates Ventilation in Humans

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Abstract
In 6 healthy male volunteers a placebo‐controlled, double‐blind, randomized, crossover trial was done to assess the effect of 1, 2, 4, and 6 mg of draflazine, a specific nucleoside transport inhibitor, on ventilation. Draflazine increased thoracic excursions dose‐dependently by maximally (median with 95% confidence interval) 114.0% (38.3–184.8%) without affecting breathing rate. Ex vivo adenosine transport was inhibited by 0% (0–1%) after placebo, and 70% (59–74%), 81% (76–85%), 90% (86–93%), and 93% (90–96%) after the 4 increasing draflazine dosages, respectively (P < .05 for each draflazine dosage versus placebo). These results indicate that endogenously released adenosine may play a role in the regulation of ventilation.

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