R7 (drug)

[1][3][2] It is a structural modification and prodrug of tropoflavin (7,8-DHF) with improved potency and pharmacokinetics, namely oral bioavailability and duration.

[1][3] R7 was superseded by R13 because while R7 had a good drug profile in animals, it showed almost no conversion into tropoflavin in human liver microsomes.

[5] Tropoflavin, a naturally occurring flavonoid, was found to act as an agonist of the TrkB with nanomolar affinity (Kd ≈ 320 nM).

[2] Moreover, R7 was found to potently activate the TrkB and the downstream Akt signaling pathway upon oral administration, an action that was tightly correlated with plasma concentrations of tropoflavin.

[2] As such, R7 has shown in vivo efficacy as an agonist of the TrkB, including central activity, similarly to tropoflavin.