R13 is a small-molecule flavonoid and orally active, potent, and selective agonist of the tropomyosin receptor kinase B (TrkB) – the main signaling receptor for the neurotrophin brain-derived neurotrophic factor (BDNF) – which is under development for the potential treatment of Alzheimer's disease.[1][2] It is a structural modification and prodrug of tropoflavin (7,8-DHF) with improved potency and pharmacokinetics, namely oral bioavailability and duration.[1] The compound is a replacement for the earlier tropoflavin prodrug R7 and has similar properties to it.[1][3] It was developed because while R7 displayed a good drug profile in animal studies, it showed almost no conversion into tropoflavin in human liver microsomes.[1] In contrast to R7, R13 is readily hydrolyzed into tropoflavin in human liver microsomes.[1]
Clinical data | |
---|---|
Other names | 4-Oxo-2-phenyl-4H-chromene-7,8-diyl bis(methylcarbamate) |
Routes of administration | By mouth[1] |
Pharmacokinetic data | |
Metabolites | Tropoflavin[1] |
Identifiers | |
| |
CAS Number |
|
PubChem CID |
|
UNII |
|
Chemical and physical data | |
Formula | C19H16N2O6 |
Molar mass | 368.345 g·mol−1 |
3D model (JSmol) |
|
| |
|