Synonyms: BHV-4157 | BHV-4157a | BHV4157 | BHV4157a | FC-4157 | trigriluzole
Compound class:
Synthetic organic
Comment: Troriluzole (BHV-4157) is a prodrug of the voltage-dependent calcium channel blocker riluzole. Chemically it is riluzole conjugated to a tripeptide carrier (IUPAC sequence H-Gly-Gly-Sar-Unk, where Unk = the riluzole component), and the active moiety is released by peptidases in vivo. The prodrug is more stable than riluzole and is suitable for once-daily dosing.
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Bioactivity Comments |
Biological activity of troriluzole will likely be associated with the active drug riluzole. The effects of riluzole are principally the result of its ability to reduce synaptic levels of the excitatory neurotransmitter glutamate. Glutamatergic dysfunction is implicated in the pathophysiology of a range of neurodegenerative and neuropsychiatric disorders. Development of troriluzole in such conditions is based on previous evidence obtained with riluzole. |