Flupirtine
A nonopioid analgesic.
General information
Flupirtine is a pyridine derivate used as a non-opioid analgesic. It is active, for example, as a potassium channel activator and NMDA receptor antagonist (DrugBank). The compound acted as a TMPRSS2 inhibitor in an enzyme assay and suppressed TMPRSS-dependent SARS-CoV-2 Spike-pseudotyped virus infection in vitro (Chen et al., 2021).
Flupirtine on PubChem
Flupirtine on Wikipedia
Marketed as
AWEGAL; EFFIRMA; EFIRET; KATADOLON; METANOR; TRANCOLONG
CCOC(=O)NC1=C(N=C(C=C1)NCC2=CC=C(C=C2)F)N
Supporting references
Link | Tested on | Impact factor | Notes | Publication date |
---|---|---|---|---|
Screening strategy of TMPRSS2 inhibitors by FRET-based enzymatic activity for TMPRSS2-based cancer and COVID-19 treatment
TMPRSS2 Small molecule Enzyme assay In vitro Mechanism |
in vitro enzyme assay; Vero E6 cells; Vero E6 cells overexpressing TMPRSS2 | 5.18 | The compound acted as a TMPRSS2 inhibitor in an enzyme assay. It also blocked the infection in standard Vero cells, but the efficacy was significantly higher in TMPRSS2-overexpressing cells. |
Mar/01/2021 |