Penfluridol

Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca²⁺-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml^[1][2][3][4]. In Vitro:Penfluridol (R-16341; 1.25-40 μM; 24, 48 h) reduces cell viability of human AML cells harboring FLT3-WT or the FLT3-ITD mutation^[2].
Penfluridol (7.5 μM; 24 h) results in the apoptosis of AML cells harboring FLT3-WT and FLT3-ITD mutation^[2].
Penfluridol (1.25-7.5 μM; 24 h) induces ROS-mediated autophagy via triggering LC3 turnover and acidic vesicular organelle (AVO) formation^[2].
Penfluridol (1 μM; for 2 h) obviously inhibits TNFα-induced phosphorylation levels of ERK, JNK, and p38^[3].
Penfluridol (1 μM; for 2 h) inhibits TNFα-induced mRNA expressions of IL-1β, IL-6, IL-17, and NOS2^[3].
Penfluridol suppresses the differentiation of spleen naive CD4+T cells to TH1 and TH17 and inhibits M1 macrophage polarization^[3].
In Vivo:Penfluridol (10 mg/kg; daily oral gavage; from the 18th day after the first immunization) significantly reduced severity of collagen-induced arthritis^[3].