Ketotifen fumarate demonstrates a broad spectrum of bioactivities, positioning it as a multifaceted compound with potential applications across various biological systems. It significantly inhibits degranulation in anti-DNP IgE sensitized rat RBL2H3 cells by reducing beta-hexosaminidase release after 10 minutes, exhibiting IC50 values of 220,000 nM and 158,000 nM. Additionally, it shows strong inhibitory activity at histamine H1 receptors in ddY mice, reducing histamine-induced skin vascular permeability by 98.0% at 3 mg/kg, and displays anti-inflammatory effects in BALB/c mice by inhibiting ovalbumin-induced ear swelling. Ketotifen fumarate also exhibits substantial antiplasmodial activity against Plasmodium falciparum, with IC50 values ranging from 794.33 nM to 10000.0 nM, and differential potency in various qHTS assays for inhibitors of proliferation of multiple Plasmodium falciparum lines.
In terms of transport proteins, Ketotifen fumarate has high inhibitory activity in OATP1B1 and OATP1B3 transfected CHO cells. It shows antianaphylactic activity, inhibiting antigen-induced histamine release and slow-reacting substance of anaphylaxis in ovalbumin-sensitized guinea pig lung. Furthermore, it displays inhibition activity against SARS-CoV-2 by inhibiting viral-induced cytotoxicity in Vero E6 and Caco-2 cells and inhibiting 3CL-Pro protease by 17.19% at 20 µM concentration.
Antifungal and antibacterial assays reveal limited inhibition against Candida albicans, Cryptococcus neoformans, and various bacterial strains, with percentages ranging from minimal to 11.46%. Additionally, it affects protein domain stability and GPCR beta-arrestin recruitment assays, displaying both inhibitory and stimulating effects on multiple receptors, signifying a complex pharmacological profile.
Overall, Ketotifen fumarate is a compound of significant interest due to its wide-ranging bioactivities, implicating its potential in antiallergic, anti-inflammatory, antiplasmodial, antiviral, and possibly antifungal and antibacterial therapeutics..
Note: Summary generated by AI. Data source: ChEMBL 