Naphazoline hydrochloride exhibits strong adrenergic activity with an EC50 of 12.0 nM against the Alpha-1 adrenergic receptor in rat aorta and an IC50 of 0.0011 nM against the Alpha-2 adrenergic receptor in human platelets. It shows potency ratios of 25.8 for Alpha-1 and 3.0 for Alpha-2 compared to medetomidine, indicating its high specificity and efficacy for these receptors. Additionally, it has antiplasmodial activity against Plasmodium falciparum strains GB4 and W2 with an IC50 of 10000.0 nM after 72 hours.
Naphazoline hydrochloride demonstrates various bioactivities, including inhibition of the ERK signaling pathway stimulated by EGF, induction of DNA re-replication in SW480 colon adenocarcinoma cells, and potential effects on hTAAR1 as both an agonist and desensitizer. It shows inhibition of USP1/UAF1 and MBNL1-poly(CUG) RNA binding, suggesting implications in cancer cell proliferation, signaling pathways, and molecular interactions.
The compound also inhibits sodium fluorescein uptake in OATP1B1- and OATP1B3-transfected CHO cells, with inhibition levels of 100.66% and 95.85%, respectively, at 10 uM concentration. However, it shows minimal activity in inhibiting cell viability in Vero E6 cells infected with SARS-CoV-2, with an inhibition index of 0.01362, while demonstrating a 5.6% inhibition rate against SARS-CoV-2 induced cytotoxicity in Caco-2 cells at 10 uM after 48 hours.
Moreover, Naphazoline hydrochloride exhibits a 27.49% inhibition on SARS-CoV-2 3CL-Pro protease activity at a concentration of 20µM. It shows some antifungal activity against Candida albicans and Cryptococcus neoformans with inhibitions of 3.38% and -4.12%, respectively. The compound also demonstrates antibacterial activities against various bacteria, including Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus MRSA with inhibitions of 2.28%, 13.63%, 21.25%, 22.4%, and 21.19%, respectively..
Note: Summary generated by AI. Data source: ChEMBL 