IC50: 0.20 μM: inhibits inducible nitric oxide synthases (iNOS).
IC50: 350 μM: blocks endothelial nitric oxide synthases (eNOS).
N-Benzylacetamidine is a potent and selective inhibitor of iNOS compared to eNOS. NOS is essential to the formation of nitric oxide (NO) via the NADPH- and O2-dependent oxidation of L-arginine, which plays a role in regulating many pathological and physiological processes, including smooth muscle relaxation and neurotransmission. INOS contributes to immune response and inflammation while eNOS plays a vital role in regulating vascular tone.
In vitro: N-Benzylacetamidine showed good iNOS and almost negligible eNOS inhibition in THP-1 cells, a human myelomonocytic leukemia cell line .
In vivo: Up to now, in vivo study of N-Benzylacetamidine is still in the development stage.
. Maccallini, C., Patruno, A., Besker, N., Ali, J., Ammazzalorso, A., & De Filippis, B. et al. Synthesis, Biological Evaluation, and Docking Studies of N-Substituted Acetamidines as Selective Inhibitors of Inducible Nitric Oxide Synthase. Journal of Medicinal Chemistry. 2009; 52(5): 1481-1485.