2-Imino-4-methylpiperidine (acetate) is a potent NOS inhibitor [1]
Nitric oxide (NO) is an endogenously produced inorganic free radical gas which has been implicated in endothelium-dependent vascular relaxation, cell-to-cell communication, and cytotoxicity associated with phagocytic cells. NO is synthesized by three isoforms of nitric oxide synthase (NOS): nNOS, eNOS and iNOS [1].
2-Imino-4-methylpiperidine (acetate) is a 2-iminopiperidine class of NOS inhibitor. In the presence of a final L-arginine concentration of 30 μM, 2-Imino-4-methylpiperidine inhibited human iNOS, eNOS, and nNOS with IC50 values of 0.1, 1.1, and 0.2 μM, respectively. 2-Imino-4-methylpiperidine exhibited 9-fold and 1-fold selectivity for iNOS compared to eNOS and nNOS, respectively [1].
In LPS-treated rats, 2-Imino-4-methylpiperidine (10 mg/kg, po) inhibited plasma nitrite levels by 87%.
Reference:
[1]. Webber RK, Metz S, Moore WM, et al. Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms. J Med Chem. 1998 Jan 1;41(1):96-101.