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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%.

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