Publications by authors named "Filip A Fedak"
Article Synopsis
- Nicotinamide N-methyltransferase (NNMT) converts nicotinamide into 1-methylnicotinamide using SAM, and its role in health and diseases like cancer, diabetes, and obesity is under investigation as a potential therapeutic target.
- * Recent studies utilized mRNA display screening to identify macrocyclic peptides that effectively bind to NNMT, showing strong inhibitory effects with low IC values (as low as 229 nM).
- * The identified cyclic peptides were found to downregulate MNA production in cells and are unique as they do not compete with existing substrates, suggesting they are the first allosteric inhibitors of NNMT.
Pharmacokinetic study of tianeptine and its active metabolite MC5 in rats following different routes of administration using a novel liquid chromatography tandem mass spectrometry analytical method.
Naunyn Schmiedebergs Arch Pharmacol
February 2018
Tianeptine is an atypical antidepressant with a unique mechanism of action and recently it has been also reported that its major metabolite, compound MC5, possesses pharmacological activity similar to that of the parent drug. The current study aims to investigate the pharmacokinetics (PK) of both tianeptine and MC5 after intravenous or intraperitoneal administration of the parent drug as well as the metabolic ratio of MC5 in rats. To achieve these goals an LC-MS/MS method using the small sample volume for the quantitation of tianeptine and its active metabolite MC5 in rat plasma and liver perfusate has been developed and validated.
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