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Chemical Compound Review:

CHEMBL1365 1-[2-(3-amino-2-hydroxy- propoxy)phenyl]-3...

Synonyms: CHEBI:408471, KST-1B9282, AC1L2UHT, AR-1A9982, FT-0665908, ...

Rouet, R. et al., Vozeh, S. et al., Fonck, K. et al., Hemeryck, A. et al.

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High impact information on N-Depropylpropafenone

Propafenone is mainly metabolized by CYP2D6 to form 5-hydroxypropafenone (5-OHP) and to a minor extent by CYP1A2 and CYP3A4 to form N-depropylpropafenone (N-DPP) [1].
The initial concentrations of the metabolite N-depropylpropafenone were surprisingly higher than those of 5-hydroxypropafenone which may also be due to saturation of CYP2D6 [2].
The two active metabolites (5-hydroxypropafenone and N-depropylpropafenone) showed non-linear kinetics in that both the dose-corrected area under the serum concentration-time curve and the amount excreted in the urine were larger after oral dosing [3].
Comparative electrophysiological effects of propafenone, 5-hydroxy-propafenone, and N-depropylpropafenone on guinea pig ventricular muscle fibers [4].
In order to examine whether its two major metabolites [5-hydroxypropafenone (5-OH-Pf) and N-depropylpropafenone (N-DP-Pf)] possess pharmacodynamical properties, we compared their electrophysiological effects to those of the parent drug on papillary muscle fibers from guinea pig ventricular myocardium [4].

References

Effect of selective serotonin reuptake inhibitors on the oxidative metabolism of propafenone: in vitro studies using human liver microsomes. Hemeryck, A., De Vriendt, C., Belpaire, F.M. Journal of clinical psychopharmacology. (2000) [Pubmed]
ECG changes and plasma concentrations of propafenone and its metabolites in a case of severe poisoning. Fonck, K., Haenebalcke, C., Hemeryck, A., Belpaire, F., Jordaens, L., Calle, P., Buylaert, W. J. Toxicol. Clin. Toxicol. (1998) [Pubmed]
Nonlinear kinetics of propafenone metabolites in healthy man. Vozeh, S., Haefeli, W., Ha, H.R., Vlcek, J., Follath, F. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
Comparative electrophysiological effects of propafenone, 5-hydroxy-propafenone, and N-depropylpropafenone on guinea pig ventricular muscle fibers. Rouet, R., Libersa, C.C., Broly, F., Caron, J.F., Adamantidis, M.M., Honore, E., Wajman, A., Dupuis, B.A. J. Cardiovasc. Pharmacol. (1989) [Pubmed]

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