Metabolism of levo-α-acetylmethadol (LAAM) by human liver cytochrome P450: involvement of CYP3A4 characterized by atypical kinetics with two binding sites

Y Oda, ED Kharasch - Journal of Pharmacology and Experimental …, 2001 - ASPET
levo-α-Acetylmethadol (LAAM) is a long-acting opioid agonist prodrug used for preventing
opiate withdrawal. LAAM undergoes bioactivation via sequential N-demethylation to nor-…

Atypical kinetic profiles in drug metabolism reactions

JM Hutzler, TS Tracy - Drug metabolism and disposition, 2002 - ASPET
… This review will highlight some specific examples of atypical kinetics, as well … atypical kinetics
with respect to in vitro-in vivo correlations. In addition, artifactual sources of atypical kinetic

N-Demethylation of levo-α-acetylmethadol by human placental aromatase

SV Deshmukh, TN Nanovskaya, GDV Hankins… - Biochemical …, 2004 - Elsevier
Levo-α-acetylmethadol (LAAM) is a methadone derivative used to treat the opiate addict. We
previously reported on the kinetics … norLAAM exhibited monophasic kinetics with apparent K …

Metabolism of methadone andlevo-α-acetylmethadol (LAAM) by human intestinal cytochrome P450 3A4 (CYP3A4): potential contribution of intestinal metabolism to …

Y Oda, ED Kharasch - Journal of Pharmacology and Experimental …, 2001 - ASPET
… Methadone and levo-α-acetylmethadol (LAAM) are opioid … tolevo-α-acetyl-N-normethadol
(nor-LAAM) andlevo-α-acetyl-N,N… multienzyme kinetics that were similar to the multisite kinetics

Identification of cytochrome P450 enzymes involved in the metabolism of 4′-methoxy-α-pyrrolidinopropiophenone (MOPPP), a designer drug, in human liver …

D Springer, RF Staack, LD Paul, T Kraemer… - Xenobiotica, 2003 - Taylor & Francis
… and KHARASCH, ED, 2001, Metabolism of levo-alpha-Acetylmethadol (LAAM) by human
liver cytochrome P450: involvement of CYP3A4 characterized by atypical kinetics with two …

Identification of cytochrome p450 enzymes involved in the metabolism of 4′-methyl-α-pyrrolidinopropiophenone, a novel scheduled designer drug, in human liver …

D Springer, LD Paul, RF Staack, T Kraemer… - Drug metabolism and …, 2003 - ASPET
… interestingly showed a biphasic kinetic profile with apparent … also revealed biphasic
nonsaturable kinetics with apparent K … Based on kinetic data corrected for the relative activity …

Atypical kinetics of cytochromes P450 catalysing 3′-hydroxylation of flavone from the white-rot fungus Phanerochaete chrysosporium

N Kasai, S Ikushiro, S Hirosue, A Arisawa… - Journal of …, 2010 - academic.oup.com
… , kinetic studies of these P450s showed a sigmoidal behaviour. Atypical kinetics was …
of two molecules of flavone in the active site of PcCYP50c that supports the atypical kinetics. …

Allosteric enzyme-and transporter-based interactions

M Subramanian, TS Tracy - Enzyme-and Transporter-Based Drug-Drug …, 2010 - Springer
levo-α-acetylmethadol, naphthalene, and nor-levo-α-… kinetics are the most common atypical
kinetic profiles observed, a few cases of heteroactivation have been reported. Atypical kinetic

Paradoxical Role of Cytochrome P450 3A in the Bioactivation and Clinical Effects of Levo-α-Acetylmethadol: Importance of Clinical Investigations to Validate In Vitro …

ED Kharasch, D Whittington, C Hoffer, K Krudys… - Clinical …, 2005 - Springer
Objective: Levo-α-acetylmethadol (LAAM, levacetylmethadol) is a long-acting opioid agonist
used for the prevention of opioid withdrawal. LAAM undergoes sequential N-demethylation …

[图书][B] Factors affecting CYP2C9-mediated metabolism

JM Hutzler - 2001 - search.proquest.com
… , and thus are becoming more cognizant of these atypical kinetic events. This is reflected
by the increase in atypical kinetic profiles reported in the literature over the past few years. …