Metabolism and disposition of varenicline, a selective α4β2 acetylcholine receptor partial agonist, in vivo and in vitro

RS Obach, AE Reed-Hagen, SS Krueger… - Drug metabolism and …, 2006 - ASPET
The metabolism and disposition of varenicline (7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine),
a partial agonist of the nicotinic acetylcholine receptor for the …

Measurement of Michaelis constants for cytochrome P450-mediated biotransformation reactions using a substrate depletion approach

RS Obach, AE Reed-Hagen - Drug Metabolism and Disposition, 2002 - ASPET
The Michaelis constant (K M ) for cytochrome P450-mediated drug biotransformation
reactions can be an important parameter in understanding the potential for a drug to exhibit …

Pharmacokinetics of ezlopitant, a novel non‐peptidic neurokinin‐1 receptor antagonist in preclinical species and metabolite kinetics of the pharmacologically active …

AE ReedHagen, M Tsuchiya… - … & drug disposition, 1999 - Wiley Online Library
The pharmacokinetics of ezlopitant were determined in the rat, gerbil, guinea pig, ferret, dog
and monkey after intravenous and oral administration. In general, ezlopitant is marked by …

Assay of ezlopitant, a substance P receptor antagonist, and metabolites in biological matrices by gas chromatography with mass spectrometric detection: simultaneous …

AE Reed-Hagen, JS Janiszewski, RO Cole… - … of Chromatography B …, 2000 - Elsevier
… Furthermore, we have used it in the analysis of ezlopitant and metabolite concentrations
in animal serum and plasma (Reed-Hagen et al., manuscript in press). Endogenous …

A theoretical validation of the substrate depletion approach to determining kinetic parameters

A Nath, WM Atkins - Drug metabolism and disposition, 2006 - ASPET
… We have shown that Obach and Reed-Hagen's (2002) method of kinetic analysis by
monitoring substrate depletion is equivalent to the traditional product formation approach. Kinetic …

[HTML][HTML] Varenicline for smoking cessation: a review of the literature

K Kaur, S Kaushal, SC Chopra - Current therapeutic research, 2009 - Elsevier
Background: Smoking is the leading preventable risk to human health. Various agents have
been used to promote smoking cessation, but none has had long-term efficacy. Varenicline, …

Explicit reformulations of time-dependent solution for a Michaelis–Menten enzyme reaction model

M Goličnik - Analytical biochemistry, 2010 - Elsevier
The exact closed-form solution to the Michaelis–Menten equation is expressed in terms of
the Lambert W(x) function. However, the utility of this solution is limited because the W(x) …

Application of substrate depletion assay for early prediction of nonlinear pharmacokinetics in drug discovery: assessment of nonlinearity of metoprolol, timolol, and …

H Komura, A Kawase, M Iwaki - Journal of pharmaceutical sciences, 2005 - Elsevier
… Obach and Reed-Hagen developed a substrate depletion assay in which K m values
could be estimated from depletion rate constants of unchanged compounds at various initial …

Human cytochrome P450 kinetic studies on six N-2-methoxybenzyl (NBOMe)-derived new psychoactive substances using the substrate depletion approach

AT Caspar, MR Meyer, HH Maurer - Toxicology Letters, 2018 - Elsevier
A huge number of new chemical derivatives of known drugs of abuse, so-called new psychoactive
substances (NPS), are sold and consumed without prior preclinical and clinical testing…

Pharmacokinetics and metabolism of metoprolol and propranolol in the female DA and female Wistar rat: the female DA rat is not always an animal model for poor …

H Komura, M Iwaki - Journal of pharmaceutical sciences, 2005 - Elsevier
… Obach and Reed-Hagen reported a substrate depletion assay that provides K m values that
are comparable to those from the conventional metabolite formation method. Furthermore, …