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 …
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 …
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 Reed‐Hagen, 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 …
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 …
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
… 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 …
monitoring substrate depletion is equivalent to the traditional product formation approach. Kinetic …
[HTML][HTML] Varenicline for smoking cessation: a review of the literature
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, …
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) …
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 …
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…
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, …
are comparable to those from the conventional metabolite formation method. Furthermore, …