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Neuropharmacology of 3,4-Methylenedioxypyrovalerone (MDPV), Its Metabolites, and Related Analogs.
TLDR
Findings in this chapter demonstrate that MDPV and its analogs represent a unique class of transporter inhibitors with a high propensity for abuse and addiction.
Linear pharmacokinetics of 3,4‐methylenedioxypyrovalerone (MDPV) and its metabolites in the rat: relationship to pharmacodynamic effects
TLDR
The results suggest that the parent compound mediates motor stimulation after systemic MDPV administration, but additionally, metabolites may be inhibitory, may not be active or may not pass the blood brain barrier.
The Corticotropin Releasing Hormone-1 (CRH1) Receptor Antagonist Pexacerfont in Alcohol Dependence: A Randomized Controlled Experimental Medicine Study
TLDR
Pexacerfont treatment had no effect on alcohol craving, emotional responses, or anxiety, and there was no effect of pexacerfont on neural responses to alcohol-related or affective stimuli, despite drug levels in CSF that predict close to 90% central CRH1 receptor occupancy.
Determination of illicit and medicinal drugs and their metabolites in oral fluid and preserved oral fluid by liquid chromatography–tandem mass spectrometry
An LC-MS/MS method using 0.5 ml of oral fluid was developed for the determination of morphine, codeine, 6-monoacetylmorphine, methadone, amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine,
4-Methoxy-α-PVP: in silico prediction, metabolic stability, and metabolite identification by human hepatocyte incubation and high-resolution mass spectrometry
TLDR
The most dominant metabolite in HLM and human hepatocyte samples was 4-hydroxy-α-PVP, also predicted as the #1 in silico metabolite, and is suggested to be a suitable analytical target in addition to the parent compound.
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