ChemInform Abstract: Analysis of Deprenyl Metabolites in the Rat Brain Using HPLC‐ES‐MS

Kalász, Huba; Bartók, Tibor; Komoroczy, R.; Szoeko, E.; Haberle, D.; Kiss, Judit; Hennings, E. C. P.; Magyar, K.; Fuerst, S.

doi:10.1002/chin.199929327

Cited by 5 publications

(5 citation statements)

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“…The concentration then dropped rapidly in the brain, while increased in the parenchymal tissues [43]. The main metabolites: methamphetamine (MA) and amphetamine (A) were identified in the brain of the animals after intraperitoneal [62] and subcutaneous [34,58] administration of R-deprenyl. These metabolites were also detected post mortem in various brain regions of treated parkinsonian patients [66].…”

Section: Pharmacokinetic Characteristics Of R-deprenylmentioning

confidence: 99%

R-Deprenyl: Pharmacological Spectrum of its Activity

et al. 2010

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Deprenyl has been discovered by Knoll and co-workers. The R-enantiomer of deprenyl (selegiline) is a selective and irreversible inhibitor of the B-isoform of monoamine oxidase (MAO-B) enzyme. Due to its dopamine potentiating and possible neuroprotective properties it has an established role in the treatment of parkinsonian patients. By inhibiting MAO-B enzyme, R-deprenyl decreases the formation of hydrogen peroxide, alleviating the oxidative stress also reduced by increased expression of antioxidant enzymes (superoxide dismutases and catalase) reported during chronic treatment. It was shown to prevent the detrimental effects of neurotoxins like MPTP and DSP-4. R-Deprenyl elicits neuroprotective and neuronal rescue activities in concentrations too low to inhibit MAO-B. It is extensively metabolized and some of the metabolites possess pharmacological activities, thus their contribution to neuroprotective properties was also suggested. The recently identified deprenyl-N-oxide is extensively studied in our laboratory. Effects other than neuroprotection, like influencing cell adhesion and proliferation cannot be neglected.

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Section: Pharmacokinetic Characteristics Of R-deprenylmentioning

confidence: 99%

R-Deprenyl: Pharmacological Spectrum of its Activity

et al. 2010

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“…The concentrations of the administered drug and that of its most important active metabolites were determined in the most relevant brain areas, e.g. in the corpus striatum and frontal cortex (Kalász et al, 1999). Penetration of trimedoxime, K027 and K074 into the rat brain (whole brain) followed and partition of these compounds among some brain areas such as the basal ganglia, frontal cortex and pontomedullary area was determined (Karasova et al, 2011(Karasova et al, , 2013.…”

Section: In Vivo Methodsmentioning

confidence: 99%

Mini review on blood–brain barrier penetration of pyridinium aldoximes

Kalász

Nurulain

Veress³

et al. 2014

J of Applied Toxicology

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This paper reviews the blood-brain barrier (BBB) penetration of newly developed pyridinium aldoximes. Pyridinium aldoximes are highly charged hydrophilic compounds used in the treatment of subjects exposed to organophosphonates because they are effective as acetylcholinesterase reactivators. Pyridinium aldoximes have antidotal effects against poisoning with cholinesterase inhibitors, a frequent problem affecting people working with organophosphate-based insecticides and pesticides. Toxic organophosphonate products such as sarin and tabun can be used by terrorists as chemical warfare agents. This poses a severe challenge to all innocent and peace-loving people worldwide. This review gives a brief summary of BBB transporters and description of the current in vitro and in vivo methods for the characterization of BBB penetration of established and novel pyridinium aldoximes. The authors provide a putative mechanism of penetration, outline some future ways of formulation and discuss the possible advantages and disadvantages of increasing BBB penetration.

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“…L-Deprenyl and its major metabolites (L-nordeprenyl, L-methamphetamine, and L-amphetamine) can be determined in serum and urine using various separation methods, such as gas chromatography (GC) [4,5], gas chromatography-mass spectrometry (GC-MS) [6,7], high-performance liquid chromatography (HPLC) [8,9], HPLC-MS [10][11][12], and capillary electrophoresis [13,14]. Specificity for the parent compound is given by the use of selected ion monitoring of either GC-MS or HPLC-MS.…”

Section: Introductionmentioning

confidence: 99%

HPLC analysis and detection ofl-deprenyl

Csomor¹,

Laufer²,

Pöstényi³

et al. 2014

Acta Chromatographica

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Summary. L-Deprenyl and its major metabolites were subjected to reversed-phase highperformance liquid chromatography (HPLC). The separation was monitored using both ultraviolet (UV) and electrochemical detectors. Ultraviolet absorbance detected L-deprenyl, L-nordeprenyl, L-methamphetamine, and L-amphetamine. Amperometric detection was specific and sensitive to the parent compound (L-deprenyl, a tertiary amine) only. Peaks of the major L-deprenyl metabolites did not give any comparable signal using amperometric monitoring.

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ChemInform Abstract: Analysis of Deprenyl Metabolites in the Rat Brain Using HPLC‐ES‐MS

Cited by 5 publications

References 1 publication

R-Deprenyl: Pharmacological Spectrum of its Activity

R-Deprenyl: Pharmacological Spectrum of its Activity

Mini review on blood–brain barrier penetration of pyridinium aldoximes

HPLC analysis and detection ofl-deprenyl

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