Pharmacokinetics and brain uptake study of novel AMPA receptor antagonist perampanel in SD rats using a validated UHPLC-QTOF-MS method

Paul, David; Allakonda, Lingesh; Sahu, Amit Kumar; Surendran, Shruti; Satheeshkumar, N.

doi:10.1016/j.jpba.2017.11.008

Cited by 17 publications

(15 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For example, after administration of the noncompetitive AMPA receptor antagonist LY300164 (talampanel) for levodopa-treated Parkinsonian monkeys lesioned with MPTP, the motor activities were potentiated and LIDs were decreased [23]. In addition, although perampanel, a novel AMPA receptor antagonist, was determined to penetrate the blood–brain barrier, adjunctive Perampanel had no effect on improving LID in PD patients [81,82].…”

Section: Key Targets Of Glutamate Receptors In Pd Treatmentmentioning

confidence: 99%

Roles of Glutamate Receptors in Parkinson’s Disease

Zhang

et al. 2019

IJMS

119

View full text Add to dashboard Cite

Parkinson’s disease is a progressive neurodegenerative disorder resulting from the degeneration of pigmented dopaminergic neurons in the substantia nigra pars compacta. It induces a series of functional modifications in the circuitry of the basal ganglia nuclei and leads to severe motor disturbances. The amino acid glutamate, as an excitatory neurotransmitter, plays a key role in the disruption of normal basal ganglia function regulated through the interaction with its receptor proteins. It has been proven that glutamate receptors participate in the modulation of neuronal excitability, transmitter release, and long-term synaptic plasticity, in addition to being related to the altered neurotransmission in Parkinson’s disease. Therefore, they are considered new targets for improving the therapeutic strategies used to treat Parkinson’s disease. In this review, we discuss the biological characteristics of these receptors and demonstrate the receptor-mediated neuroprotection in Parkinson’s disease. Pharmacological manipulation of these receptors during anti-Parkinsonian processes in both experimental studies and clinical trials are also summarized.

show abstract

Section: Key Targets Of Glutamate Receptors In Pd Treatmentmentioning

confidence: 99%

Roles of Glutamate Receptors in Parkinson’s Disease

Zhang

et al. 2019

IJMS

119

View full text Add to dashboard Cite

show abstract

“…Based on the high PER and STP hydrophobicity, given by their octanol-water partition coefficients (log P) of 3.70 [49] and 3.53 [47] respectively, a high percentage of organic modifier was expected to be required to achieve acceptable retention times. So, bearing in mind this characteristic and also considering the different studies already published for PER [13] and STP [14][15][16][17] quantification in different rodent matrices, acetonitrile was initially tested in a percentage of 40%. However, with this condition, the obtained retention times of both antiepileptics and IS were not acceptable, having a need to slowly increase the percentage of acetonitrile until the best conditions regarding retention times and selectivity were achieved.…”

Section: Optimization Of Chromatographic Conditionsmentioning

confidence: 99%

“…Acetonitrile is one of the most frequently water-miscible organic solvent used in SALLE techniques [13,[24][25][26] and also the organic solvent with a polarity index more close to that of water (5.8 and 10.2, respectively) [48]. Therefore, acetonitrile was initially chosen for testing the effect of different inorganic salts for IS, PER, and STP extraction to the organic phase.…”

Section: Investigation Of Different Organic Solvents and Salting-out mentioning

confidence: 99%

“…In this context, accurate bioanalytical methods are required to quantify PER and STP in rodents' matrices, even as single entities or simultaneously, being the availability of these methods, up to day, very scarce. Specifically for rodents, as far as we know, only Paul et al [13] developed a UHPLC-Q-TOF-MS method for PER quantification in rat plasma and brain. For STP, there are some methods coupled with ultraviolet or fluorescence detection that quantify this drug in rodents and monkey matrices [14][15][16][17][18][19].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Salting‐out assisted liquid–liquid extraction method optimized by design of experiments for the simultaneous high‐performance liquid chromatography analysis of perampanel and stiripentol in mouse matrices

Meirinho

Campos

Rodrigues

et al. 2020

J of Separation Science

View full text Add to dashboard Cite

We report a high-performance liquid chromatography method development able to simultaneously determine perampanel and stiripentol, two third-generation antiepileptics whose therapeutic spectrum can potentially be extended, in several mouse matrices. A salting-out assisted liquid-liquid extraction optimized by a design of experiments approach was adopted for sample preparations. Isopropanol and magnesium sulfate were the extraction solvent and salting-out agent, respectively. Both drugs and internal standard (terbinafine) were separated using a LiChroCART R Purospher Star column (C 18 , 55 × 4 mm; 3 μm) isocratically pumped with mobile phase [1% triethylamine in water (pH 2.5) and acetonitrile (53:47, v/v)] at 1 mL/min. Stiripentol and terbinafine were detected by fluorescence at 254/372 nm and perampanel at 275/430 nm. Good linearity was demonstrated for perampanel at 1-500 ng/mL range in brain, 2-2000 ng/mL in liver and 1-2000 ng/mL in plasma and kidney (r 2 ≥ 0.9922), and for stiripentol between 10 and 2000 ng/mL in brain and 10 and 20 000 ng/mL in the remaining matrices (r 2 ≥ 0.9917). Precision (CV ≤ 15%) and accuracy (bias ±15%) were also verified, with obtained recovery values consistent with those predicted by the experimental design. This method was applied in preliminary pharmacokinetic studies to quantify perampanel or stiripentol after oral administration to mice, showing to be a promising bioanalytical tool to support future nonclinical in vivo pharmacokinetic studies.

show abstract

“…After vortexing for 1 min, the tubes were centrifuged at 9168g (4°C, 5 min). The supernatant was collected and 1 μL was injected into the LC-MS system for analysis (Paul, Allakonda, & Satheeshkumar, 2017;Paul, Allakonda, Sahu, Surendran, & Satheeshkumar, 2018).…”

Section: Sample Preparationmentioning

confidence: 99%

An assessment of the impact of green tea extract on palbociclib pharmacokinetics using a validated UHPLC–QTOF–MS method

Paul

Surendran

Chandrakala

et al. 2019

Biomedical Chromatography

Self Cite

View full text Add to dashboard Cite

Green tea extracts (GTE) has been reported to be a kinase inhibitor and modulator for various drug metabolizing enzymes. It may give synergetic antioncogenic effect, but with a possibility of pharmacokinetic interactions with various co‐administered anticancer agents like palbociclib (PAL), a selective inhibitor of CDK‐4/6 primarily metabolized by CYP3A enzyme. To explore the impact of GTE on PAL pharmacokinetics in Sprague–Dawley rats, a rapid and sensitive UHPLC–QTOF–MS method was established. Chromatographic separation was carried out on an Acquity UPLC BEH C18 (100 × 2.1 mm, 1.7 μm) column using a gradient mobile phase system consisting of 0.1% formic acid and acetonitrile. Sample preparation was based on a simple protein precipitation method. Estimation of target ions [M + H]+ at m/z 448.2455 for PAL and m/z 441.2044 for ibrutinib (IS) was performed in selective ion mode ESI–HRMS. Good sensitivity (1.0 ng/mL) and linearity over a wide concentration range of 1–2000 ng/mL was exhibited by the method. The results indicated that the administration of GTE resulted in decreased oral bioavailability of PAL in both short‐ and long‐term conditions. However, when both conditions were compared, the variation was less for the peak concentration and area under the concentration–time curve level of PAL.

show abstract

Pharmacokinetics and brain uptake study of novel AMPA receptor antagonist perampanel in SD rats using a validated UHPLC-QTOF-MS method

Cited by 17 publications

References 22 publications

Roles of Glutamate Receptors in Parkinson’s Disease

Roles of Glutamate Receptors in Parkinson’s Disease

Salting‐out assisted liquid–liquid extraction method optimized by design of experiments for the simultaneous high‐performance liquid chromatography analysis of perampanel and stiripentol in mouse matrices

An assessment of the impact of green tea extract on palbociclib pharmacokinetics using a validated UHPLC–QTOF–MS method

Contact Info

Product

Resources

About