Epilepsy or epileptic syndromes affect more than 70 million people, often comorbid with autism spectrum disorders (ASD). Seizures are concerned as a factor for social regression in ASD. A stepwise experimental approach to this problem requires an animal model to provoke seizures and monitor subsequent behavior.
View Article and Find Full Text PDFBinding densities to dopamine D1-like and D2-like receptors (D1DR and D2DR) were studied in brain regions of animals with genetic generalized audiogenic (AGS) and/or absence (AbS) epilepsy (KM, WAG/Rij-AGS, and WAG/Rij rats, respectively) as compared to non-epileptic Wistar (WS) rats. Convulsive epilepsy (AGS) exerted a major effect on the striatal subregional binding densities for D1DR and D2DR. An increased binding density to D1DR was found in the dorsal striatal subregions of AGS-prone rats.
View Article and Find Full Text PDFResistance to antiepileptic drugs (AEDs) is a major clinical problem. The overexpression of P-glycoprotein (Pgp), one of the main transporters limiting the entry of xenobiotics into the brain, is among the factors contributing to the AED resistance. Presently, there is no consensus on the interaction of carbamazepine (CBZ) with the Pgp.
View Article and Find Full Text PDFBackground: Ifenprodil as a specific antagonist of NMDA receptors containing a dominant NR2B subunit exhibits age-dependent anticonvulsant action. Possible changes of this action due to status epilepticus (SE) elicited at early stage of development were studied using cortical epileptic afterdischarges (ADs) as a model.
Methods: Lithium-pilocarpine SE was induced at postnatal day 12 and effects of ifenprodil were studied 3, 6, 9, and 13 days after SE in rat pups with implanted epidural electrodes.
Poly(lactide-co-glycolide) (PLGA) nanoparticles coated with poloxamer 188 (Pluronic((R)) F-68) or polysorbate 80 (Tween((R)) 80) enable an efficient brain delivery of the drugs after intravenous injection. This ability was evidenced by two different pharmacological test systems employing as model drugs the anti-tumour antibiotic doxorubicin and the agonist of opioid receptors loperamide, which being P-gp substrates can cross the blood-brain barrier (BBB) only in pharmacologically insignificant amounts: binding of doxorubicin to the surfactant-coated PLGA nanoparticles, however, enabled a high anti-tumour effect against an intracranial 101/8 glioblastoma in rats, and the penetration of nanoparticle-bound loperamide into the brain was demonstrated by the induction of central analgesic effects in mice. Both pharmacological tests could demonstrate that therapeutic amounts of the drugs were delivered to the sites of action in the brain and showed the high efficiency of the surfactant-coated PLGA nanoparticles for brain delivery.
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