Corrigendum to “Antiabsence effects of carbenoxolone in two genetic animal models of absence epilepsy (WAG/Rij rats and lh/lh mice)”
Corrigendum to ‘‘Antiabsence effects of carbenoxolone in two genetic animal models of absence epilepsy (WAG/Rij rats and lh/lh mice)’’ Pietro Gareri , Daniele Condorelli , Natale Belluardo , Rita Citraro , Vincenza Barresi , Angela Trovato-Salinaro , Giuseppa Mudo‘ , Guido Ferreri Ibbadu , Emilio Russo , Giovambattista De Sarro a,* a Section of Pharmacology, Department of Experimental and Clinical Medicine, Faculty of Medicine and Surgery, University of Catanzaro, Catanzaro, Italy b Section of Biochemistry and Molecular Biology, Department of Chemical Sciences, University of Catania, Catania, Italy Department of Experimental Medicine, University of Palermo, Palermo, Italy
Novel Potent Anticonvulsant Agent Containing a Tetrahydroisoquinoline Skeleton
In our studies on the development of new anticonvulsants, we planned the synthesis of N-substituted 1,2,3,4-tetrahydroisoquinolines to explore the structure-activity relationships. All derivatives were evaluated against audiogenic seizures in DBA/2 mice, and the 1-(4'-bromophenyl)-6,7-dimethoxy-2-(piperidin-1-ylacetyl) derivative (26) showed the highest activity with a potency comparable to that of talampanel, the only noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist in clinical trials as an anticonvulsant agent. Electrophysiological experiments indicated that 26 acts as noncompetitive AMPA receptor modulator.
Synthesis, resolution, stereochemistry, and molecular modeling of (R)- and (S)-2-acetyl-1-(4’-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline AMPAR antagonists
Abstract Recently we identified ( R , S )-2-acetyl-1-(4′-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline ( 6 ) as a potent non-competitive AMPA receptor antagonist able to prevent epileptic seizures. We report here the optimized synthesis of compound 6 , its resolution by chiral preparative HPLC, and the absolute configuration of ( R )-enantiomer established by X-ray diffractometry. The biological tests of the single enantiomers revealed that higher anticonvulsant and antagonistic effects reside in ( R )-enantiomer as also suggested by molecular modeling studies.
Corrigendum to “Anticonvulsant effects of carbenoxolone in genetically epilepsy prone rats (GEPRs)”[Neuropharmacology 47 (2004) 1205-1216]
Lacosamide in patients with temporal lobe epilepsy: An observational multicentric open-label study.
Abstract Purpose The aim of this study was to evaluate the efficacy and tolerability of lacosamide (LCM) both as add-on therapy and monotherapy in patients with temporal lobe epilepsy (TLE) based on an observational, prospective, multicenter study. Methods We enrolled 100 patients (mean age: 43.4 ± 12.53 years, 57 females) with nonlesional TLE and TLE with hippocampal sclerosis (HS) that did not respond to the first drug and who were referred to epilepsy centers of the University of Catanzaro, University of Palermo, IRCSS Neuromed of Pozzilli, and Otto-von-Guericke University of Magdeburg. In this open-label, multicenter trial, patients were initiated on oral LCM as add-on therapy to first …
The Mental Health of Caregivers and Their Patients With Dementia During the COVID-19 Pandemic: A Systematic Review
Background: Coronavirus Disease 2019 (COVID-19) is a worldwide public health concern. It continues to spread rapidly throughout the world causing multiple physical and psychological consequences in the population. Especially, people affected by severe psychiatric or neurological diseases are highly susceptible to serious health complications not only due to the direct effect of the infection but also to the indirect effect of COVID-19 following social distancing during lockdowns and its general social consequences. Indeed, lockdown and difficulties in using the care services produced psychological consequences in caregivers such as depression, anxiety, and worsening of the quality of life w…
Anticonvulsant effects of carbenoxolone in genetically epilepsy prone rats (GEPRs).
Carbenoxolone (CBX), the succinyl ester of glycyrrhetinic acid, is an inhibitor of gap junctional intercellular communication. Systemic administration of CBX was able to decrease the seizure severity score and to increase the latency time of seizure onset in genetically epilepsy prone rats (GEPRs). In particular, intravenous or intraperitoneal administration of carbenoxolone (5-30 mg/kg) produced a dose-dependent and significant reduction in the clonic and tonic phases of the audiogenic seizures in GEPRs. The anticonvulsant doses were not associated with an impairment of motor coordination. The bilateral microinjection of CBX (0.001-0.50 microg/0.5 microl) into the inferior colliculi, the s…