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Pharmacological Profile of the Novel Antiepileptic Drug Candidate Padsevonil: Interactions with Synaptic Vesicle 2 Proteins and the GABAA Receptor.
Wood M, Daniels V, Provins L, Wolff C, Kaminski RM, Gillard M. Wood M, et al. J Pharmacol Exp Ther. 2020 Jan;372(1):1-10. doi: 10.1124/jpet.119.261149. Epub 2019 Oct 16. J Pharmacol Exp Ther. 2020. PMID: 31619465
In addition, its binding was not potentiated by the allosteric modulator UCB1244283. At recombinant GABA(A) receptors, padsevonil displayed low to moderate affinity (pIC(50)6.1) for the benzodiazepine site, and in electrophysiological studies, its relative efficacy compare …
In addition, its binding was not potentiated by the allosteric modulator UCB1244283. At recombinant GABA(A) receptors, padsevonil dis …
Evidence for a differential interaction of brivaracetam and levetiracetam with the synaptic vesicle 2A protein.
Wood MD, Gillard M. Wood MD, et al. Epilepsia. 2017 Feb;58(2):255-262. doi: 10.1111/epi.13638. Epub 2016 Dec 24. Epilepsia. 2017. PMID: 28012162 Free article.
In this study, we used a recently identified SV2A allosteric modulator, UCB1244283, that appears to induce conformational changes in SV2A, to probe the binding properties of labeled BRV and LEV. ...
In this study, we used a recently identified SV2A allosteric modulator, UCB1244283, that appears to induce conformational changes in …
Modulation of the conformational state of the SV2A protein by an allosteric mechanism as evidenced by ligand binding assays.
Daniels V, Wood M, Leclercq K, Kaminski RM, Gillard M. Daniels V, et al. Br J Pharmacol. 2013 Jul;169(5):1091-101. doi: 10.1111/bph.12192. Br J Pharmacol. 2013. PMID: 23530581 Free PMC article.
UCB1244283 significantly slowed down both the association and dissociation kinetics of [(3)H]UCB30889. Following i.c.v. administration in sound-sensitive mice, UCB1244283 showed a clear protective effect against both tonic and clonic convulsions. ...
UCB1244283 significantly slowed down both the association and dissociation kinetics of [(3)H]UCB30889. Following i.c.v. administratio …