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Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration.
Eskildsen J, Redrobe JP, Sams AG, Dekermendjian K, Laursen M, Boll JB, Papke RL, Bundgaard C, Frederiksen K, Bastlund JF. Eskildsen J, et al. Among authors: laursen m. Bioorg Med Chem Lett. 2014 Jan 1;24(1):288-93. doi: 10.1016/j.bmcl.2013.11.022. Epub 2013 Nov 20. Bioorg Med Chem Lett. 2014. PMID: 24291041
A small molecule activator of Nav 1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo.
Frederiksen K, Lu D, Yang J, Jensen HS, Bastlund JF, Larsen PH, Liu H, Crestey F, Dekermendjian K, Badolo L, Laursen M, Hougaard C, Yang C, Svenstrup N, Grunnet M. Frederiksen K, et al. Among authors: laursen m. Eur J Neurosci. 2017 Aug;46(3):1887-1896. doi: 10.1111/ejn.13626. Epub 2017 Jul 20. Eur J Neurosci. 2017. PMID: 28635024
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