General paperHuman α 7 nicotinic acetylcholine receptor responses to novel ligands
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Alpha7 nicotinic acetylcholine receptors and neural network synaptic transmission in human induced pluripotent stem cell-derived neurons
2019, Stem Cell ResearchCitation Excerpt :PNU-282987 (10 μM) alone had no effect, but the signal strongly increased with co-application of PNU-120596 (Fig. 2E). The α7 antagonist, methyllycaconitine (MLA, 1 μM) (Briggs et al., 1995; Macallan et al., 1988) strongly reduced acetylcholine and nicotine signals, while it abolished the PNU-282987 signal (Fig. 2E). The α4β2 antagonist DhβE (1 μM) did not significantly reduce the signal of acetylcholine and nicotine (Fig. 2E).
Cholinergic modulation of the immune system presents new approaches for treating inflammation
2017, Pharmacology and TherapeuticsSymptomatic thinking: the current state of Phase III and IV clinical trials for cognition in schizophrenia
2017, Drug Discovery TodayCitation Excerpt :The first compound of the class (discounting galantamine which has activity at the receptor) registered for clinical trials: AQW051, went into humans in 2006 (NCT00418002). Moreover, pharmaceutical companies such as Abbott Laboratories were publishing on the target as early as 1995 [20]. In fact, one of the compounds identified in [20]: GTS-21, would eventually go into clinical trials for schizophrenia (NCT01400477), although the outcome of this trial has not been published yet.
A comparative study of the effects of ABT-418 and methylphenidate on spatial memory in an animal model of ADHD
2012, Neuroscience LettersCitation Excerpt :Recently, studies have indicated that the nicotine system plays a role in the pathophysiology of ADHD [12] and that neuronal nicotinic acetylcholine receptor (nAChR) agonists are effective in treating ADHD, particularly in attention/cognitive deficits [2,28,31]. ABT-418, a nAChR agonist, binds with high affinity to the α4β2, α2β2 and α7 receptor subtypes [6,16]. In addition, ABT-418 is used in the treatment of for Alzheimer's disease [17], and more recently for ADHD [25,29].
Creating an α7 nicotinic acetylcholine recognition domain from the acetylcholine-binding protein: Crystallographic and ligand selectivity analyses
2011, Journal of Biological Chemistry