The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement
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Cited by (8)
1,3,4-Oxadiazoles
2021, Comprehensive Heterocyclic Chemistry IVAlpha7 nicotinic acetylcholine receptor agonists and PAMs as adjunctive treatment in schizophrenia. An experimental study
2016, European NeuropsychopharmacologyCitation Excerpt :Although the NOR test is not without limitations, it has several advantages compared to other cognitive tests and is used extensively in schizophrenia research, both as a model to study cognitive impairments associated with the disease (such as the effect of genetic manipulations of disease associated genes) as well as to investigate the effect of novel pharmacological treatments focusing on cognitive impairments (Lyon et al., 2012; Grayson et al., 2015 and references therein). Indeed, α7 agonists as well as α7 PAMs have been shown to improve performance in tests that involve exploratory behaviour, attention and memory (Boess et al., 2013; Ng et al., 2007; Skidmore et al., 2012), which in turn require active cholinergic input (see Proulx et al. (2014)). Here we show that both NS1738 and PNU282987 enhanced recognition memory, but a higher dose than that used in the CAR test was needed for PNU282987, i.e. 3 mg/kg.
Seven-membered rings
2013, Progress in Heterocyclic ChemistryCitation Excerpt :A quinazolinedione sulfonamide 185, substituted with a 1,4-oxazepine unit at the 6-position, was identified as an orally active competitive AMPA receptor antagonist with significant anticonvulsant activity 〈12BML996〉. A 1,3,4-oxadiazol-2-amine containing a tethered 1,4-oxazepine unit was a potent α7 nicotinic acetylcholine receptor agonist 〈12BML3531〉. An imidazo[1,2-a]pyridine featuring a 7-substituted 1,4-benzoxazepine unit was a weakly active positive allosteric modulator of the metabotropic glutamate 2 receptor 〈12JME2688〉.
Therapeutic targeting of α7 nicotinic acetylcholine receptors
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2016, Molecular Pharmaceutics
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Present address: The University Chemical Laboratory, The University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
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Present address: DDO Limited, Rectory Farm Business Park, Upper Stondon, Bedfordshire SG16 6LJ, UK.
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Present address: GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
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Present address: Neurosciences division, Johnson and Johnson PRF, Turnhoutseweg 30, B2340 Beerse, Belgium.