S 18986, a positive modulator of AMPA receptors with cognition-enhancing properties, increases ACh release in the hippocampus of young and aged rat☆
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Acknowledgements
The work was supported by a grant from the Institut de Recherches Internationales Servier.
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Central inspiratory activity rhythmically activates synaptic currents of airway vagal preganglionic neurons in neonatal rats
2019, Neuroscience LettersCitation Excerpt :PIOCs in II-AVPNs could be inhibited coincidentally with the inhibition of hypoglossal inspiratory bursts in vitro, and are thus unlikely to be due to blockade of inhibitory transmission in the respiratory reflex network [30]. In view of the effects of synaptic activation of AMPA receptors on gamma-aminobutyric acid (GABA) neurotransmission [32], it is reasonable to postulate that glycinergic neurons innervating II-AVPNs during inspiratory bursts could be regulated by glutamatergic synaptic inputs from PBC. Thus, the second aim of the current study was to clarify this possibility at the synaptic level.
Design, stereoselective synthesis, configurational stability and biological activity of 7-chloro-9-(furan-3-yl)-2,3,3a,4-tetrahydro-1H-benzo[e]pyrrolo[2,1- c][1,2,4]thiadiazine 5,5-dioxide
2014, Bioorganic and Medicinal ChemistryCitation Excerpt :7-Chloro-9-(furan-3-yl)-2,3,3a,4-tetrahydro-1H-benzo[e]pyrrolo[2,1-c][1,2,4]thiadiazine 5,5-dioxide (3) was designed and synthesized in order to enhance configurational and chemical stability preserving the relevant biological activity (Fig. 1). Recently (S)-2 (S18986) has attracted particular attention since in vivo experiments demonstrated its cognition enhancing properties when it is administered orally at low dose.36–38 Subsequent stereo and chemical evaluation studies have suggested that (S)-2 (S18986) is stable to enantiomerization and hydrolysis.33
The AMPA receptor modulator S18986 in the prelimbic cortex enhances acquisition and retention of an odor-reward association
2013, Neuroscience LettersCitation Excerpt :In addition to their effects on LTP and neurotrophic factors, memory-enhancing effects of AMPA allosteric modulators may lie in their capacity to modulate several neurotransmitter systems. Thus, S18986 enhances acetylcholine in the hippocampus of freely moving rats, noradrenaline in both hippocampal and frontal cortex slices, and dopamine in frontal cortex slices [13,17]. Such neurotransmitter release in the frontal cortex may underlie memory improvement as the activation of closely related brain regions, particularly in the frontal cortex (PLC, infralimbic, orbital) and the amygdala, has been described specifically for ODT [19].
Quantitative analysis of acetylcholine in rat brain microdialysates by liquid chromatography coupled with electrospray ionization tandem mass spectrometry
2010, Journal of Neuroscience MethodsCitation Excerpt :The difference between ACh release in saline and IDRA21 treated rats, calculated as mean percent changes and calculated between 15 and 120 min for each treatment, was statistically significant (P < 0.01) as shown in the inset. These data are in accordance with those previously reported for positive AMPA modulators structurally similar to IDRA21 (Rosi et al., 2004). A LC/MS/MS method has been developed to quantify small levels of Ach in rat brain microdialysates.
Behavioral and biological effects of chronic S18986, a positive AMPA receptor modulator, during aging
2008, Experimental NeurologyS18986: A positive modulator of AMPA-receptors enhances (S)-AMPA-mediated BDNF mRNA and protein expression in rat primary cortical neuronal cultures
2007, European Journal of Pharmacology
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This paper is in honor of Professor Manfred Zimmermann's 70th birthday.
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Present address: Arizona Research Laboratories, Division of Neural Systems, Memory and Aging, University of Arizona, Tucson, AZ 85724, USA.