Neuron
ArticleModulation of excitatory synaptic transmission by drugs that reduce desensitization at AMPA/kainate receptors
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2019, Tetrahedron LettersCitation Excerpt :Su and co-workers synthesized benzothiadiazine 1,1-dioxides via reductive cyclization of N,N-diethyl o-nitro benzenesulfonamide with nitriles using SmI2 as a reducing agent [18]. Another method involving condensation of o-halosubstituted benzenesulfonyl chloride with amidines was reported by Lukin et al. [19] In 2015, Laha and co-workers developed potassium persulfate-mediated cyclization of N-aryl benzylamines followed by their oxidation to give benzothiadiazine 1,1-dioxides [20]. Although these methods offer benzothiadiazine 1,1-dioxides in moderate to good yields, they suffer from drawbacks such as use of toxic reagents, stoichiometric quantity of catalysts, low product yields etc.
Correlation of 3-mercaptopropionic acid induced seizures and changes in striatal neurotransmitters monitored by microdialysis
2014, European Journal of Pharmaceutical SciencesCitation Excerpt :If the time in which Glu resides in the synaptic cleft is greater than the time in which the AMPA receptor is open, the receptor may become desensitized (Trussell et al., 1993; Tran et al., 1999; Vyklicky et al., 1991), entering a permanently “closed” state, thereby not allowing the reuptake of Glu into glia. AMPA receptor desensitization can be selectively blocked with CTZ (Trussell et al., 1993; Vyklicky et al., 1991). The use of CTZ to “resensitize” the AMPA receptors was explored in the 3-MPA seizure model in order to try to explain the increase in Glu well past the spontaneous termination of status.
Coupled Control of Desensitization and Gating by the Ligand Binding Domain of Glutamate Receptors
2012, NeuronCitation Excerpt :Schemes with long lived desensitized states connected to open states were previously proposed to describe the activation of native glutamate receptors (Häusser and Roth, 1997; Jonas et al., 1993). However, in other studies, desensitization was taken to proceed only from shut states (Vyklicky et al., 1991; Robert and Howe, 2003) or from either shut or open states (Lin and Stevens, 1994; Raman and Trussell, 1995), and the concept of desensitization from open states has remained controversial (Colquhoun and Hawkes, 1995a). Because connecting these two states forms a reversible loop, changes in the rate d2– must be compensated by changes in another rate constant to ensure microscopic reversibility is obeyed (Colquhoun et al., 2004).
A novel class of allosteric modulators of AMPA/Kainate receptors
2009, Bioorganic and Medicinal Chemistry Letters
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L. V. and D. K. P. contributed equally to this study.