货号 | 16335-10mg |
描述 | Receptors for AMPA are ionotropic glutamate receptors with critical roles in neurological development and function.1,2,3 Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 µM).4,5,6 It blocks the rapid agonist-induced desensitization of AMPA receptors, resulting in enhanced excitatory activity.6 Cyclothiazide is also a negative modulator of GABAA receptors, reversibly inhibiting both evoked and spontaneous inhibitory postsynaptic currents (IC50 = 58 µM).7,8 |
别名 | Doburil; |
供应商 | Cayman |
应用文献 | |
1.Gouaux, E. Structure and function of AMPA receptors. Journal of Physiology 554(2), 249-253 (2004). 2.Schoepp, D.D. Unveiling the functions of presynaptic metabotropic glutamate receptors in the central nervous system. Journal of Pharmacology and Experimental Therapeutics 299(1), 12-20 (2001). 3.Scannevin, R.H. and Huganir, R.L. Postsynaptic organization and regulation of excitatory synapses. Nature Reviews.Neuroscience 1, 133-141 (2000). 4.Partin, K.M.,Patneau, D.K.,Winters, C.A., et al. Selective modulation of desensitization at AMPA versus kainate receptors by cyclothiazide and concanavalin A. Neuron 11(6), 1069-1082 (1993). 5.Ornstein, P.L.,Zimmerman, D.M.,Arnold, M.B., et al. Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)-propanoic acid (AMPA) receptors. Journal of Medicinal Chemistry 43(23), 4354-4358 (2000). 6.Bräuner-Osborne, H.,Egebjerg, J.,Nielsen, E.O., et al. Ligands for glutamate receptors: Design and therapeutic prospects. J. Med. Chem. 43(14), 2609-2645 (2000). 7.Deng, L. and Chen, G. Cyclothiazide potently inhibits γ-aminobutyric acid type A receptors in addition to enhancing glutamate responses. Proceedings of the National Academy of Sciences of the United States of America 100(200), 13025-13029 (2003). 8.Johnston, G.A.R.,Chebib, M.,Hanrahan, J.R., et al. Neurochemicals for the investigation of GABAC receptors. Neurochemical Research 35(12), 1970-1977 (2010). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 389.9 |
分子式 | C14H16ClN3O4S2 |
CAS号 | 2259-96-3 |
稳定性 | ≥ 2 years |
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