货号 | 16266-500ug |
描述 | NMDA receptors are neuroreceptors that have binding sites for glycine or D-serine as well as L-glutamate.1 MDL 29951 is an antagonist of NMDA receptors with high affinity for the glycine binding site (Ki = 140 nM).2 It is functional both in vitroandin vivo.2 MDL 29951 blocks NMDA receptor-dependent convulsions in audiogenic seizure-susceptible DBA/2J mice.2 It is used to evaluate the role of the glycine site of the NMDA receptor in neurological signaling.3,4 MDL 29951 is also an agonist of the G protein-coupled receptor GPR17 (EC50 values range from 7 nM to 6 µM, depending on the assay).5 GPR17 is thought to be involved in oligodendrocyte differentiation and myelin formation/repair.5 |
供应商 | Cayman |
应用文献 | |
1.Karakas, E. and Furukawa, H. Crystal structure of a heterotetrameric NMDA receptor ion channel. Science 344(6187), 992-997 (2014). 2.Baron, B.M.,Harrison, B.L.,McDonald, I.A., et al. Potent indole- and quinoline-containing N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site. Journal of Pharmacology and Experimental Therapeutics 262, 947-956 (1992). 3.Millan, M.J. and Seguin, L. Chemically-diverse ligands at the glycine B site coupled to N-methyl-D-aspartate (NMDA) receptors selectively block the late phase of formalin-induced pain in mice. Neuroscience Letters 178, 139-143 (1994). 4.Heppenstall, P.A. and Fleetwood-Walker, S.M. The glycine site of the NMDA receptor contributes to neurokinin1 receptor agonist facilitation of NMDA receptor agonist-evoked activity in rat dorsal horn neurons. Brain Research 744, 235-245 (1997). 5.Hennen, S.,Wang, H.,Peters, L., et al. Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist. Science Signaling 6(298), 2-16 (2013). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 302.1 |
分子式 | C12H9Cl2NO4 |
CAS号 | 130798-51-5 |
稳定性 | ≥ 2 years |
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