161230-88-2
基本信息
MDL 105,519
MDL 105,519 >=98% (HPLC), solid
(Z)-2-CARBOXY-4,6-DICHLOROINDOLE-3-(2'-PHENYL-2'-CARBOXY)-ENE
3-[(1E)-2-Carboxy-2-phenylethenyl]-4,6-dichloro-1H-indole-2-carboxylic acid
1H-Indole-2-carboxylic acid, 3-[(1E)-2-carboxy-2-phenylethenyl]-4,6-dichloro-
物理化學性質
報價日期 | 產品編號 | 產品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-15085 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 MDL 105519 | 161230-88-2 | 5mg | 1000元 |
2024/11/08 | HY-15085 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 MDL 105519 | 161230-88-2 | 10mM * 1mLin DMSO | 1100元 |
2024/11/08 | HY-15085 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 MDL 105519 | 161230-88-2 | 10mg | 1700元 |
常見問題列表
MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [ 3 H]glycine to rat brain membranes with a K i value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [ 3 H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca 2+ and Na + -Ca 2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine.
MDL 105519 is an NMDA receptor antagonist in vivo . Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo . This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex.