Cas No.: | 118876-58-7 |
Chemical Name: | NBQX free acid |
Synonyms: | NBQX free acid |
SMILES: | O=C(N1)C(NC2=C1C3=C(C([N+]([O-])=O)=C2)C(S(N)(=O)=O)=CC=C3)=O |
Formula: | C12H8N4O6S |
M.Wt: | 336.278 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | NBQX is a highly selective and competitive AMPA receptor antagonist. |
Target: | AMPA receptor[1] |
In Vivo: | NBQX is neuroprotective in a focal ischaemia model in the rat when given as an i.v. bolus dose of 30 mg/kg at the time of MCA occlusion and again at 1 h post occlusion[1]. NBQX provides potent anticonvulsant protection against AMPA. The ED50 values for the protection against AMPA-induced seizures by NBQX (30 min, i.p.) is 23.6 (11.6- 48.0)[2]. |
In Vitro: | NBQX has a high affinity for AMPA and kainate binding sites with little or no affinity for the glutamate recognition site on the NMDA receptor complex[1]. |
Animal Administration: | Rats[1] Male Sprague-Dawley rats weighing 350-390 g are used for study. 30 mg/kg of NBQX (2x15 mg/mL) is administered i.v. as a bolus dose followed by an infusion of 10 mg/kg/h for 4 h, the bolus dose and infusion are started immediately after MCA occlusion. Blood samples are taken from these animals at 1, 2, 3 and 4 h after the start of the infusion and the plasma level of NBQX in each sample is measured[1]. Mice[1] The time course for the anticonvulsant action of NBQX and of GYKI 52466 against AMPA-induced seizures is determined by pretreating groups (n=10) of Swiss mice with 30 and 60/zmol/kg NBQX or GYKI 52466 (i.p.) 15-120 min before challenging the mice with a convulsant dose of AMPA (5 nmol) i.c.v[2]. |
References: | [1]. Fukushima K, et al. Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors. J Biomol Screen. 2014 Sep; 19(8):1174-84. |