Ro 25-6981 Maleate

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Chemical Information

Product name：Ro 25-6981 Maleate	Purity：98% min
CAS NO：1312991-76-6	Solubility：DMSO : ≥ 61 mg/mL (133.91 mM)
Molecular Formula：C₂₆H₃₃NO₆	Package：Package according to customer requirements
Molecular Weight：455.543	Storage：Store at 2-8°C

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Remarks

Ro 25-6981 maleate is a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity.

References

[1]. Fischer G, et al. Ro 25-6981, a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro. J Pharmacol Exp Ther. 1997 Dec;283(3):1285-92.

[2]. Lynch DR, et al. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (epsilon2) subunit. Eur J Pharmacol. 2001 Mar 30;416(3):185-95.

[3]. Jiang M, et al. Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. Pharmacol Biochem Behav. 2013 Nov;112:56-63.