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Co 101244 HCl
Chemical Name:1-[2-(4-Hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl
]-4-piperidinol hydrochloride
Biological Activity:
Novel, potent and selective antagonist of NR2B-containing NMDA
receptors (IC50 values are 0.043, > 100 and > 100 μM for NR1A/2B, NR1A/2A and NR1A/2C subunit combinations
respectively). Displays neuroprotective effects in vivo and in vitro.
Zhouet al (1999) 4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine:
a novel, potent, and selective NR1/2B NMDA receptor antagonist. J.Med.Chem. 42
2993. Gillet al (2002) Pharmacological characterization of Ro
63-1908 (1-[2-(4-hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a
novel subtype-selective N-methyl-D-aspartate antagonist. J.Pharmacol.Exp.Ther. 302
940. Higgins et al (2003) Evaluation of the NR2B-selective NMDA
receptor antagonist Ro 63-1908 on rodent behaviour: evidence for an involvement
of NR2B NMDA receptors in response inhibition. Neuropharmacology 44
324.