Co 101244 hydrochloride
Chemical Name: 1-[2-(4-Hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]-4-piperidinol hydrochloride
Purity: ≥99%
Biological Activity
Co 101244 hydrochloride is a novel, potent and selective antagonist of GluN2B (formally NR2B)-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for GluN1A/2B (NR1A/2B), GluN1A/2A (NR1A/2A) and GluN1A/2C (NR1A/2C) subunit combinations respectively). Displays neuroprotective effects in vivo and in vitro.Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Zhou et al.
J.Med.Chem., 1999;42:2993 -
Pharmacological characterization of Ro 63-1908 (1-[2-(4-hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-MthD.-aspartate antagonist.
Gill et al.
J.Pharmacol.Exp.Ther., 2002;302:940 -
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.
Higgins et al.
Neuropharmacology, 2003;44:324
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Citations for Co 101244 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Co 101244 hydrochloride include:
3 Citations: Showing 1 - 3
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Region-specific role for GluN2B-containing NMDA receptors in injury to Purkinje cells and CA1 neurons following global cerebral ischemia.
Authors: Quillinan Et al.
J Cell Biol 2015;284:555
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Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala.
Authors: Mirante Et al.
Am J Physiol Renal Physiol 2014;7:62
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TRPV1 mediates the uterine capsaicin-induced NMDA NR2B-dependent cross-organ reflex sensitization in anesthetized rats.
Authors: Peng Et al.
Neuroscience 2008;295:F1324
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