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Co 101244 hydrochloride
Biological Activity for Co 101244 hydrochloride
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.
Compound Libraries for Co 101244 hydrochloride
Technical Data for Co 101244 hydrochloride
|Storage||Store at +4°C|
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.
Solubility Data for Co 101244 hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Co 101244 hydrochloride
The following data is based on the product molecular weight 377.91. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.65 mL||13.23 mL||26.46 mL|
|5 mM||0.53 mL||2.65 mL||5.29 mL|
|10 mM||0.26 mL||1.32 mL||2.65 mL|
|50 mM||0.05 mL||0.26 mL||0.53 mL|
Product Datasheets for Co 101244 hydrochloride
References for Co 101244 hydrochloride
References are publications that support the biological activity of the product.
Zhou et 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 PMID: 10425109
Gill et 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-MthD.-aspartate antagonist. J.Pharmacol.Exp.Ther. 302 940 PMID: 12183650
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 PMID: 12604092
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Keywords: Co 101244 hydrochloride, Co 101244 hydrochloride supplier, selective, NR2B, antagonists, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, Co101244, hydrochloride, PD174494, Ro63-1908, GluN2B, PD, 174494, Ro, 63-1908, 2456, Tocris Bioscience
3 Citations for Co 101244 hydrochloride
Citations are publications that use Tocris products. Selected citations for Co 101244 hydrochloride include:
Mirante et al (2014) Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala. Am J Physiol Renal Physiol 7 62 PMID: 25071439
Peng et al (2008) TRPV1 mediates the uterine capsaicin-induced NMDA NR2B-dependent cross-organ reflex sensitization in anesthetized rats. Neuroscience 295 F1324 PMID: 18632800
Quillinan et al (2015) Region-specific role for GluN2B-containing NMDA receptors in injury to Purkinje cells and CA1 neurons following global cerebral ischemia. J Cell Biol 284 555 PMID: 25450957
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.