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Potent and selective mGlu7 antagonist (IC50 = 88 nM); inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice. Displays no effects on the LTP of mGlu7 deficient mice. Exhibits novel activity by binding to the mGlu7 Venus flytrap domain (VFTD). Exhibits anti-anxiety effects in rodent models. Brain penetrant.
|Storage||Store at -20°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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 380.13. 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||2.63 mL||13.15 mL||26.31 mL|
|5 mM||0.53 mL||2.63 mL||5.26 mL|
|10 mM||0.26 mL||1.32 mL||2.63 mL|
|50 mM||0.05 mL||0.26 mL||0.53 mL|
References are publications that support the biological activity of the product.
Gee et al (2014) Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. J.Biol.Chem. 289 10975 PMID: 24596089
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Keywords: XAP 044, XAP 044 supplier, XAP044, potent, specific, mGlu7, antagonists, glutamate, metabotropic, group, III, receptors, venus, flytrap, domain, VFTD, anti-anxiety, Brain, penetrant, Glutamate, (Metabotropic), Group, Receptors, 5248, Tocris Bioscience
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We have studied the cross-talk between mGlu7 and alpha1-adrenergic receptor in recombinant HEK293 cells and XAP 044 was successfully used to antagonize the effect of L-AP4. Briefly, after transfection, we measured the modulation of L-AP4, the mGlu7 receptor agonist on phenylephrine-induced stimulation of inositol phosphates formation. The effect of L-AP4 was antagonised by XAP044 (at 10 and 100 micromolar)
Literature in this Area
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
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.
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.
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.