| Name | XAP044 |
| Description | XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1]. |
| In vitro | Previous study showed that in contrast to all previous mGlu7-selective drugs, XAP044 did not act through the seven-transmembrane region but rather via a binding pocket localized in mGlu7's extracellular Venus flytrap domain, a region identified for orthosteric agonist binding, which was suggested by the chimeric receptor studies in recombinant cell line assays [1]. |
| In vivo | In rodent behavioral paradigms, XAP044 demonstrated good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy. In addition, XAP044 could reduce freezing during acquisition of Pavlovian fear and innate anxiety, which was consistent with the phenotypes of mGlu7-deficient mice. Moreover, XAP044 was able to inhibit lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm. It was alos found that there was no effect of XAP044 on LTP of mGlu7-deficient mice, suggesting that such pharmacological effect was mGlu7-dependent [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (157.84 mM), Sonication is recommended.
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| Keywords | XAP-044 | XAP044 | XAP 044 | wide spectrum | neurotransmission | mGluR | mGlu7 | Metabotropic glutamate receptors | Inhibitor | inhibit | CNS | brain exposure | anxiolytic-like | anti-stress | antidepressant |
| Inhibitors Related | S-Sulfo-L-cysteine sodium salt | IDRA-21 | Urethane | Decanoic Acid | DCB | L-Cysteic acid monohydrate | Evans blue | L-Glutamine | Direct Blue 1 | L-Glutamic acid monosodium salt | Memantine hydrochloride | O-Phospho-L-serine |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Glutamine Metabolism Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max |
United States
