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High affinity and selective negative modulator of AMPA receptors containing TARP-γ8 (Ki = 26 nM). Exhibits <50% binding against a panel of 52 receptors, ion channels and transporters (except 5HT2B and melatonin receptors 78% and 57%, respectively). Also displays minimal activity against other TARP-less AMPARs and AMPARs coexpressed with other TARPs or CNIH2. Orally bioavailable and brain penetrant. Anticonvulsant.
Sold with the permission of Janssen Pharmaceutica N.V.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 328.67. 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||3.04 mL||15.21 mL||30.43 mL|
|5 mM||0.61 mL||3.04 mL||6.09 mL|
|10 mM||0.3 mL||1.52 mL||3.04 mL|
|50 mM||0.06 mL||0.3 mL||0.61 mL|
References are publications that support the biological activity of the product.
Maher et al (2016) Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8. J.Pharmacol.Exp.Ther. 357 394 PMID: 26989142
Witkin et al (2016) A Comment on "Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8". J.Pharmacol.Exp.Ther. 358 502 PMID: 27528544
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Keywords: JNJ 55511118, JNJ 55511118 supplier, JNJ55511118, High, affinity, selective, negative, modulators, modulates, AMPA, receptors, containing, TARP-gamma8, TARP-γ8, Receptors, 6278, Tocris Bioscience
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Literature in this Area
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Learning & Memory Poster
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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.