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Submit ReviewLY 456236 hydrochloride
Description: Selective mGlu1 antagonist
Alternative Names: MPMQ hydrochloride
Chemical Name: 6-Methoxy-N-(4-methoxyphenyl)-4-quinazolinamine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for LY 456236 hydrochloride
LY 456236 hydrochloride is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). Reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.
Technical Data for LY 456236 hydrochloride
| M. Wt | 317.77 |
| Formula | C16H15N3O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 338736-46-2 |
| PubChem ID | 9926998 |
| InChI Key | AVKFOWUSTVWZQN-UHFFFAOYSA-N |
| Smiles | Cl.COC1=CC=C(NC2=C3C=C(OC)C=CC3=NC=N2)C=C1 |
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 LY 456236 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.36 | 20 |
Preparing Stock Solutions for LY 456236 hydrochloride
The following data is based on the product molecular weight 317.77. 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 |
|---|---|---|---|
| 0.2 mM | 15.73 mL | 78.67 mL | 157.35 mL |
| 1 mM | 3.15 mL | 15.73 mL | 31.47 mL |
| 2 mM | 1.57 mL | 7.87 mL | 15.73 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.15 mL |
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Product Datasheets for LY 456236 hydrochloride
References for LY 456236 hydrochloride
References are publications that support the biological activity of the product.
Shannon et al (2005) Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology 49 188 PMID: 16011839
Bertorelli et al (2005) Selective blockade of metabotropic glutamate subtype mGluR1 receptors induce anti-nociceptive effects. Neuropharmacology 49 231
If you know of a relevant reference for LY 456236 hydrochloride, please let us know.
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Citations for LY 456236 hydrochloride
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Reviews for LY 456236 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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Action via NMDA receptors.
By
Sergiy Sylantyev on 04/02/2021
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: Hippocampus
1 microM LY 456236 was tested on action potentials generated by current injection into CA3 hippocampal neuron. Application of LY increased significantly a number of action potentials. This effect disappeared after partial block of NMDA receptors. Illustration: control recording of action potentials (top) and recording with LY 456236 (bottom).
Can be easily diluted, no problem with long-time storage in aliquots.
Literature in this Area
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