| Description | VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM). |
| In vivo | VU0360172 在体内刺激多磷酸肌醇(PI)的水解作用，但在mGlu5受体基因敲除的小鼠中此作用被消除[4]。 |
| Target activity | mGlu5:16 nM(EC50), mGlu5:195 nM(Ki) |
| Synonyms | VU-0360172, VU 0360172 |
| molecular weight | 294.32 |
| Molecular formula | C18H15FN2O |
| CAS | 1310012-12-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 83 mg/mL (282.01 mM), Sonication is recommended. |
| References | 1. Notartomaso S, Mascio G, Scarselli P, Martinello K, Fucile S, Gradini R, Bruno V, Battaglia G, Nicoletti F. Expression of the K(+)/Cl(-) cotransporter, KCC2, in cerebellar Purkinje cells is regulated by group-I metabotropic glutamate receptors. Neuropharmacology. 2017 Mar 15;115:51-59. doi: 10.1016/j.neuropharm.2016.07.032. Epub 2016 Aug 3. PubMed PMID: 27498071. 2. Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017 Mar 15;115:60-72. doi: 10.1016/j.neuropharm.2016.07.001. Epub 2016 Jul 5. PubMed PMID: 27392634; PubMed Central PMCID: PMC5217481. 3. D'Amore V, Raaijmakers RH, Santolini I, van Rijn CM, Ngomba RT, Nicoletti F, van Luijtelaar G. The anti-absence effect of mGlu5 receptor amplification with VU0360172 is maintained during and after antiepileptogenesis. Pharmacol Biochem Behav. 2016 Jul-Aug;146-147:50-9. doi: 10.1016/j.pbb.2016.05.004. Epub 2016 May 10. PubMed PMID: 27178815. 4. Kiritoshi T, Ji G, Neugebauer V. Rescue of Impaired mGluR5-Driven Endocannabinoid Signaling Restores Prefrontal Cortical Output to Inhibit Pain in Arthritic Rats. J Neurosci. 2016 Jan 20;36(3):837-50. doi: 10.1523/JNEUROSCI.4047-15.2016. PubMed PMID: 26791214; PubMed Central PMCID: PMC4719019. |