| Description | Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human). |
| In vivo | Lu AF21934的治疗在应激引起的高体温、四板和掩埋大理石测试中表现出剂量依赖性的抗焦虑样效应。在SIH测试中，Lu AF21934（5 mg/kg）的抗高体温效应被苯二氮卓类受体拮抗剂氟马西尼（10 mg/kg）抑制，并且这种效应不依赖于血清素。Lu AF21934在小鼠的尾悬挂测试中不产生抗抑郁样效应；然而，它能降低未适应活动笼的小鼠的基础运动活性。 |
| Target activity | mGlu4 (human):500 nM |
| molecular weight | 315.2 |
| Molecular formula | C14H16Cl2N2O2 |
| CAS | 1445605-23-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 16.67 mg/mL (52.88 mM), Sonication is recommended. |
| References | 1. Sławińska A, et al. Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu₄ receptor. Neuropharmacology. 2013 Mar;66:225-35. 2. Ossowska K, et al. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology. 2014 Aug;83:28-35. 3. Sławińska, A., Wierońska, J., Stachowicz, K., Marciniak, M., Łasoń-Tyburkiewicz, M., & Gruca, P. et al. (2013). The antipsychotic-like effects of positive allosteric modulators of metabotropic glutamate mGlu4receptors in rodents. British Journal Of Pharmacology, 169(8), 1824-1839. doi: 10.1111/bph.12254 |