货号 | 5275/50 |
别名 | N-(1-Methylethyl)-5-[2-(4-pyridinyl |
供应商 | Tocris |
生物活性 | Potent and selective positive allosteric modulator at the mGlu5 receptor (EC50 = 24 nM). Has no activity at mGlu1-4, mGlu8 and GABAB receptors. Reverses methylazoxymethanol acetate (MAM)-induced deficits in reversal learning memory and normalizes SDZ 220-581 and RO 63-1908-induced alterations in instrumental responses in rat models. Promotes wakefulness in vivo. Brain penetrant and orally active. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 265.31 |
分子式 | C16H15N3O |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 20 mM in ethanol |
参考文献 | Gastambideet al (2013) The mGlu5 positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology 64 240. PMID: 22884612. Gilmouret al(2013)In vitro characterisation of the novel positive allosteric modulators of the mGlu5 receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology 64 224. PMID: 22884720. Gastambideet al (2012) Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology 37 1057. PMID: 22129780. |