LSN2463359

A brain penetrant positive allosteric modulator of the mGluR5

LSN2463359 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5; EC50 = 24 nM).1 It is without effect at other mGluRs. LSN2463359 is brain penetrant and reverses learning deficits in a rat model of schizophrenia.1,2 Through its effects on mGluR5, LSN2463359 attenuates deficits in performance in operant behavior induced by SDZ-220581, an NMDA (Item No. 14581) receptor antagonist, in rats.3,2 It also promotes wakefulness in animals.2

265.3

≥98%

O=C(NC(C)C)C(C=C1)=NC=C1C#CC2=CC=NC=C2

C16H15N3O

1401031-52-4

≥ 4 years

DMF: 30 mg/ml DMSO: 30 mg/ml Ethanol: 30 mg/ml

1.Gastambide, F.,Cotel, M.-C.,Gilmour, G., et al. Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology 37(4), 1057-1066 (2012).
2.Gilmour, G.,Broad, L.M.,Wafford, K.A., et al. 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, 224-239 (2013).
3.Gastambide, F.,Gilmour, G.,Robbins, T.W., et al. The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology 64, 240-247 (2013).