Catalog Number: 5275
Chemical Name: N-(1-Methylethyl)-5-[2-(4-pyridinyl)ethynyl]-2-pyridinecarboxamide
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator.
    Gastambide et al.
    Neuropsychopharmacology, 2012;37:1057
  2. 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.
    Gilmour et al.
    Neuropharmacology, 2013;64:224
  3. The mGlu5 positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat.
    Gastambide et al.
    Neuropharmacology, 2013;64:240
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