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LSN2463359

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Metabotropic glutamate receptor 5 positive allosteric modulator
LSN2463359
Names
IUPAC name N-Propan-2-yl-5-(2-pyridin-4-ylethynyl)pyridine-2-carboxamide
Identifiers
CAS Number
3D model (JSmol)
ChEMBL
ChemSpider
EC Number
  • 802-759-0
IUPHAR/BPS
PubChem CID
CompTox Dashboard (EPA)
InChI
  • InChI=1S/C16H15N3O/c1-12(2)19-16(20)15-6-5-14(11-18-15)4-3-13-7-9-17-10-8-13/h5-12H,1-2H3,(H,19,20)Key: STAFRSGTRKNXHF-UHFFFAOYSA-N
SMILES
  • CC(C)NC(=O)C1=NC=C(C=C1)C#CC2=CC=NC=C2
Properties
Chemical formula C16H15N3O
Molar mass 265.316 g·mol
Hazards
GHS labelling:
Pictograms GHS07: Exclamation mark
Signal word Warning
Hazard statements H302, H315, H319, H335
Precautionary statements P261, P264, P264+P265, P270, P271, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P319, P321, P330, P332+P317, P337+P317, P362+P364, P403+P233, P405, P501
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). Infobox references
Chemical compound

LSN2463359 is a drug used in scientific research.

Mechanism of action

LSN2463359 is a positive allosteric modulator of the mGluR5, which means it increases the activity of glutamate (an excitatory neurotransmitter) at this receptor.

Potential uses

A study has found that LSN2463359 and similar drugs can be used as a treatment to some aspects of cognitive deficits in schizophrenia. Another study also mention that it could be used in the treatment of schizophrenia due to the potential interactions between NMDA receptors and mGluR5.

References

  1. "N-Isopropyl-5-(pyridin-4-ylethynyl)picolinamide". pubchem.ncbi.nlm.nih.gov.
  2. Gilmour, Gary; Broad, Lisa M.; Wafford, Keith A.; Britton, Thomas; Colvin, Ellen M.; Fivush, Adam; Gastambide, Francois; Getman, Brian; Heinz, Beverly A.; McCarthy, Andrew P.; Prieto, Lourdes; Shanks, Elaine; Smith, Janice W.; Taboada, Lorena; Edgar, Dale M. (January 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: 224–239. doi:10.1016/j.neuropharm.2012.07.030. ISSN 1873-7064. PMID 22884720.
  3. Gastambide, Francois; Cotel, Marie-Caroline; Gilmour, Gary; O'Neill, Michael J.; Robbins, Trevor W.; Tricklebank, Mark D. (March 2012). "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. doi:10.1038/npp.2011.298. ISSN 1740-634X. PMC 3280638. PMID 22129780.
  4. Gastambide, Francois; Gilmour, Gary; Robbins, Trevor W.; Tricklebank, Mark D. (January 2013). "The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat". Neuropharmacology. 64: 240–247. doi:10.1016/j.neuropharm.2012.07.039. ISSN 1873-7064. PMID 22884612.
Metabotropic glutamate receptor modulators
Group I
mGluR1Tooltip Metabotropic glutamate receptor 1
mGluR5Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2Tooltip Metabotropic glutamate receptor 2
mGluR3Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4Tooltip Metabotropic glutamate receptor 4
mGluR6Tooltip Metabotropic glutamate receptor 6
mGluR7Tooltip Metabotropic glutamate receptor 7
mGluR8Tooltip Metabotropic glutamate receptor 8
See also: Receptor/signaling modulatorsIonotropic glutamate receptor modulatorsGlutamate metabolism/transport modulators
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