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LSN2463359

From Wikipedia, the free encyclopedia
Metabotropic glutamate receptor 5 positive allosteric modulator
LSN2463359
Names
IUPAC name
N-Propan-2-yl-5-(2-pyridin-4-ylethynyl)pyridine-2-carboxamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
EC Number
  • 802-759-0
  • 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
  • CC(C)NC(=O)C1=NC=C(C=C1)C#CC2=CC=NC=C2
Properties
C16H15N3O
Molar mass265.316 g·mol−1
Hazards
GHS labelling:[1]
GHS07: Exclamation mark
Warning
H302,H315,H319,H335
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 theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

LSN2463359 is a drug used in scientific research.

Mechanism of action

[edit]

LSN2463359 is a positive allosteric modulator of themGluR5,[2] which means it increases the activity ofglutamate (an excitatory neurotransmitter) at this receptor.

Potential uses

[edit]

A study has found that LSN2463359 and similar drugs can be used as a treatment to some aspects of cognitive deficits in schizophrenia.[3] Another study also mention that it could be used in the treatment of schizophrenia due to the potential interactions betweenNMDA receptors and mGluR5.[4]

References

[edit]
  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.
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
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