LSN2463359
Metabotropic glutamate receptor 5 positive allosteric modulator
LSN2463359
Names
IUPAC name
N -Propan-2-yl-5-(2-pyridin-4-ylethynyl)pyridine-2-carboxamide
Identifiers
ChEMBL
ChemSpider
EC Number
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
C 16 H 15 N 3 O
Molar mass
265.316 g·mol−1
Hazards
GHS labelling :[ 1]
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 their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
LSN2463359 is a drug used in scientific research.
Mechanism of action
LSN2463359 is a positive allosteric modulator of the mGluR5 ,[ 2] 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.[ 3] Another study also mention that it could be used in the treatment of schizophrenia due to the potential interactions between NMDA receptors and mGluR5 .[ 4]
References
^ "N-Isopropyl-5-(pyridin-4-ylethynyl)picolinamide" . pubchem.ncbi.nlm.nih.gov .
^ 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 .
^ 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 .
^ 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
mGluR1 Tooltip Metabotropic glutamate receptor 1 mGluR5 Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2 Tooltip Metabotropic glutamate receptor 2 mGluR3 Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4 Tooltip Metabotropic glutamate receptor 4 mGluR6 Tooltip Metabotropic glutamate receptor 6 mGluR7 Tooltip Metabotropic glutamate receptor 7 mGluR8 Tooltip Metabotropic glutamate receptor 8