Stereochemistry | ACHIRAL |
Molecular Formula | C17H21N5OS |
Molecular Weight | 343.447 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C1=CC=NC2=C1C3=C(S2)C(=O)N(C=N3)N4CCCCCC4
InChI
InChIKey=GYWGXEGOXODOQU-UHFFFAOYSA-N
InChI=1S/C17H21N5OS/c1-20(2)12-7-8-18-16-13(12)14-15(24-16)17(23)22(11-19-14)21-9-5-3-4-6-10-21/h7-8,11H,3-6,9-10H2,1-2H3
A-841720, a novel, potent and non-competitive mGluR1 antagonist in models of pain and of motor and cognitive function, is being under development by Merz Pharmaceuticals GmbH. It is a selective non-competitive mGlu1 receptor antagonist (IC50: 10 nM); showing 34-fold selectivity over mGluR5 and no significant activity at other mGluR receptors, neurotransmitter receptors, ion channels, and transporters. A-841720 demonstrated full efficacy in various in vivo animal pain models.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
A-841720 significantly reduced formalin-induced behaviours,
such as hindpaw flinching and licking, at the doses
of 10 and 30 mg/kg
Route of Administration:
Intraperitoneal