For research use only. Not for therapeutic Use.
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface[1].
SJM-3 binds at the high-affinity benzodiazepine binding site at theα+/γ- subunit interface but effects its action through another site presumably located within the transmembrane domain. The binding affinity of SJM-3 at wild type receptors is determined by displacement of [3H]-Flunitrazepam and [3H]-Ro15-1788 and indicates a Ki of SJM-3 amounting to 218±70 nM and 242±38 nM, respectively[1].
Catalog Number | I045436 |
CAS Number | 1234977-97-9 |
Synonyms | (6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-(2-pyrazin-2-yl-1,3-thiazol-4-yl)methanone |
Molecular Formula | C18H15FN4OS |
Purity | ≥95% |
InChI | InChI=1S/C18H15FN4OS/c1-11-2-3-12-8-13(19)4-5-16(12)23(11)18(24)15-10-25-17(22-15)14-9-20-6-7-21-14/h4-11H,2-3H2,1H3 |
InChIKey | MCMRMBOJJFVNHG-UHFFFAOYSA-N |
SMILES | CC1CCC2=C(N1C(=O)C3=CSC(=N3)C4=NC=CN=C4)C=CC(=C2)F |
Reference | [1]. Simon J Middendorp, et al. Positive modulation of synaptic and extrasynaptic GABAA receptors by an antagonist of the high affinity benzodiazepine binding site. Neuropharmacology. 2015 Aug;95:459-67. |