Lorediplon

Lorediplon is a ligand for alpha1 subunit-containing GABAA receptors. In vivo, lorediplon inhibits spontaneous motor activity and increases duration of sleep in mice (ED50s = 0.13 and 1.2 mg/kg, respectively). It selectively inhibits spontaneous motor activity, which is driven by alpha1 subunit-containing GABAA receptors, over modification of muscular tone in mice, an alpha2 subunit-containing GABAA receptor-stimulated activity. Lorediplon (0.13 and 1.2 mg/kg) also decreases latency to slow wave sleep (SWS) and paradoxical sleep (PS) in mice. Formulations containing lorediplon have been used in the treatment of insomnia.Formal Name: N-[2-fluoro-5-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methyl-acetamide. CAS Number: 917393-39-6. Molecular Formula: C20H15FN4O2S. Formula Weight: 394.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 14 mg/ml. lambdamax: 230, 312, 343 nm. SMILES: O=C(C1=CC=CS1)C2=C3N(N=C2)C(C4=CC=C(F)C(N(C)C(C)=O)=C4)=CC=N3. InChi Code: InChI=1S/C20H15FN4O2S/c1-12(26)24(2)17-10-13(5-6-15(17)21)16-7-8-22-20-14(11-23-25(16)20)19(27)18-4-3-9-28-18/h3-11H,1-2H3. InChi Key: NQPOCLFSADOXBR-UHFFFAOYSA-N.