LORECLEZOLE
Biochem/physiol Actions
Loreclezole (R72063) is a sedative and anticonvulsant that exerts subtype-selective positive allosteric modulator (PAM) potency toward beta2 (β2)- or β3-containing GABAA gamma-aminobutyric acid (GABA) receptors (% potentiation by 1 µM Loreclezole of GABA EC20-stimulated current/human α1βγ2 = 100/α1β2γ2, 120/α1β3γ2, 13/α1β1γ2; α1β2γ2 EC50 = 1 µM) with >300-fold lower β1 affinity, while acting as a negative allosteric modulator (NAM) against the homomeric rho1 (ρ1) GABAA-rho receptor (rat GABAC IC50 = 0.5 µM against GABA EC10-induced current).
| Colour | white to beige |
|---|---|
| InChI key | XGLHZTBDUXXHOM-WMZJFQQLSA-N |
| InChI | 1S/C10H6Cl3N3/c11-7-1-2-8(9(12)3-7)10(13)4-16-6-14-5-15-16/h1-6H/b10-4- |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | room temp |
| Solubility | DMSO: 2 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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