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 GABA_A 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) GABA_A-rho receptor (rat GABA_C IC50 = 0.5 µM against GABA EC10-induced current).