Lusaperidone

214548-46-6

C22H21N3O2

10 mM in DMSO

GPCR/G Protein; Neuronal Signaling

Lusaperidone (R107474) is an alpha2 adrenergic receptor antagonist with K_is of 0.13 and 0.15 nM for alpha2A and alpha2C, respectively. IC50 & Target: Ki: 0.13 nM (alpha2A adrenergic receptor), 0.15 nM (alpha2C adrenergic receptor)^[1] In Vitro: Lusaperidone has subnanomolar affinity for alpha2A and alpha2C adrenergic receptor (K_i=0.13 and 0.15 nM, respectively) and shows nanomolar affinity for the halpha2B adrenergic receptor and h5-HT7 receptors (K_i=1 and 5 nM, respectively). Lusaperidone interacts weakly (K_i values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3 and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 uM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Lusaperidone has been shown to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human alpha2A and alpha2C adrenoceptors expressed in cell lines (K_b is 2.8 and 4.4 nM, respectively) and is a full antagonist on both receptor subtypes^[1]. In Vivo: Lusaperidone occupies the alpha2A and alpha2C adrenergic receptor with an ED₅₀ of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 after in vivo intravenous administration is very rapid; in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection^[1].