Lusaperidone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lusaperidone (R107474) 是一种α2肾上腺素受体 (adrenergic receptor) 拮抗剂，对α2A和α2C的 Ki 值分别为0.13和0.15 nM。

Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.

Lusaperidone has subnanomolar affinity for α2A and α2C adrenergic receptor (Ki=0.13 and 0.15 nM, respectively) and shows nanomolar affinity for the hα2B adrenergic receptor and h5-HT7 receptors (Ki=1 and 5 nM, respectively). Lusaperidone interacts weakly (Ki 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 μM, 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 α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4 nM, respectively) and is a full antagonist on both receptor subtypes.

Lusaperidone occupies the α2A and α2C 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.

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GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

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214548-46-6

359.42

C22H21N3O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 3.45 mg/mL (9.60 mM; 超声助溶 (<60°C)

Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1

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(-20℃)

With Ice Pack

≥ 2 years