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Lusaperidone

Catalog No. T11894 CAS 214548-46-6

Synonyms: R107474

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

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Lusaperidone, CAS 214548-46-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 328.00
10 mg	In stock	$ 529.00
25 mg	In stock	$ 1,090.00
50 mg	In stock	$ 1,850.00
100 mg	In stock	$ 2,720.00

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Purity: 99.64%

Biological Description

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Description	Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.
Targets&IC50	α2C-adrenoceptor:0.15 nM(Ki), α2A-adrenoceptor:2.8 nM (Kb,human), α2A-adrenoceptor:0.13 nM (Ki), α2B-adrenoceptor (human):1 nM (Ki), H5-HT7 receptor:5 nM(Ki), α2C-adrenoceptor:4.4 nM (Kb,human)
In vitro	Lusaperidone exhibits subnanomolar affinity for α2A and α2C adrenergic receptors (Ki=0.13 and 0.15 nM, respectively) and demonstrates nanomolar affinity for hα2B adrenergic receptors and h5-HT7 receptors (Ki=1 and 5 nM, respectively). It 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. Furthermore, Lusaperidone has been demonstrated 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 acts as a full antagonist on both receptor subtypes[1].
In vivo	Lusaperidone occupies the α2A and α2C adrenergic receptors 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 is very rapid after in vivo intravenous administration; in most tissues, including the brain, it reaches maximum concentration at 5 min after tracer injection[1].

Synonyms	R107474
Molecular Weight	359.42
Formula	C22H21N3O2
CAS No.	214548-46-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 1 mg/mL (2.78 mM), Sonification is recommended.

References and Literature

1. Van der Mey M, et al. Synthesis and biodistribution of [11C]R107474, a new radiolabeled alpha2-adrenoceptor antagonist. Bioorg Med Chem. 2006 Jul 1;14(13):4526-34.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library

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Keywords

Lusaperidone 214548-46-6 GPCR/G Protein Neuroscience Adrenergic Receptor R107474 inhibitor inhibit

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