Lusaperidone
Based on 1 Customer Validation
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 214548-46-6
- Formula: C22H21N3O2
- Molecular Weight:359.42
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
Endocrinology Compound Library
HY-L047
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
Heterocyclic Compound Library
HY-L138
-
Antihypertensive Compound Library
HY-L145
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
MCE Bioactive Compound Library
HY-L001V
-
High-Throughput Bioactive Compound Library
HY-L205
-
Lactylation Compound Library
HY-L249
All Adrenergic Receptor Isoforms
More
Biological Activity
Ki: 0.13 nM (α2A adrenergic receptor), 0.15 nM (α2C adrenergic receptor)[1]
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 214548-46-6
-
Appearance Solid
-
Molecular Weight 359.42
-
Formula C22H21N3O2
-
Color White to light yellow
-
SMILES
O=C1C(CCN2CCC(OC3=CC=CC=C34)=C4C2)=C(C)N=C5N1C=CC=C5
-
Synonyms
R107474
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 3.45 mg/mL (9.60 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Rats: Radio labeled Lusaperidone (24–28 GBq/μmol) is injected into the tail vein of diethyl ether anesthetized male Wistar rats (200–250 g). The rats received 30–40 MBq (injected at the start of the experiment) in 300 μL saline including 10% (v/v) ethanol. The rats are sacrificed by cervical dislocation at 5, 10, 20, and 30 min post injection under diethyl ether anesthesia. A blood sample is taken by cardiac puncture and selected tissues are rapidly dissected and weighed. The radioactivity is measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7823 mL | 13.9113 mL | 27.8226 mL | 69.5565 mL |
| 5 mM | 0.5565 mL | 2.7823 mL | 5.5645 mL | 13.9113 mL |
Lusaperidone Related Classifications
HY-U00117 Related Classifications
Powered by Bioz