Spiroxatrine
Based on 1 Customer Validation
Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 1054-88-2
- Formula: C22H25N3O3
- Molecular Weight:379.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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α2-adrenergic receptor |
5-HT1A Receptor 3.94 nM (Ki) |
5-HT1B/D Receptor 224000 nM (Ki) |
5-HT2 Receptor 118.5 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
20 μM
Compound: Spiroxatrine
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
35.5 μM
Compound: Spiroxatrine
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
Spiroxatrine (0.01-0.1 μM, 15 mins) increases contraction in vas deferenstissues from α2A/D-adrenoceptor knockout mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Spiroxatrine (4 mg/kg/day for i.p., 5 mins) increases the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats [4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The nerve injury rat model and Carrageenan (HY-125474)-induced rat inflammation model[3]
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Dosage:1, 10, 25 ug, 5 days
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Administration:Intraperitoneal injection (i.p.)
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Result:Increased hindpaw withdrawal latencies to thermal and mechanical stimulation.
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Animal Model:Fluoxetine (HY-B0102) -induced reduction of ethanol Intake by the P Line of rats[4]
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Dosage:4 mg/kg/day, 5 mins
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Administration:Intraperitoneal injection (i.p.)
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Result:Increased the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats.
Chemical Information
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CAS No. 1054-88-2
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Appearance Solid
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Molecular Weight 379.45
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Formula C22H25N3O3
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Color White to off-white
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SMILES
O=C1NCN(C2=CC=CC=C2)C13CCN(CC4OC5=CC=CC=C5OC4)CC3
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Synonyms
R 5188
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 1.92 mg/mL (5.06 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)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. D L Nelson, et al. Spiroxatrine: a selective serotonin1A receptor antagonist. Eur J Pharmacol. 1986 May 13;124(1-2):207-8. [Content Brief]
[2]. Linda Cleary, et al. Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice. Br J Pharmacol. 2002 Jul;136(6):857-64. [Content Brief]
[3]. Z-Y Liu, et al. Involvement of 5-hydroxytryptamine(1A) receptors in the descending anti-nociceptive pathway from periaqueductal gray to the spinal dorsal horn in intact rats, rats with nerve injury and rats with inflammation. Neuroscience. 2002;112(2):399-407. [Content Brief]
[4]. W J McBride, et al. Spiroxatrine augments fluoxetine-induced reduction of ethanol intake by the P line of rats. Pharmacol Biochem Behav. 1989 Oct;34(2):381-6. [Content Brief]
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 | 2.6354 mL | 13.1770 mL | 26.3539 mL | 65.8848 mL |
| 5 mM | 0.5271 mL | 2.6354 mL | 5.2708 mL | 13.1770 mL |
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