Robalzotan hydrochloride
Robalzotan hydrochloride (NAD-299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.
For research use only. We do not sell to patients.
- CAS No.: 184674-99-5
- Formula: C18H24ClFN2O2
- Molecular Weight:354.85
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1A Receptor |
Robalzotan hydrochloride (5, 50 µg/kg; i.v.) increases the firing rate of the 5-HT cells[1].
Robalzotan hydrochloride (2-100 µg/kg; i.v.) occupies 5-HT1A receptors in a dose-dependent in monkeys[2].
Robalzotan hydrochloride (0.3; 1 and 3 µmol/kg s.c) causes a dose-dependent increase of extracellular ACh levels in the rat FC[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:300-600 g, male Sprague-Dawley rats (5-HT cells)[1]
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Dosage:1, 5, 12.5, 25, 50, 100 µg/kg
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Administration:I.v.
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Result:Significantly increased the activity of such neurons at 5 µg/kg, increasing doses of robalzotan 5-100 µg/kg or 50-400 mg/kg did not further affect the firing rate of 5-HT neurons.
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Animal Model:3-4 kg, cynomolgus monkeys[2]
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Dosage:2, 10, 20, 100 µg/kg
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Administration:I.v.
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Result:Occupied 5-HT1A receptors in a dose-dependent and saturable manner and he highest 5-HT1A receptor occupancy (70-80%) was attained after 100 μg/kg.
Chemical Information
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CAS No. 184674-99-5
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Appearance Solid
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Molecular Weight 354.85
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Formula C18H24ClFN2O2
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Color White to off-white
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SMILES
O=C(C1=C2C[C@@H](N(C3CCC3)C4CCC4)COC2=C(F)C=C1)N.[H]Cl
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Synonyms
NAD-299 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (281.81 mM; Need ultrasonic and warming; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (278 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Arborelius L, et al. The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing. Eur J Pharmacol. 1999 Oct 8;382(2):133-8. [Content Brief]
[2]. Farde L, et al. PET-Determination of robalzotan (NAD-299) induced 5-HT(1A) receptor occupancy in the monkey brain. Neuropsychopharmacology. 2000 Apr;22(4):422-9. [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 (sealed storage, away from moisture and light). 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 | 2.8181 mL | 14.0905 mL | 28.1809 mL | 70.4523 mL |
| 5 mM | 0.5636 mL | 2.8181 mL | 5.6362 mL | 14.0905 mL | |
| 10 mM | 0.2818 mL | 1.4090 mL | 2.8181 mL | 7.0452 mL | |
| 15 mM | 0.1879 mL | 0.9394 mL | 1.8787 mL | 4.6968 mL | |
| 20 mM | 0.1409 mL | 0.7045 mL | 1.4090 mL | 3.5226 mL | |
| 25 mM | 0.1127 mL | 0.5636 mL | 1.1272 mL | 2.8181 mL | |
| 30 mM | 0.0939 mL | 0.4697 mL | 0.9394 mL | 2.3484 mL | |
| 40 mM | 0.0705 mL | 0.3523 mL | 0.7045 mL | 1.7613 mL | |
| 50 mM | 0.0564 mL | 0.2818 mL | 0.5636 mL | 1.4090 mL | |
| 60 mM | 0.0470 mL | 0.2348 mL | 0.4697 mL | 1.1742 mL | |
| 80 mM | 0.0352 mL | 0.1761 mL | 0.3523 mL | 0.8807 mL | |
| 100 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.7045 mL |
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