SB-200646A
Based on 1 Customer Validation
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
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- Pureté : 99.14%
- CAS No.: 143797-62-0
- Formule: C15H15ClN4O
- Masse moléculaire:302.76
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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5-HT2B Receptor 7.5 (pKi) |
5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2C Receptor 6.9 (pKi) |
5-HT2A Receptor 5.2 (pKi) |
In Vitro
SB200646A (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male albino Sprague-Dawley rats (200-225 g at the beginning of treatment and 300-350 g at the time of the experiment)[1]
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Dosage:20 mg/kg
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Administration:Intravenous injection; daily; for 21 days
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Result:Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons.
Chemical Information
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CAS No. 143797-62-0
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Appearance Solid
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Masse moléculaire 302.76
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Formule C15H15ClN4O
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CN=C1)NC2=CC3=C(N(C)C=C3)C=C2.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 250 mg/mL (825.74 mM; Need ultrasonic; 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). 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). 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)
Pureté et documentation
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Fiche technique (272 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Blackburn TP, et al. The acute and chronic administration of the 5-HT(2B/2C) receptor antagonist SB-200646A significantly alters the activity of spontaneously active midbrain dopamine neurons in the rat: An in vivo extracellular single cell study. Synapse. 2006 Jun 15;59(8):502-12. [Content Brief]
[2]. Kennett GA, et al. In vivo properties of SB 200646A, a 5-HT2C/2B receptor antagonist. Br J Pharmacol. 1994 Mar;111(3):797-802. [Content Brief]
[3]. Theile JW, et al. Role of 5-hydroxytryptamine2C receptors in Ca2+-dependent ethanol potentiation of GABA release onto ventral tegmental area dopamine neurons. J Pharmacol Exp Ther. 2009 May;329(2):625-33. [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). 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 | 3.3029 mL | 16.5147 mL | 33.0295 mL | 82.5737 mL |
| 5 mM | 0.6606 mL | 3.3029 mL | 6.6059 mL | 16.5147 mL | |
| 10 mM | 0.3303 mL | 1.6515 mL | 3.3029 mL | 8.2574 mL | |
| 15 mM | 0.2202 mL | 1.1010 mL | 2.2020 mL | 5.5049 mL | |
| 20 mM | 0.1651 mL | 0.8257 mL | 1.6515 mL | 4.1287 mL | |
| 25 mM | 0.1321 mL | 0.6606 mL | 1.3212 mL | 3.3029 mL | |
| 30 mM | 0.1101 mL | 0.5505 mL | 1.1010 mL | 2.7525 mL | |
| 40 mM | 0.0826 mL | 0.4129 mL | 0.8257 mL | 2.0643 mL | |
| 50 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6515 mL | |
| 60 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL | 1.3762 mL | |
| 80 mM | 0.0413 mL | 0.2064 mL | 0.4129 mL | 1.0322 mL | |
| 100 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL |
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