SB-200646
SB-200646 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-200646 is orally active and has electrophysiological and anxiolytic properties in vivo.
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- CAS No.: 143797-63-1
- Formule: C15H14N4O
- Masse moléculaire:266.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2B Receptor 7.5 (pKi) |
5-HT2C Receptor 6.9 (pKi) |
5-HT2A Receptor 5.2 (pKi) |
SB-200646A (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.
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. 143797-63-1
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Masse moléculaire 266.30
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Formule C15H14N4O
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SMILES
O=C(NC1=CC=CN=C1)NC2=CC3=C(N(C)C=C3)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SB-200646 Related Classifications
HY-103129A Related Classifications
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