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SB-200646A

Catalog No. T22423 CAS 143797-62-0

SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.

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SB-200646A, CAS 143797-62-0

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 35.00
1 mL * 10 mM (in DMSO)	5 days	$ 76.00

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Description	SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.
In vitro	SB200646A (4 μM) eliminates the increase in miniature inhibitory postsynaptic current (mIPSC) frequency induced by ethanol, without affecting the basal mIPSC frequency.
In vivo	SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons. 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].

Molecular Weight	302.76
Formula	C15H15ClN4O
CAS No.	143797-62-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225 mg/mL (743.2 mM), Sonication is recommended.

References and Literature

1. Blackburn TP, Suzuki K, Ashby CR Jr. 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. 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. 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.

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Keywords

SB-200646A 143797-62-0 GPCR/G Protein Neuroscience 5-HT Receptor SB 200646A SB200646A inhibitor inhibit

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