SB-200646

Modify Date: 2024-01-10 19:01:15

SB-200646 structure	Common Name	SB-200646
	CAS Number	143797-63-1	Molecular Weight	266.29800
	Density	1.26g/cm3	Boiling Point	390.9ºC at 760mmHg
	Molecular Formula	C₁₅H₁₄N₄O	Melting Point	N/A
	MSDS	N/A	Flash Point	190.2ºC

Use of 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[1][2].

Name	1-(1-methylindol-5-yl)-3-pyridin-3-ylurea
Synonym	More Synonyms

Description	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[1][2].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2B Receptor:7.5 (pKi) 5-HT2C Receptor:6.9 (pKi) 5-HT2A Receptor:5.2 (pKi)
In Vitro	SB-200646 (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency[1].
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[1]. 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]. 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] Dosage: 20 mg/kg Administration: Intravenous injection; daily; for 21 days Result: Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons.
References	[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. [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.

Density	1.26g/cm3
Boiling Point	390.9ºC at 760mmHg
Molecular Formula	C₁₅H₁₄N₄O
Molecular Weight	266.29800
Flash Point	190.2ºC
Exact Mass	266.11700
PSA	58.95000
LogP	3.36330
Vapour Pressure	2.57E-06mmHg at 25°C
Index of Refraction	1.663
Storage condition	2-8°C

Mip-urea

Tocris-1371

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: SB 200646 HYDROCHLORIDE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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