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].
Product Specifications
CAS Number
143797-63-1
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
Target
5-HT Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/sb-200646.html
Solubility
10 mM in DMSO
Smiles
O=C(NC1=CC=CN=C1)NC2=CC3=C(N(C)C=C3)C=C2
Molecular Formula
C15H14N4O
Molecular Weight
266.30
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-HT2 Receptor; α-1 microglobulin
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