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.