SB-200646 

SB-200646 is the first selective 5-HT_2B/2C over 5-HT_2A receptor antagonist with pK_i values of 7.5, 6.9 and 5.2 for 5-HT_2B, 5-HT_2C and 5-HT_2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo^[1][2].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

266.30

C₁₅H₁₄N₄O

143797-63-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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. Synaps  [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]