2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (SB-200646A) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

SB-200646 Chemical Structure

SB-200646 Chemical Structure

CAS No. : 143797-63-1

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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].

IC50 & Target[1][2]

5-HT2B Receptor

7.5 (pKi)

5-HT2C Receptor

6.9 (pKi)

5-HT2A Receptor

5.2 (pKi)

In Vitro

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].

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

SB-200646 Related Antibodies
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].

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

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.
Molecular Weight

266.30

Formula

C15H14N4O
CAS No.
SMILES

O=C(NC1=CC=CN=C1)NC2=CC3=C(N(C)C=C3)C=C2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SB-200646 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-200646143797-63-1SB200646SB 2006465-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2B5-HT2CSNCdopaminergicneuronsantipsychoticelectrophysiologicalanxiolyticInhibitorinhibitorinhibit

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