1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. SB-200646A

SB-200646A 

Cat. No.: HY-103129 Purity: 99.47%
Handling Instructions

SB-200646A 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-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.

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

SB-200646A Chemical Structure

SB-200646A Chemical Structure

CAS No. : 143797-62-0

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10 mM * 1  mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
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10 mg USD 145 In-stock
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50 mg USD 480 In-stock
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100 mg USD 760 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

SB-200646A 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-200646A 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

SB200646A (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.
Molecular Weight

302.76

Formula

C₁₅H₁₅ClN₄O

CAS No.

143797-62-0

SMILES

O=C(NC1=CC=CN=C1)NC2=CC3=C(N(C)C=C3)C=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (825.74 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3029 mL 16.5147 mL 33.0295 mL
5 mM 0.6606 mL 3.3029 mL 6.6059 mL
10 mM 0.3303 mL 1.6515 mL 3.3029 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

SB-200646A5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2B5-HT2CSNCdopaminergicneuronsantipsychoticelectrophysiologicalanxiolyticInhibitorinhibitorinhibit

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SB-200646A
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HY-103129
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