SB 206553 hydrochloride

Catalog # Availability Size / Price Qty
1661/10
1661/50
5-HT2C Receptor Antagonists Small Molecule
1 Image
Description: Potent and selective 5-HT2B and 5-HT2C antagonist; orally active

Chemical Name: 3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide hydrochloride

Purity: ≥99%

Product Details
Citations (8)
Supplemental Products
Reviews (1)

Biological Activity

Potent and selective 5-HT2B/5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92). Displays > 80-fold selectivity over all other 5-HT receptor subtypes and a variety of other receptors (pKi < 6). Centrally active following oral administration in vivo.

Technical Data

M.Wt:
328.8
Formula:
C17H16N4O.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at RT
CAS No:
1197334-04-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

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Citations for SB 206553 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for SB 206553 hydrochloride include:

8 Citations: Showing 1 - 8

  1. Synthesis, transport, and metabolism of serotonin formed from exogenously applied 5-HTP after spinal cord injury in rats.
    Authors: Li Et al.
    J Neurophysiol  2014;111:145
  2. A xanthine-derivative K(+)-channel opener protects against serotonin-induced cardiomyocyte hypertrophy via the modulation of protein kinases.
    Authors: Kuo Et al.
    Int J Biol Sci  2014;10:64
  3. 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization.
    Authors: Bigford Et al.
    J Biol Chem  2012;287:11049
  4. Pulmonary vascular effects of serotonin and selective serotonin reuptake inhibitors in the late-gestation ovine fetus.
    Authors: Delaney Et al.
    Am J Physiol Lung Cell Mol Physiol  2011;301:L937
  5. The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen.
    Authors: Canal Et al.
    Psychopharmacology (Berl)  2010;209:163
  6. Recovery of motoneuron and locomotor function after spinal cord injury depends on constitutive activity in 5-HT2C receptors.
    Authors: Murray Et al.
    Nat Med  2010;16:694
  7. Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors.
    Authors: Fouad Et al.
    J Neurophysiol  2010;104:2975
  8. Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
    Authors: Hampson Et al.
    Diabetologia  2007;50:1743

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Effects of SB-206553 on MDMA-induced changes in dorsal striatal electrophysiology
By Kevin Ball on 01/25/2019
Species: Rat

We assessed the effect of SB-206553 (2.0 mg/kg, s.c.) on dorsal striatal single-unit electrophysiology following MDMA (ecstasy; 5.0 mg/kg) administration. A coefficient-of-variation analysis indicated significantly less variability in the magnitude of both MDMA-induced neuronal excitations and inhibitions in rats that were pretreated with SB-206553 compared to vehicle (shown in figure).

PMID: 16001122 Reference

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