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Submit ReviewSB 216641 hydrochloride
Description: Selective h5-HT1B antagonist
Chemical Name: N-[3-[3-(Dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for SB 216641 hydrochloride
SB 216641 hydrochloride is a selective h5-HT1B antagonist with approximately 25-fold selectivity over h5-HT1D and little or no affinity for a range of other receptor types.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data for SB 216641 hydrochloride
| M. Wt | 523.03 |
| Formula | C28H30N4O4.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 193611-67-5 |
| PubChem ID | 10392025 |
| InChI Key | JPBMDMNORXKGHZ-UHFFFAOYSA-N |
| Smiles | Cl.COC1=C(OCCN(C)C)C=C(NC(=O)C2=CC=C(C=C2)C2=CC=C(C=C2C)C2=NOC(C)=N2)C=C1 |
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.
Solubility Data for SB 216641 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 26.15 | 50 |
Preparing Stock Solutions for SB 216641 hydrochloride
The following data is based on the product molecular weight 523.03. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.82 mL | 19.12 mL | 38.24 mL |
| 2.5 mM | 0.76 mL | 3.82 mL | 7.65 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.82 mL |
| 25 mM | 0.08 mL | 0.38 mL | 0.76 mL |
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Product Datasheets for SB 216641 hydrochloride
References for SB 216641 hydrochloride
References are publications that support the biological activity of the product.
Hagan et al (1997) Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig. Eur.J.Pharmacol. 331 169 PMID: 9274976
Price et al (1997) SB-216641 and BRL-15572 - compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch.Pharmacol. 356 312 PMID: 930567
Schlicker et al (1997) Effects of selective h5-HT1B (SB-216641) and 5-HT1D (BRL-15572) receptor ligands on guinea pig and human 5-HT auto- and heteroreceptors. Naunyn Schmiedebergs Arch.Pharmacol. 356 321 PMID: 9303568
If you know of a relevant reference for SB 216641 hydrochloride, please let us know.
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Keywords: SB 216641 hydrochloride, SB 216641 hydrochloride supplier, Selective, h5-HT1B, antagonist, Serotonin, Receptors, SB216641, hydrochloride, GlaxoSmithKline, GSK, 5-HT1B, 1242, Tocris Bioscience
5 Citations for SB 216641 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 216641 hydrochloride include:
Soll et al (2012) Expression of serotonin receptors in human hepatocellular cancer. Clin Cancer Res 18 5902 PMID: 23087410
Dunbar et al (2010) Endogenous extracellular serotonin modulates the spinal locomotor network of the neonatal mouse. J Physiol 588 139 PMID: 19884315
Krishnan (2016) Amygdala-hippocampal phospholipase D (PLD) signaling as novel mechanism of cocaine-environment maladaptive conditioned responses. Int.J.Neuropsychopharmacol. 19 1 PMID: 26802567
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
Watakabe et al (2009) Enriched expression of serotonin 1B and 2A receptor genes in macaque visual cortex and their bidirectional modulatory effects on neuronal responses. J Biol Chem 19 1915 PMID: 19056862
Do you know of a great paper that uses SB 216641 hydrochloride from Tocris? Please let us know.
Reviews for SB 216641 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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Excellent product.
By
Anonymous on 06/03/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: CHO
1µM
After reaching 80% confluence, cells were treated with the selective 5-HT2CR antagonist SB242084 (300nM) or the 5-HT1BR antagonist SB216641 (1µM), applied 10 minutes prior to agonist application.
Literature in this Area
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