Molecular structure of Desformylflustrabromine hydrochloride, CAS Number: 951322-11-5
Desformylflustrabromine hydrochloride (CAS 951322-11-5)
Alternate Names:
6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride
Application:
Desformylflustrabromine hydrochloride is a positive allosteric modulator of α4β2 nicotinic acetylcholine receptors
CAS Number:
951322-11-5
Purity:
>98%
Molecular Weight:
357.72
Molecular Formula:
C16H21BrN2•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Desformylflustrabromine hydrochloride is a positive allosteric modulator of AChR alpha 4 AChR beta2 (alpha4beta2 nicotinic acetylcholine receptors, nAChRs). It is additionally noted to selectively increase the ionic current through alpha4beta2 in the presence of ACh (acetylcholine). Desformylflustrabromine hydrochloride shows a 14-fold selectivity of alpha4beta2 versus alpha7, homomeric receptors is also observed. Other studies note the display of moderate cytotoxicity in HCT-116 cell cultures.
Desformylflustrabromine hydrochloride (CAS 951322-11-5) References
- Isolation and structure elucidation of deformylflustrabromine from the North Sea bryozoan Flustra foliacea. | Lysek, N., et al. 2002. Z Naturforsch C J Biosci. 57: 1056-61. PMID: 12562094
- Potentiation of human alpha4beta2 neuronal nicotinic receptors by a Flustra foliacea metabolite. | Sala, F., et al. 2005. Neurosci Lett. 373: 144-9. PMID: 15567570
- Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator. | Kim, JS., et al. 2007. Bioorg Med Chem Lett. 17: 4855-60. PMID: 17604168
- Pharmacological characterization of the allosteric modulator desformylflustrabromine and its interaction with alpha4beta2 neuronal nicotinic acetylcholine receptor orthosteric ligands. | Weltzin, MM. and Schulte, MK. 2010. J Pharmacol Exp Ther. 334: 917-26. PMID: 20516140
- Deconstruction of the α4β2 nicotinic acetylcholine receptor positive allosteric modulator desformylflustrabromine. | German, N., et al. 2011. J Med Chem. 54: 7259-67. PMID: 21905680
- Allosteric modulation of alpha4beta2 nicotinic acetylcholine receptors by HEPES. | Weltzin, MM., et al. 2014. Eur J Pharmacol. 732: 159-68. PMID: 22732654
- Desformylflustrabromine (dFBr) and [3H]dFBr-Labeled Binding Sites in a Nicotinic Acetylcholine Receptor. | Hamouda, AK., et al. 2015. Mol Pharmacol. 88: 1-11. PMID: 25870334
- Nicotinic acetylcholine receptor-mediated GABAergic inputs to cholinergic interneurons in the striosomes and the matrix compartments of the mouse striatum. | Inoue, R., et al. 2016. Neuropharmacology. 105: 318-328. PMID: 26808315
- Effects of nicotine in combination with drugs described as positive allosteric nicotinic acetylcholine receptor modulators in vitro: discriminative stimulus and hypothermic effects in mice. | Moerke, MJ., et al. 2016. Eur J Pharmacol. 786: 169-178. PMID: 27238974
- Nicotine facilitates nicotinic acetylcholine receptor targeting to mitochondria but makes them less susceptible to selective ligands. | Uspenska, K., et al. 2017. Neurosci Lett. 656: 43-50. PMID: 28700952
- Positive allosteric modulators of α7* or β2* nicotinic acetylcholine receptors trigger different kinase pathways in mitochondria. | Uspenska, K., et al. 2018. Int J Biochem Cell Biol. 99: 226-235. PMID: 29704624
- Desformylflustrabromine, a positive allosteric modulator of α4β2-containing nicotinic acetylcholine receptors, enhances cognition in rats. | Nikiforuk, A., et al. 2020. Pharmacol Rep. 72: 589-599. PMID: 32207091
Activator of:
AChR α 4, and AChRbeta2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Desformylflustrabromine hydrochloride, 10 mg | sc-358800 | 10 mg | $175.00 | |||
| US: Only available in the US | ||||||
Desformylflustrabromine hydrochloride, 50 mg | sc-358800A | 50 mg | $645.00 | |||
| US: Only available in the US | ||||||