Desformylflustrabromine hydrochloride - CAS 951322-11-5
Category: Inhibitor
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Molecular Formula:
C16H21BrN2.HCl
Molecular Weight:
357.72
COA:
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Targets:
nAChR
Description:
The hydrochloride salt form of Desformylflustrabromine, which has been found to be a positive allosteric modulator of α4β2 nicotinic acetylcholine receptors.
Purity:
≥98% by HPLC
Appearance:
Off-white Solid
Synonyms:
6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride
MSDS:
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InChIKey:
GEZWEAPBLKXKGN-UHFFFAOYSA-N
InChI:
InChI=1S/C16H21BrN2.ClH/c1-5-16(2,3)15-13(8-9-18-4)12-7-6-11(17)10-14(12)19-15;/h5-7,10,18-19H,1,8-9H2,2-4H3;1H
Canonical SMILES:
CC(C)(C=C)C1=C(C2=C(N1)C=C(C=C2)Br)CCNC.Cl
1.Nicotine facilitates nicotinic acetylcholine receptor targeting to mitochondria but makes them less susceptible to selective ligands.
Uspenska K;Lykhmus O;Gergalova G;Chernyshov V;Arias HR;Komisarenko S;Skok M Neurosci Lett. 2017 Aug 24;656:43-50. doi: 10.1016/j.neulet.2017.07.009. Epub 2017 Jul 9.
Several nicotinic acetylcholine receptor (nAChR) subtypes are expressed in mitochondria to regulate the internal pathway of apoptosis in ion channel-independent manner. However, the mechanisms of nAChR activation in mitochondria and targeting to mitochondria are still unknown. Nicotine has been shown to favor nAChR pentamer assembly, folding, and maturation on the way of biosynthesis. The idea of the present work was to determine whether nicotine affects the content, glycosylation, and function of mitochondrial nAChRs. Experiments were performed in isolated liver mitochondria from mice, that either consumed or not nicotine with the drinking water (200μL/L) for 7days. Mitochondria detergent lysates were studied by sandwich or lectin ELISA for the presence and carbohydrate composition of different nAChR subunits. Intact mitochondria were examined by flow cytometry for the binding of fluorescently labeled α-cobratoxin and were tested in functional assay of cytochrome c release under the effect of either Ca;2+; or wortmannin in the presence or absence of nAChR-selective ligands, including PNU-282987 (1nM), dihydro-β-erythroidine (DhβE, 1μM), PNU-120596 (0.3, 3, or 10μM) and desformylflustrabromine hydrochloride (dFBr, 0.
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CAS 951322-11-5 Desformylflustrabromine hydrochloride

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