Desformylflustrabromine hydrochloride

Modify Date: 2024-01-14 18:35:16

Desformylflustrabromine hydrochloride Structure
Desformylflustrabromine hydrochloride structure
Common Name Desformylflustrabromine hydrochloride
CAS Number 951322-11-5 Molecular Weight 357.71600
Density N/A Boiling Point N/A
Molecular Formula C16H22BrClN2 Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of Desformylflustrabromine hydrochloride


Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.

 Names

Name 2-[6-Bromo-2-(2-methyl-3-buten-2-yl)-1H-indol-3-yl]-N-methylethan amine hydrochloride (1:1)
Synonym More Synonyms

 Desformylflustrabromine hydrochloride Biological Activity

Description Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
Related Catalog
Target

α4β2 nAChR

In Vitro Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48[1]. ACh-induced currents are potentiated and inhibited by Desformylflustrabromine hydrochloride in the high sensitivity (HS) and low sensitivity (LS) isoform preparations, although Desformylflustrabromine hydrochloride displays a higher potency on the LS isoform (pEC50=6.4±0.2) compare with the HS isoform (pEC50=5.6±0.2). Desformylflustrabromine hydrochloride potentiates ACh-induced responses of wild-type receptors expressed using the HS isoform preparation maximally by 350±20%, which is similar to receptors expressed via the LS isoform preparation (350±30%)[2].
Kinase Assay Receptors expressed via the high sensitivity (HS) isoform preparation are evaluated for Desformylflustrabromine hydrochloride modulation by coapplication of 10 μM ACh with increasing concentrations of Desformylflustrabromine hydrochloride (0.001 to 100 μM). To compare responses from different oocytes, individual responses to Desformylflustrabromine hydrochloride application are normalized to the control responses elicited using either 10 or 100 μM ACh for receptors expressed by the HS or LS isoform preparations, respectively, for both wild-type and mutated receptors. Data are collected from at least four replicate experiments using oocytes obtained from at least two different frogs[2].
References

[1]. Nadezhda German, et al. Deconstruction of the α4β2 Nicotinic Acetylchloine (nACh) Receptor Positive Allosteric Modulator des-Formylflustrabromine (dFBr). J Med Chem. 2011 Oct 27;54(20):7259-67.

[2]. Weltzin MM, et al. Desformylflustrabromine Modulates α4β2 Neuronal Nicotinic Acetylcholine Receptor High- and Low-Sensitivity Isoforms at Allosteric Clefts Containing the β2 Subunit. J Pharmacol Exp Ther. 2015 Aug;354(2):184-94.

 Chemical & Physical Properties

Molecular Formula C16H22BrClN2
Molecular Weight 357.71600
Exact Mass 356.06500
PSA 27.82000
LogP 5.34880
Storage condition 2-8℃

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

N-Methyllidocaine iodide
Deformylflustrabromine hydrochloride
Desformylflustrabromine hydrochloride
6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride
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