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24003-58-5

24003-58-5 structure
24003-58-5 structure

Name QX-314 (bromide)
Synonyms Hepato-Scan
Lidofenin
2,6-dimethylacetanilideiminodiacetic acid
Ellipticine
Lidocaine N-ethyl bromide
Hida
Description QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker[1].
Related Catalog
Target

sodium channel[1]

In Vitro QX-314 bromide exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels (TRPV1) in vitro [1]. QX-314 bromide (1–60 mM) directly activates TRPV1 in a concentration-dependent manner[1]. QX-314 bromide (≥ 30 mM) produces oocyte membrane blackening and cell death [1]. QX-314 bromide inhibits calcium currents in hippocampal CA1 pyramidal neurons intracellular, and the low-threshold (T-type) Ca2+ currents are on average < 10% of control amplitude [3]. QX-314 bromide shifts the current-voltage relationships (I-Vs) in the positive voltage direction due to the presence of intracellular Br- [3].
In Vivo QX-314 bromide (1.6 mg/kg; i.c.) abolishes responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin[2]. Animal Model: Male Sprague-Dawley rats (250-290 g)[2] Dosage: 1.6 mg/kg Administration: Intracutaneous injection Result: Abolished responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin.
References

[1]. Rivera-Acevedo RE, et al. The quaternary lidocaine derivative, QX-314, exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels in vitro. Anesthesiology. 2011 Jun;114(6):1425-34.

[2]. Binshtok AM, et al. Coapplication of lidocaine and the permanently charged sodium channel blocker QX-314 produces a long-lasting nociceptive blockade in rodents. Anesthesiology. 2009 Jul;111(1):127-37.

[3]. Talbot MJ, et al. Intracellular QX-314 inhibits calcium currents in hippocampal CA1 pyramidal neurons. J Neurophysiol. 1996 Sep;76(3):2120-4.

Molecular Formula C16H27BrN2O
Molecular Weight 343.30200
Exact Mass 342.13100
PSA 29.10000
LogP 0.19540

~%

24003-58-5 structure

24003-58-5

Literature: Loefgren; Fischer Svensk Kemisk Tidskrift, 1946 , vol. 58, p. 219,229
Precursor  2

DownStream  0

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