Vanoxerine (Synonyms: GBR 12909; I893) |
| Katalog-Nr.GC13322 |
Vanoxerin (GBR-12909) ist ein kompetitiver, potenter und hochselektiver Dopamin-Wiederaufnahmehemmer (Ki=1 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 67469-69-6
Sample solution is provided at 25 µL, 10mM.
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Vanoxerine is an antagonist of dopamine transporter (DAT1) with Ki value of 16.9nM [1].
As an antagonist of DAT, vanoxerine is developed for treatment of Parkinson's disease and depression but has no effect on these diseases. Vanoxerine is also found to have desirable cardiac antiarrhythmic properties. It is a blocker of cardiac hERG (hKv11.1) with IC50 value of 0.84nM. It also blocks the ICa,L and hNav1.5 channel with IC50 values of 320nM and 830nM, respectively. Vanoxerine does not significantly prolong Purkinje fiber APD60 and APD90 and has no significant effect on QT or TDR. Further, the clinical trial demonstrates that the effective concentrations of vanoxerine are well tolerated and safe in man [2].
References:
[1] Giros B, el Mestikawy S, Godinot N, Zheng K, Han H, Yang-Feng T, Caron MG. Cloning, pharmacological characterization, and chromosome assignment of the human dopamine transporter. Mol Pharmacol. 1992 Sep;42(3):383-90.
[2] Lacerda AE, Kuryshev YA, Yan GX, Waldo AL, Brown AM. Vanoxerine: cellular mechanism of a new antiarrhythmic. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.
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