Vanoxerine - CAS 67469-69-6
Catalog number: 67469-69-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C28H32F2N2O
Molecular Weight:
450.56
COA:
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Targets:
Dopamine Reuptake Inhibitor
Description:
Vanoxerine is a is a potent and selective DRI acts to block cardiac ion channels.
Purity:
≥98%
Appearance:
Solid Powder
Synonyms:
1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine; GBR-12909; I-893;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
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Application:
DAT1 antagonist
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
NAUWTFJOPJWYOT-UHFFFAOYSA-N
InChI:
1S/C28H32F2N2O/c29-26-12-8-24(9-13-26)28(25-10-14-27(30)15-11-25)33-22-21-32-19-17-31(18-20-32)16-4-7-23-5-2-1-3-6-23/h1-3,5-6,8-15,28H,4,7,16-22H2
Canonical SMILES:
C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
Current Developer:
Gist-Brocades
1.Kinetic mechanism of dopamine transporter interaction with 1-(2-(bis-(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)piperazine (GBR 12909).
Stepanov V1, Järv J. Neurochem Int. 2008 Dec;53(6-8):370-3. doi: 10.1016/j.neuint.2008.09.005. Epub 2008 Sep 18.
Interaction of piperazine-based dopamine transporter inhibitor GBR12909 with rat dopamine transporters has been studied by means of competition kinetics analysis, employing [(3)H]PE2I as the reporter ligand. It has been found that GBR12909 is capable of inducing so-called "slow isomerization step" upon binding to DAT, probably consisting of a conformational change in the transporter protein. The mechanism exhibited by GBR12909 appears to be similar to the mechanism of PE2I that has been reported earlier and also confirms previous observations for GBR12783 made by Do-Rego and co-workers using dopamine uptake data. It appears that the isomerization phenomenon previously described for PE2I is not limited to tropane-based DAT inhibitors, but is, in fact, a general property of dopamine transporter protein, similar to "isomerization" process reported previously for G-protein coupled receptors. The rapid first step of association of the GBR 12909 is characterized by the equilibrium constant K(L)=34+/-11nM and the second slow step by k(i)=0.
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