| CAS |
67469-78-7 |
| Chinese Name |
伐诺司林二盐酸盐 |
| English Name |
Vanoxerine Dihydrochloride |
| Synonyms |
GBR-12909;I893 dihydrochloride |
| Molecular Formula |
C28H34Cl2F2N2O |
| Molecular Weight |
523.49 |
| Solubility |
Soluble in Water/DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00055193 |
| SMILES |
C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl |
| InChIKey |
MIBSKSYCRFWIRU-UHFFFAOYSA-N |
| InChI |
InChI=1S/C28H32F2N2O.2ClH/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;2*1H |
| PubChem CID |
104920 |
| Target Point |
Dopamine Transporter |
| Passage |
Neuronal Signaling;Membrane Transporter&Ion Channel |
| Background |
It is a competitive, highly selective inhibitor of dopamine reuptake that binds to a target on the dopamine transporter (DAT). |
| Biological Activity |
Vanoxerine Dihydrochloride 是一种竞争性、强效、高选择性多巴胺再摄取抑制剂（Ki=1 nM），可与多巴胺转运体（DAT）上的靶点结合。[1-2] |
| In Vitro |
Vanoxerine dihydrochloride(GBR 12909)was a potent and selective inhibitor of synaptosomal dopamine uptake(KI = 1 nM)，with a 20-fold lower affinity for the histamine H1-receptor and a more than 100-fold affinity for the noradrenaline and 5-HT uptake carriers，the dopamine D-1，D-2，5-HT2，5-HT1A and alpha 1-receptors and voltage-dependent sodium channels. GBR 12909(3 microM)was without effect on muscarinic，alpha 2，beta 1 + 2，gamma-aminobutyric acid(GABA)and benzodiazepine receptors，and on choline and GABA uptake carriers.[2] |
| In Vivo |
The single administration of over 10 mg/kg of vanoxerine dihydrochloride(GBR)，i.p. and p.o.，significantly increased the ambulatory activity. The repeated administration of GBR，at only 10 mg/kg，produced a reverse tolerance to its ambulation-increasing effect. A cross-reverse tolerance was induced between GBR(10 and 20 mg/kg)and methamphetamine(2 mg/kg)in both directions.[1] |
| Data Literature Source |
[1]. Hirate K，et al. Characteristics of the ambulation-increasing effect of GBR-12909，a selective dopamine uptake inhibitor，in mice. Jpn J Pharmacol. 1991 Apr;55(4):501-11.
[2]. Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. 1989 Aug 3;166(3):493-504. |
| Unit |
Bottle |
| Specification |
10mg |
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