Date published: 2025-9-25

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GBR-12909 (CAS 67469-78-7)

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Alternate Names:
Vanoxerine dihydrochloride;1-(2-(bis-(4-Fluorophenyl)methoxy)ethyl)-4-(3-phenyl-2-propyl)piperazine 2HCl
Application:
GBR-12909 is a potent dopamine transport blocker studied extensively in rats
CAS Number:
67469-78-7
Purity:
≥98%
Molecular Weight:
523.49
Molecular Formula:
C28H32F2N2O•2HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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GBR-12909 is a potent dopamine transport blocker studied extensively in rats. By inhibiting DAT function, GBR-12909 was able to induce a bipolar disorder mania-like phenotypes in mice. Also shown to cause postnatal changes to produce useful ADHD animal models. GBR-12909 caused an increase in core body temperature when administered to serotonin transporter knockout mice. Reportedly mimics cocaine-mediated enhancement of Tat neurotoxicity in rat midbrain primary cell cultures. Analogs of GBR-12909 continue to be investigated for cocaine addiction treatments.


GBR-12909 (CAS 67469-78-7) References

  1. Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).  |  Zhang, Y., et al. 2000. J Med Chem. 43: 4840-9. PMID: 11123994
  2. Interleukin-2 potentiates novelty- and GBR 12909-induced exploratory activity.  |  Zalcman, SS. 2001. Brain Res. 899: 1-9. PMID: 11311862
  3. Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.  |  Zhang, Y., et al. 2001. J Med Chem. 44: 3937-45. PMID: 11689080
  4. Interaction between a hydroxypiperidine analogue of 4-(2-benzhydryloxy-ethyl)-1-(4-fluorobenzyl)piperidine and Aspartate 68 in the human dopamine transporter.  |  Zhen, J., et al. 2004. Eur J Pharmacol. 506: 17-26. PMID: 15588620
  5. Synthesis of dopamine transporter selective 3-diarylmethoxymethyl-8-arylalkyl-8-azabicyclo[3.2.1]octane derivatives.  |  Zhang, S., et al. 2006. Bioorg Med Chem. 14: 7943-52. PMID: 16905323
  6. Imipramine as a discriminative stimulus.  |  Zhang, L. and Barrett, JE. 1991. J Pharmacol Exp Ther. 259: 1088-93. PMID: 1762063
  7. Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction.  |  Rothman, RB., et al. 2008. Biochem Pharmacol. 75: 2-16. PMID: 17897630
  8. Different effects of selective dopamine uptake inhibitors, GBR 12909 and WIN 35428, on HIV-1 Tat toxicity in rat fetal midbrain neurons.  |  Aksenov, MY., et al. 2008. Neurotoxicology. 29: 971-7. PMID: 18606182
  9. Behavioural characterisation of the effects of acute and repeated administration of GBR 12909 in rats: further evaluation of a potential model of ADHD.  |  Hewitt, KN., et al. 2009. Neuropharmacology. 57: 678-86. PMID: 19699754
  10. GBR 12909 administration as a mouse model of bipolar disorder mania: mimicking quantitative assessment of manic behavior.  |  Young, JW., et al. 2010. Psychopharmacology (Berl). 208: 443-54. PMID: 20020109
  11. 3,4-Methylenedioxymethamphetamine, mephedrone, and β-phenylethylamine release dopamine from the cytoplasm by means of transporters and keep the concentration high and constant by blocking reuptake.  |  Zsilla, G., et al. 2018. Eur J Pharmacol. 837: 72-80. PMID: 30172789
  12. TRH Analog, Taltirelin Improves Motor Function of Hemi-PD Rats Without Inducing Dyskinesia via Sustained Dopamine Stimulating Effect.  |  Zheng, C., et al. 2018. Front Cell Neurosci. 12: 417. PMID: 30555300
  13. Discovery of vanoxerine dihydrochloride as a CDK2/4/6 triple-inhibitor for the treatment of human hepatocellular carcinoma.  |  Zhu, Y., et al. 2021. Mol Med. 27: 15. PMID: 33579185

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GBR-12909, 5 mg

sc-200398
5 mg
$64.00

GBR-12909, 25 mg

sc-200398A
25 mg
$188.00