Vanoxerine HCl
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MedKoo CAT#: 531328

CAS#: 67469-78-7 (HCl)

Description: Vanoxerine, also known as GBR 12909, is a potent inhibitor that blocks dopamine uptake (IC50 = 1-51 nM). GBR 12909 effectively inhibits dopamine uptake in vivo. GBR-12909 binds to the target site on the dopamine transporter (DAT) ~ 50 times more strongly than cocaine, but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels, giving vanoxerine only mild stimulant effects.[2] Vanoxerine has also been observed to be a potent blocker of the IKr (hERG) channel. GBR-12909 also binds with nanomolar affinity to the serotonin transporter.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 2 Weeks
25mg USD 250 2 Weeks
50mg USD 450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-07-07. Prices are subject to change without notice.

Vanoxerine HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 531328
Name: Vanoxerine HCl
CAS#: 67469-78-7 (HCl)
Chemical Formula: C28H34Cl2F2N2O
Exact Mass: 522.2016
Molecular Weight: 523.4898
Elemental Analysis: C, 64.24; H, 6.55; Cl, 13.54; F, 7.26; N, 5.35; O, 3.06


Related CAS #: 67469-69-9 (free base)   67469-78-7 (HCl)    

Synonym: Vanoxerine dihydrochloride; GBR 12909; GBR-12909; GBR12909.

IUPAC/Chemical Name: 1-(2-[bis(4-Fluorophenyl)methoxy]ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride

InChi Key: MIBSKSYCRFWIRU-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[H]Cl.[H]Cl


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Lane EL, Cheetham S, Jenner P. Dopamine uptake inhibitor-induced rotation in 6-hydroxydopamine-lesioned rats involves both D1 and D2 receptors but is modulated through 5-hydroxytryptamine and noradrenaline receptors. J Pharmacol Exp Ther. 2005 Mar;312(3):1124-31. PubMed PMID: 15542624.

2: Mike A, Karoly R, Vizi ES, Kiss JP. A novel modulatory mechanism of sodium currents: frequency-dependence without state-dependent binding. Neuroscience. 2004;125(4):1019-28. PubMed PMID: 15120861.

3: Choong KC, Shen RY. Methylphenidate restores ventral tegmental area dopamine neuron activity in prenatal ethanol-exposed rats by augmenting dopamine neurotransmission. J Pharmacol Exp Ther. 2004 May;309(2):444-51. PubMed PMID: 14724217.

4: Rahman S, Engleman E, Simon J, McBride WJ. Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 dopamine uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44. PubMed PMID: 11230993.

5: Romualdi P, D'Addario C, Ferri S, Cox BM, Izenwasser S. Chronic GBR 12909 administration differentially alters prodynorphin gene expression compared to cocaine. Eur J Pharmacol. 2001 Feb 16;413(2-3):207-12. PubMed PMID: 11226394.

6: Howell LL, Czoty PW, Kuhar MJ, Carrol FI. Comparative behavioral pharmacology of cocaine and the selective dopamine uptake inhibitor RTI-113 in the squirrel monkey. J Pharmacol Exp Ther. 2000 Feb;292(2):521-9. PubMed PMID: 10640288.

7: Mochizuki T, Villemagne VL, Scheffel U, Liu X, Musachio JL, Dannals RF, Wagner HN Jr. A simple probe measures the pharmacokinetics of[125I]RTI-55 in mouse brain in vivo. Eur J Pharmacol. 1997 Oct 29;338(1):17-23. PubMed PMID: 9407999.

8: Nagase T, Hotta K, Morita S, Sakai K, Yamane M, Omote M, Mizusawa H. [Pharmacological effects of the novel dopamine uptake inhibitor 1-[2-[bis(4-fluorophenyl)-methoxy]ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride (I-893) on the central nervous system]. Nihon Yakurigaku Zasshi. 1991 Aug;98(2):121-41. Japanese. PubMed PMID: 1833294.

9: Mount H, Boksa P, Chaudieu I, Quirion R. Phencyclidine and related compounds evoked [3H]dopamine release from rat mesencephalic cell cultures by a mechanism independent of the phencyclidine receptor, sigma binding site, or dopamine uptake site. Can J Physiol Pharmacol. 1990 Sep;68(9):1200-6. PubMed PMID: 1980428.

10: Nagase T, Ishiko J, Takaori S. [Effects of 1-[2-[bis(fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride (I-893) on turnover of dopamine and norepinephrine in the brain]. Nihon Yakurigaku Zasshi. 1987 Aug;90(2):105-14. Japanese. PubMed PMID: 3119439.