[CAS NO. 67469-78-7] Vanoxerinedihydrochloride

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PRODUCTS SPECIFICATIONS [67469-78-7]

Catalog

HY-13217

Brand

MCE

CAS

67469-78-7

DESCRIPTION [67469-78-7]

Overview

MDL	MFCD00055193
Molecular Weight	523.49
Molecular Formula	C28H34Cl2F2N2O
SMILES	FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[2HCl]

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor ( K _i =1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT) ^[1] .

IC50 & Target

Ki: 1 nM (dopamine reuptake) ^[1]

In Vitro

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) inhibits the uptake of dopamlne (DA), with an IC ₅₀ in the low nanomolar range, and is several-fold less potent as inhibitors of the uptake of noradrenaline and 5-HT ^[2] .
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vanoxerine dihydrochloride (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male mice (ddY strain at 6 weeks of age) ^[3]
Dosage:	2.5, 5, 10, 20 mg/kg
Administration:	Intraperitoneal injection
Result:	The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01691313	Laguna Pharmaceuticals, Inc.	Symptomatic Atrial Fibrillation\|Atrial Flutter	November 2012	Phase 2
NCT00089687	National Institute on Drug Abuse (NIDA)	Cocaine-Related Disorders	April 2004	Phase 1
NCT00100113	National Institute on Drug Abuse (NIDA)	Cocaine-Related Disorders	June 2004	Phase 1
NCT00218049	National Institute on Drug Abuse (NIDA)\|University of Texas	Cocaine Abuse\|Cocaine-Related Disorders	December 2004	Phase 1
NCT02454283	Laguna Pharmaceuticals, Inc.	Atrial Fibrillation or Flutter	September 2015	Phase 3
NCT00051896	National Institute on Drug Abuse (NIDA)	Cocaine-Related Disorders	August 2002	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 9.4 mg/mL ( 17.96 mM ; Need ultrasonic and warming)

H ₂ O : 1 mg/mL ( 1.91 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9103 mL	9.5513 mL	19.1026 mL
5 mM	0.3821 mL	1.9103 mL	3.8205 mL
10 mM	0.1910 mL	0.9551 mL	1.9103 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Piperazine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)-, hydrochloride (1:2)

Piperazine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)-, dihydrochloride

GBR 12909

I 893

Vanoxerine dihydrochloride

1-(2-(Bis(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride