Home >> Research Area >>GPCR/G protein>>Adrenergic Transporters>> Bicifadine hydrochloride

Bicifadine hydrochloride

Noradrenalin, 5-HT and dopamine re-uptake inhibitor CAS# 66504-75-4

Bicifadine hydrochloride

Catalog No. BCC7925----Order now to get a substantial discount!

Product Name & Size Price Stock
Bicifadine hydrochloride: 5mg $115 In Stock
Bicifadine hydrochloride: 10mg Please Inquire In Stock
Bicifadine hydrochloride: 20mg Please Inquire Please Inquire
Bicifadine hydrochloride: 50mg Please Inquire Please Inquire
Bicifadine hydrochloride: 100mg Please Inquire Please Inquire
Bicifadine hydrochloride: 200mg Please Inquire Please Inquire
Bicifadine hydrochloride: 500mg Please Inquire Please Inquire
Bicifadine hydrochloride: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Bicifadine hydrochloride

Number of papers citing our products

Chemical structure

Bicifadine hydrochloride

3D structure

Chemical Properties of Bicifadine hydrochloride

Cas No. 66504-75-4 SDF Download SDF
PubChem ID 47952 Appearance Powder
Formula C12H16ClN M.Wt 209.72
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane;hydrochloride
SMILES CC1=CC=C(C=C1)C23CC2CNC3.Cl
Standard InChIKey OTZOPAFTLUOBOM-UHFFFAOYSA-N
Standard InChI InChI=1S/C12H15N.ClH/c1-9-2-4-10(5-3-9)12-6-11(12)7-13-8-12;/h2-5,11,13H,6-8H2,1H3;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Bicifadine hydrochloride

DescriptionPotent antagonist of the noradrenalin transporter (IC50 = 55 nM); also displays antagonist activity at the 5-HT and dopamine transporters (IC50 values are 117 nM and 910 nM respectively). Orally active. Exhibits antinociceptive and antiallodynic activity in rodent models of acute, persistent, and chronic pain.

Bicifadine hydrochloride Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Bicifadine hydrochloride Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Bicifadine hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.7683 mL 23.8413 mL 47.6826 mL 95.3652 mL 119.2066 mL
5 mM 0.9537 mL 4.7683 mL 9.5365 mL 19.073 mL 23.8413 mL
10 mM 0.4768 mL 2.3841 mL 4.7683 mL 9.5365 mL 11.9207 mL
50 mM 0.0954 mL 0.4768 mL 0.9537 mL 1.9073 mL 2.3841 mL
100 mM 0.0477 mL 0.2384 mL 0.4768 mL 0.9537 mL 1.1921 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on Bicifadine hydrochloride

The oral analgesic efficacy of bicifadine hydrochloride in postoperative pain.[Pubmed:7096604]

J Clin Pharmacol. 1982 Apr;22(4):160-4.

The analgesic efficacy of 75 and 150 mg Bicifadine hydrochloride was compared to 650 mg aspirin and placebo in a double-blind, single-dose study. Oral doses were administered to 100 patients suffering from moderate to severe postoperative pain. Significant analgesic activity was demonstrated with 650 mg aspirin and 150 mg bicifadine as compared to 75 mg bicifadine or placebo. No significant treatment difference was found between 75 mg bicifadine and placebo. Side effects were minor and did not interfere with the course of therapy.

Determination of the polymorphic forms of bicifadine hydrochloride by differential scanning calorimetry-thermogravimetric analysis, X-ray powder diffraction, attenuated total reflectance-infrared spectroscopy, and attenuated total reflectance-near-infrared spectroscopy.[Pubmed:16316514]

Appl Spectrosc. 2005 Nov;59(11):1365-71.

The pharmaceutical compound Bicifadine hydrochloride, which has been found to crystallize in two polymorphic forms, has been characterized by thermal analysis, X-ray powder diffraction (XRPD), infrared (IR) spectroscopy, and near-infrared (NIR) spectroscopy. A series of 22 sample mixtures of polymorph 1 and polymorph 2 were prepared and calibration models for the quantitation of these binary mixtures have been developed for each of the XRPD, attenuated total reflectance (ATR)-IR, and ATR-NIR analytical techniques. The quantitative results were obtained using a partial least squares (PLS) algorithm, which predicted the concentration of polymorph 1 from the XRPD spectra with a root mean standard error of prediction (RMSEP) of 4.4%, from the IR spectra with a RMSEP of 3.8%, and from the NIR spectra with a RMSEP of 1.4%. The studies indicate that when analyses are carried out on equivalent sets of spectra, NIR spectroscopy offers significant advantages in quantitative accuracy as a tool for the determination of polymorphs in the solid state and is also more convenient to use than both the ATR-IR and XRPD methods. Density functional theory (DFT) B3LYP calculations and IR spectral simulation have been used to determine the nature of the vibrational modes that are the most sensitive in the analysis.

Characterization of the antinociceptive actions of bicifadine in models of acute, persistent, and chronic pain.[Pubmed:17325229]

J Pharmacol Exp Ther. 2007 Jun;321(3):1208-25.

Bicifadine (1-p-tolyl-3-azabicyclo[3.1.0]hexane) inhibits monoamine neurotransmitter uptake by recombinant human transporters in vitro with a relative potency of norepinephrine > serotonin > dopamine (approximately 1:2:17). This in vitro profile is supported by microdialysis studies in freely moving rats, where bicifadine (20 mg/kg i.p.) increased extrasynaptic norepinephrine and serotonin levels in the prefrontal cortex, norepinephrine levels in the locus coeruleus, and dopamine levels in the striatum. Orally administered bicifadine is an effective antinociceptive in several models of acute, persistent, and chronic pain. Bicifadine potently suppressed pain responses in both the Randall-Selitto and kaolin models of acute inflammatory pain and in the phenyl-p-quinone-induced and colonic distension models of persistent visceral pain. Unlike many transport inhibitors, bicifadine was potent and completely efficacious in both phases of the formalin test in both rats and mice. Bicifadine also normalized the nociceptive threshold in the complete Freund's adjuvant model of persistent inflammatory pain and suppressed mechanical and thermal hyperalgesia and mechanical allodynia in the spinal nerve ligation model of chronic neuropathic pain. Mechanical hyperalgesia was also reduced by bicifadine in the streptozotocin model of neuropathic pain. Administration of the D(2) receptor antagonist (-)-sulpiride reduced the effects of bicifadine in the mechanical hyperalgesia assessment in rats with spinal nerve ligations. These results indicate that bicifadine is a functional triple reuptake inhibitor with antinociceptive and antiallodynic activity in acute, persistent, and chronic pain models, with activation of dopaminergic pathways contributing to its antihyperalgesic actions.

1-Aryl-3-azabicyclo[3.1.0]hexanes, a new series of nonnarcotic analgesic agents.[Pubmed:7241504]

J Med Chem. 1981 May;24(5):481-90.

A series of 1-aryl-3-azabicyclo[3.1.0]hexanes was synthesized by hydride reduction of 1-arylcyclopropanedicarboximides. Hydroxyphenyl analogues 20, 22, and 24 were prepared by EtSNa--DMF ether cleavage of the corresponding methoxyphenyl analogues 2m, 2n, and 23, respectively, with the secondary amines 20 and 22 going through the N-formyl intermediate 19 and 21. The p-ethoxy analogue 26 was obtained by O-ethylation of 19, followed by base hydrolysis of the amide 25. The greatest analgesic potency in mouse writhing and rat paw-pain assays was observed for para-substituted compounds. Bicifadine, 1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane (2b), was the most potent member of the series and is presently undergoing clinical trials in man. Analgesic activity of 2b is limited to the (+) enantiomer 2v, which has the 1R,5S absolute configuration as determined by single-crystal X-ray analysis. The N-methyl analogue (27d) of 2b showed significant analgesic potency, whereas the N-allyl (27a), N-(cyclopropylmethyl) (27b), and N-(n-hexyl) (27c) analogues were inactive. Bicifadine (2b) showed a nonnarcotic profile different from analogous azabicycloalkane and 3-phenylpyrrolidine analgesics.

Keywords:

Bicifadine hydrochloride,66504-75-4,Natural Products,Adrenergic Transporters, buy Bicifadine hydrochloride , Bicifadine hydrochloride supplier , purchase Bicifadine hydrochloride , Bicifadine hydrochloride cost , Bicifadine hydrochloride manufacturer , order Bicifadine hydrochloride , high purity Bicifadine hydrochloride

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: