Buclizine hydrochloride - CAS 129-74-8
Catalog number: B0084-056872
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H35Cl3N2
Molecular Weight:
505.952
COA:
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Targets:
Histamine Receptor
Description:
Buclizine hydrochloride is an antihistamine and anticholinergic of the piperazine derivative family.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-056872 1 g $199 In stock
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Purity:
> 98%
Related CAS:
129-74-8 (free base)
Appearance:
White to Off-white Solid
Synonyms:
Buclizine dihydrochloride; 1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride
MSDS:
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Melting Point:
230-240°C
InChIKey:
SDBHDSZKNVDKNU-UHFFFAOYSA-N
InChI:
InChI=1S/C28H33ClN2.2ClH/c1-28(2,3)25-13-9-22(10-14-25)21-30-17-19-31(20-18-30)27(23-7-5-4-6-8-23)24-11-15-26(29)16-12-24;;/h4-16,27H,17-21H2,1-3H3;2*1H
Canonical SMILES:
CC(C)(C)C1=CC=C(C=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl.Cl.Cl
1.Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects.
Fischer MJ1, Paulussen JJ, Horbach DA, Roelofsen EP, van Miltenburg JC, de Mol NJ, Janssen LH. Inflamm Res. 1995 Feb;44(2):92-7.
In a model for mucosal mast cells (RBL-2H3 cells) a set H1-antagonist derived anti-allergic drugs containing a diphenylmethyl piperazinyl moiety was examined for their ability to inhibit release of the mediator beta-hexosaminidase. Cells were activated with antigen or the calcium ionophore A23187, whether or not in combination with the phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA). Oxatomide, hydroxyzine and cetirizine inhibit the antigen induced beta-hexosaminidase release. The release triggered by A23187, whether or not in combination with TPA is hardly influenced by the compounds. A biphasic dependence of the inhibition of exocytosis in RBL cells on lipophilicity is observed with the optimum at log P is 5-6. The extremely lipophilic compounds meclozine and buclizine are not active in this model. pH dependence of the effect of the drugs shows that especially the uncharged species are active in inhibiting exocytosis. The investigated compounds show an effect on phase transitions in L-alpha-phosphatidylcholine dipalmitoyl liposomes as assayed with differential scanning calorimetry (DSC).
2.Quantitation of buclizine hydrochloride in pharmaceutical formulations and human serum by RP-HPLC.
Arayne MS1, Sultana N, Siddiqui FA. Pak J Pharm Sci. 2006 Oct;19(4):326-9.
An isocratic reversed phase high-performance liquid chromatographic (HPLC) method with ultraviolet detection at 230 nm has been developed for the determination of buclizine hydrochloride in human serum and dosage formulation. Methylparaben was successfully used as an internal standard. Good chromatographic separation between buclizine and internal standard peaks was achieved by using a stainless steel analytical column Nucleosil, C18 (10 microm, 25 cm x 0.46 cm). The system was operated at room temperature using a mobile phase consisting of acetonitrile-water (1:1) (pH 2.6) with phosphoric acid 85% at a flow rate of 2 ml/min. The calibration curve for buclizine hydrochloride in human serum was linear over the tested concentration range of 10, 3, 1.5, 0.5, 0.15, 0.05, and 0.025 microg/ml with a correlation coefficient of 0.9999. The intra- and inter-run precision and accuracy results were 98.07 to 100.34. The proposed method was validated for selectivity, linearity, accuracy, and precision.
3.Buclizine.
Mostafa GA, Al-Badr AA. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33. doi: 10.1016/B978-0-12-387667-6.00001-4. Epub 2011 Jun 23.
A comprehensive profile on buclizine hydrochloride, the piperazine derivative which is a sedating antihistamine with antimuscarinic and moderate sedative action and used mainly for its antiemetic effect in the prevention of motion sickness and migraine, is prepared. This profile contains the following sections: description, uses and applications, methods of preparation, physical characteristics, methods of analysis and stability. The physical characteristics section includes solubility, melting range, X-ray powder diffraction pattern, ultraviolet/visible spectroscopy, infrared spectroscopy, proton and carbon-13 nuclear magnetic resonance spectrometry, and mass spectrometry. Methods of analysis section includes compendial BP methods, spectrophotometry, potentiometry, and chromatography (TLC, GC, HPLC).
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Chemical Structure

CAS 129-74-8 Buclizine hydrochloride

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