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:
Inquire
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
Bulk Inquiry
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:
Inquire
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).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Histamine Receptor Products


CAS 523-87-5 Dramamine

Dramamine
(CAS: 523-87-5)

Dimenhydrinate is an over-the-counter antiemetic used to prevent nausea and motion sicknes composed of 8-Chlorotheophylline and Diphenhydramine.

CAS 108612-45-9 Mizolastine

Mizolastine
(CAS: 108612-45-9)

Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic r...

CAS 362665-56-3 Tiprolisant

Tiprolisant
(CAS: 362665-56-3)

Tiprolisant is potent and selective nonimidazole inverse agonist at the histamine H3 receptor. (Ki=0.16 nM).

CAS 459168-41-3 JNJ-7777120

JNJ-7777120
(CAS: 459168-41-3)

JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other h...

CAS 639089-06-8 VUF 5681 dihydrobromide

VUF 5681 dihydrobromide
(CAS: 639089-06-8)

VUF 5681 dihydrobromide is a potent histamine H3 receptor silent antagonist (pKi = 8.35).

CAS 77-38-3 Chlorphenoxamine

Chlorphenoxamine
(CAS: 77-38-3)

Chlorphenoxamine is an analog of diphenhydramine. It has antimuscarinic and antihistaminic properties. It has been used as an antipruritic and antiparkinsonian ...

CAS 56897-53-1 Carcinine ditrifluoroacetate

Carcinine ditrifluoroacetate
(CAS: 56897-53-1)

The ditrifluoroacetate salt form of Carcinine, which is a highly selective histamine H3 receptor antagonist and could act as a natural antioxidant.

CAS 68-88-2 Hydroxyzine

Hydroxyzine
(CAS: 68-88-2)

Hydroxyzine is a histamine H1-receptor antagonist.

CAS 140873-26-3 Aminopotentidine

Aminopotentidine
(CAS: 140873-26-3)

Aminopotentidine is a high selectivity and high affinity histamine H2 receptor antagonist. Its KB values are 220 and 280 nM at human and guinea pig H2 receptors...

CAS 129-74-8 Buclizine hydrochloride

Buclizine hydrochloride
(CAS: 129-74-8)

Buclizine hydrochloride is an antihistamine and anticholinergic of the piperazine derivative family.

CAS 1229-35-2 METHDILAZINE HYDROCHLORIDE (200 MG)

METHDILAZINE HYDROCHLORIDE (200 MG)
(CAS: 1229-35-2)

This active molecular is a first-generation antihistamine and belongs to phenothiazine class. Methdilazine Hydrochloride is a Histamine H1 receptor antagonist w...

CAS 10500-82-0 Famotine hydrochloride

Famotine hydrochloride
(CAS: 10500-82-0)

Famotine hydrochloride is a histamine H2 receptor antagonist. lt has no effect on the cytochrome P450 enzyme system, and does not appear to interact with other ...

CAS 720690-73-3 GSK 189254A

GSK 189254A
(CAS: 720690-73-3)

GSK-189,254 is a H3 histamine receptor inverse agonist. It has subnanomolar affinity for the H3 receptor with Ki of 0.2nM. It possesses stimulant and nootropic ...

CAS 195867-54-0 HTMT dimaleate

HTMT dimaleate
(CAS: 195867-54-0)

HTMT dimaleate is a histamine H1 and H2 receptor agonist with 4x104 fold activity over histamine in H2-mediated effects in natural suppressor cells. HTMT dimale...

CAS 103294-47-9 LY-150310

LY-150310
(CAS: 103294-47-9)

LY-150310 is a histamine H1-receptor antagonist. It could alter prostanoid concentrations in vitro and in vivo.

CAS 58-73-1 Diphenhydramine

Diphenhydramine
(CAS: 58-73-1)

Diphenhydramine is a histamine H1 antagonist. t competitively inhibits the histamine-1 (H1) receptor, thereby alleviating the symptoms caused by endogenous hist...

CAS 154-69-8 Tripelennamine hydrochloride

Tripelennamine hydrochloride
(CAS: 154-69-8)

Tripelennamine hydrochloride, the hydrochloride salt form of tripelennamine, is a blood-brain barrier penetrant and orally active H1-receptor antagonist. Tripel...

CAS 135-87-5 Piperoxane hydrochloride

Piperoxane hydrochloride
(CAS: 135-87-5)

Piperoxan is an antihistamine drug which is derived from benzodioxan. At first it was investigated by Fourneau as an α-adrenergic-blocking agent, then they foun...

CAS 84545-30-2 ICI 162,846

ICI 162,846
(CAS: 84545-30-2)

ICI 162,846 is a potent histamine H2 receptor antagonist.

CAS 13073-96-6 Decloxizine hydrochloride

Decloxizine hydrochloride
(CAS: 13073-96-6)

The hydrochloride salt form of Decloxizine, a hydroxyzine analogue, is a histamine 1 receptor antagonist and often known as an impurity of Hydroxyzine.

Chemical Structure

CAS 129-74-8 Buclizine hydrochloride

Quick Inquiry

Verification code

Featured Items