Buclizine free base | CAS#82-95-1 | antihistamine

Buclizine
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 591415

CAS#: 82-95-1 (free base)

Description: Buclizine is an antihistamine and anticholinergic of the diphenylmethylpiperazine group. It is considered to be an antiemetic, similar to meclizine.

Chemical Structure

Buclizine

CAS# 82-95-1 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 591415
Name: Buclizine
CAS#: 82-95-1 (free base)
Chemical Formula: C28H33ClN2
Exact Mass: 432.23
Molecular Weight: 433.040
Elemental Analysis: C, 77.66; H, 7.68; Cl, 8.19; N, 6.47

Price and Availability

Size	Price	Availability
250mg	USD 650	2 weeks
1g	USD 1450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 129-74-8 (HCl) 82-95-1 (free base)

Synonym: Buclizine; Histabutizine; Histabutyzine

IUPAC/Chemical Name: Piperazine, 1-((4-chlorophenyl)phenylmethyl)-4-((4-(1,1-dimethylethyl)phenyl)methyl)- (9CI)

InChi Key: MOYGZHXDRJNJEP-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H33ClN2/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

SMILES Code: CC(C1=CC=C(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)C=C1)(C)C

Appearance: 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

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 433.04 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Seo EJ, Fischer N, Efferth T. Role of TCTP for Cellular Differentiation and Cancer Therapy. Results Probl Cell Differ. 2017;64:263-281. doi: 10.1007/978-3-319-67591-6_14. PubMed PMID: 29149414.

2: Seo EJ, Efferth T. Interaction of antihistaminic drugs with human translationally controlled tumor protein (TCTP) as novel approach for differentiation therapy. Oncotarget. 2016 Mar 29;7(13):16818-39. doi: 10.18632/oncotarget.7605. PubMed PMID: 26921194; PubMed Central PMCID: PMC4941353.

3: Borukhova S, Noël T, Hessel V. Continuous-Flow Multistep Synthesis of Cinnarizine, Cyclizine, and a Buclizine Derivative from Bulk Alcohols. ChemSusChem. 2016 Jan 8;9(1):67-74. doi: 10.1002/cssc.201501367. Epub 2015 Dec 9. PubMed PMID: 26663906.

4: Kuminek G, Stulzer HK, Tagliari MP, Oliveira PR, Bernardi LS, Rauber GS, Cardoso SG. High-performance column liquid chromatographic method for the simultaneous determination of buclizine, tryptophan, pyridoxine, and cyanocobalamin in tablets and oral suspension. J AOAC Int. 2011 Nov-Dec;94(6):1785-90. PubMed PMID: 22320085.

5: Babu TA. Buclizine is back again! This time as a pediatric appetite stimulant. Indian J Pharmacol. 2011 Apr;43(2):219. doi: 10.4103/0253-7613.77383. PubMed PMID: 21572667; PubMed Central PMCID: PMC3081471.

6: Mostafa GA, Al-Badr AA. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33. doi: 10.1016/B978-0-12-387667-6.00001-4. Epub 2011 Jun 23. PubMed PMID: 22469258.

7: Arayne MS, Sultana N, Mirza AZ, Siddiqui FA. Simultaneous determination of gliquidone, fexofenadine, buclizine, and levocetirizine in dosage formulation and human serum by RP-HPLC. J Chromatogr Sci. 2010 May-Jun;48(5):382-5. PubMed PMID: 20515533.

8: Arayne MS, Sultana N, Siddiqui FA. Quantitation of buclizine hydrochloride in pharmaceutical formulations and human serum by RP-HPLC. Pak J Pharm Sci. 2006 Oct;19(4):326-9. PubMed PMID: 17105713.

9: El Walily AF, El Gindy A, Bedair MF. Application of first-derivative UV-spectrophotometry, TLC-densitometry and liquid chromatography for the simultaneous determination of mebeverine hydrochloride and sulpiride. J Pharm Biomed Anal. 1999 Nov;21(3):535-48. PubMed PMID: 10701420.

10: Fischer MJ, Paulussen JJ, Horbach DA, Roelofsen EP, van Miltenburg JC, de Mol NJ, Janssen LH. Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects. Inflamm Res. 1995 Feb;44(2):92-7. PubMed PMID: 7655991.

11: Adam EI. A treatment for the acute migraine attack. J Int Med Res. 1987 Mar-Apr;15(2):71-5. PubMed PMID: 3556262.

12: Behrendt WA, Cserepes J. Acute toxicity and analgesic action of a combination of buclizine, codeine and paracetamol ('Migraleve') in tablet and suppository form in rats. Pharmatherapeutica. 1985;4(5):322-31. PubMed PMID: 4070325.

13: Burgess HA, Merrington DM, Oliver WJ, Thomson A, Rogers HJ. The relative bioavailability of paracetamol after rectal administration of suppositories containing a mixture of paracetamol, codeine phosphate and buclizine hydrochloride in healthy volunteers. Curr Med Res Opin. 1985;9(9):634-41. PubMed PMID: 3902377.

14: Persaud N, Johnson ES, Merrington D, Oliver W. The relative bioavailability of paracetamol and codeine after oral administration of a combination of buclizine, paracetamol and codeine, with or without docusate, and of paracetamol alone in healthy volunteers. Curr Med Res Opin. 1985;9(9):626-33. PubMed PMID: 2414066.

15: Novack GD, Stark LG, Peterson SL. Anticonvulsant effects of benzhydryl piperazines on maximal electroshock seizures in rats. J Pharmacol Exp Ther. 1979 Mar;208(3):480-4. PubMed PMID: 34712.

16: Jorgensen PB, Weightman D, Foster JB. Comparison of migraleve and buclizine in prophylaxis of migraine. Curr Ther Res Clin Exp. 1974 Dec;16(12):1276-80. PubMed PMID: 4218156.

17: Kulkarni SD, Joglekar GV, Balwani JH. Anabolic activity of buclizine on rats. Eur J Pharmacol. 1972 Feb;17(2):312-4. PubMed PMID: 4402100.

18: Hermans W. [Clinical evaluation of buclizine for underweight patients]. Brux Med. 1971 Apr;51(4):295-8. French. PubMed PMID: 4931282.

19: Bormans A. [Double-blind study of the eutrophic effect of buclizine on children]. Brux Med. 1971 Apr;51(4):291-3. French. PubMed PMID: 4931281.

20: Lamy F. [Appetite stimulation and weight increase with buclizine]. Brux Med. 1971 Apr;51(4):287-90. French. PubMed PMID: 4931280.

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