Introduction：Basic information about CAS 82-95-1|Buclizine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Buclizine |
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| CAS Number | 82-95-1 | Molecular Weight | 433.02800 |
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| Density | / | Boiling Point | / |
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| Molecular Formula | C28H33ClN2 | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | buclizine |
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| Synonym | More Synonyms |
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Buclizine BiologicalActivity
| Description | Buclizine is an orally active antihistamine antiallergic compound. Buclizine is a potent teratogen in the rat and shows anti-tumor activity[1][2][3]. |
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| Related Catalog | Research Areas >>CancerSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
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| In Vitro | Buclizine (0.1-100 μM; 72 h) inhibits growth of MCF-7 cells[2]. Buclizine (9.625-77 μM; 72 h) arrests the cell cycle in the G1 phase in a dose-dependent manner[2]. Buclizine (0-75 μM; 72 h) decreases TCTP (translationally controlled tumor protein) and cell cycle regulatory proteins expression in MCF-7 cells, increases pro-apoptotic MCL-1S expression[2]. Cell Proliferation Assay[2] Cell Line: MCF-7 cells Concentration: 0-100 μM Incubation Time: 72 hours Result: Showed considerable growth inhibition (IC50=19.18 μM). Cell Cycle Analysis[2] Cell Line: MCF-7 cells Concentration: 9.625, 19.25, 38.5, and 77 μM Incubation Time: 72 hours Result: Increased the percentages of cells in the G1 phase to 73% at 77 μM. Western Blot Analysis[2] Cell Line: MCF-7 cells Concentration: 0-75 μM Incubation Time: 72 hours Result: Decreased TCTP expression by 40% at 75 μM. Decreased cyclin D1, cyclin D3, CDK2 and CDK4 expression after 72 h. |
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| In Vivo | Buclizine dihydrochloride (30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation) shows potent teratogens in the rat[3]. Animal Model: Eighty-seven mature female rats weighing 240±20 grams[3] Dosage: 30, 40, 60, 100, and 200 mg/kg Administration: 30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation Result: Resulted in malformations in 100% of the young at a dose level of 60-100 mg/kg. |
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| References | [1]. Gamal A E Mostafa, et al. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33. [2]. Ean-Jeong Seo, et al. 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. [3]. C T King, et al. Teratogenic effect of buclizine and hydroxyzine in the rat and chlorcyclizine in the mouse. Am J Obstet Gynecol. 1966 May 1;95(1):109-11. |
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Chemical & Physical Properties
| Molecular Formula | C28H33ClN2 |
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| Molecular Weight | 433.02800 |
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| Exact Mass | 432.23300 |
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| PSA | 6.48000 |
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| LogP | 6.42050 |
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| InChIKey | MOYGZHXDRJNJEP-UHFFFAOYSA-N |
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| SMILES | CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 |
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| Storage condition | 2-8°C |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- TL0260000
- CHEMICAL NAME :
- Piperazine, 1-(p-tert-butylbenzyl)-4-(p-chloro-alpha-phenylbenzyl )-
- CAS REGISTRY NUMBER :
- 82-95-1
- BEILSTEIN REFERENCE NO. :
- 0349567
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 1
- MOLECULAR FORMULA :
- C28-H33-Cl-N2
- MOLECULAR WEIGHT :
- 433.08
- WISWESSER LINE NOTATION :
- T6N DNTJ AYR&R DG& D1R DX1&1&1
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 320 mg/kg
- SEX/DURATION :
- female 13-16 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - homeostasis
- REFERENCE :
- TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 17,67,1970
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Safety Information
| Hazard Codes | Xi |
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| HS Code | 2933599090 |
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Customs
| HS Code | 2933599090 |
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| Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| Buclozin |
| 1-<4-Chlor-benzhydryl>-4-<4-tert.-butyl-benzyl>-piperazin |
| Histabuticine |
| BUCLIZINE |
| AH 2526 |
| Buclifen |
| aphilan-rbase |
| Postafen |
| Bucladin |
| Hitabutyzyne |
