Introduction:Basic information about CAS 1420-55-9|thiethylperazine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | thiethylperazine |
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| CAS Number | 1420-55-9 | Molecular Weight | 399.61600 |
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| Density | 1.24g/cm3 | Boiling Point | 559.8ºC at 760mmHg |
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| Molecular Formula | C22H29N3S2 | Melting Point | 62-64° |
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| MSDS | / | Flash Point | 292.4ºC |
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Names
| Name | thiethylperazine |
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| Synonym | More Synonyms |
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thiethylperazine BiologicalActivity
| Description | Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3]. |
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| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>InfectionSignaling Pathways >>GPCR/G Protein >>Dopamine ReceptorSignaling Pathways >>Neuronal Signaling >>Dopamine ReceptorResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Anti-infection >>Bacterial |
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| Target | D2 Receptor H1 Receptor |
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| In Vitro | Thiethylperazine can enhance the antibiotic (Vancomycin) activity at a concentration as low as 2 μg/mL. Thiethylperazine inhibits Vancomycin-sensitive E. faecalis ATCC 29212, Vancomycin-resistant E. faecalis ATCC 51299 and vancomycin-resistant E. faecalis (VREF) isolates with MIC values of 8 μg/mL, 16 μg/mL and 8 μg/mL, respectively[3]. |
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| In Vivo | Thiethylperazine (3 mg/kg; intramuscular injection; twice daily; for 30 days) significantly reduces Aβ42 levels in young APP/PS1 mice[2]. Animal Model: Young Aβ precursor protein (APPswe) and mutant presenilin-1 (PS1) (APP/PS1) mice[2] Dosage: 3 mg/kg Administration: Intramuscular injection; twice daily; for 30 days Result: Significantly reduced Aβ42 levels in APP/PS1 mice. |
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| References | [1]. Czeizel AE, et al. Case-control study of teratogenic potential of thiethylperazine, an anti-emetic drug. BJOG. 2003 May;110(5):497-9. [2]. Krohn M, et al. Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice. J Clin Invest. 2011 Oct;121(10):3924-31. [3]. Rahbar M, et al. Enhancement of vancomycin activity by phenothiazines against vancomycin-resistant Enterococcus faecium in vitro. Basic Clin Pharmacol Toxicol. 2010 Aug;107(2):676-9. |
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Chemical & Physical Properties
| Density | 1.24g/cm3 |
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| Boiling Point | 559.8ºC at 760mmHg |
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| Melting Point | 62-64° |
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| Molecular Formula | C22H29N3S2 |
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| Molecular Weight | 399.61600 |
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| Flash Point | 292.4ºC |
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| Exact Mass | 399.18000 |
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| PSA | 60.32000 |
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| LogP | 4.97960 |
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| Index of Refraction | 1.5605 (estimate) |
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| InChIKey | XCTYLCDETUVOIP-UHFFFAOYSA-N |
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| SMILES | CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- SP0280000
- CHEMICAL NAME :
- Phenothiazine, 2-(ethylthio)-10-(3-(4-methyl-1-piperazinyl)propyl)-
- CAS REGISTRY NUMBER :
- 1420-55-9
- LAST UPDATED :
- 199512
- DATA ITEMS CITED :
- 4
- MOLECULAR FORMULA :
- C22-H29-N3-S2
- MOLECULAR WEIGHT :
- 399.66
- WISWESSER LINE NOTATION :
- T C666 BN ISJ ES2 B3- AT6N DNTJ D1
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Rectal
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 857 ug/kg/2D-I
- TOXIC EFFECTS :
- Behavioral - ataxia
- REFERENCE :
- DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969- Volume(issue)/page/year: 19,550,1985
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 680 mg/kg
- TOXIC EFFECTS :
- Behavioral - antipsychotic
- REFERENCE :
- DNEUD5 Developments in Neuroscience (Amsterdam). (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.1- 1977- Volume(issue)/page/year: 7,45,1980
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 71600 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4792 No. of Facilities: 18 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1333 (estimated) No. of Female Employees: 656 (estimated)
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Synonyms
| Ethylthioperazine. |
| Torecane |
| Tietylperazine |
| thietylperazine |