CAS 1179-69-7|Thiethylperazine dimaleate
Introduction：Basic information about CAS 1179-69-7|Thiethylperazine dimaleate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Thiethylperazine dimaleate | ||
|---|---|---|---|
| CAS Number | 1179-69-7 | Molecular Weight | 631.760 |
| Density | 1.24g/cm3 | Boiling Point | 559.8ºC at 760 mmHg |
| Molecular Formula | C30H37N3O8S2 | Melting Point | 62-64ºC |
| MSDS | / | Flash Point | 292.4ºC |
Names
| Name | thiethylperazine maleate |
|---|---|
| Synonym | More Synonyms |
Thiethylperazine dimaleate BiologicalActivity
| Description | Thiethylperazine dimaleate is a phenothiazine derivate, and an orally active dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a slective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects[1][2][3]. |
|---|---|
| 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 |
| Target | Dopamine D2-receptor[1] Histamine H1-receptor[1] ABCC1[2] Enterococcus faecalis[3] |
| In Vitro | Thiethylperazine could 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]. |
| In Vivo | Thiethylperazine (3 mg/kg; intramuscular injection; twice daily; for 30 days; young APP/PS1 mice) treatment significantly reduces Aβ42 levels in 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. |
| 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. |
Chemical & Physical Properties
| Density | 1.24g/cm3 |
|---|---|
| Boiling Point | 559.8ºC at 760 mmHg |
| Melting Point | 62-64ºC |
| Molecular Formula | C30H37N3O8S2 |
| Molecular Weight | 631.760 |
| Flash Point | 292.4ºC |
| Exact Mass | 631.202209 |
| PSA | 209.52000 |
| LogP | 4.40320 |
| Vapour Pressure | 1.46E-12mmHg at 25°C |
| InChIKey | RVBRTNPNFYFDMZ-SPIKMXEPSA-N |
| SMILES | CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2.O=C([O-])C=CC(=O)[O-].O=C([O-])C=CC(=O)[O-].[H+].[H+].[H+].[H+] |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 1260 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,51,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 90 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,51,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 680 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,51,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 217 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- MEXPAG Medicina Experimentalis. (Basel, Switzerland) V.1-11, 1959-64; V.18-19, 1968-69. For publisher information, see JNMDBO. Volume(issue)/page/year: 4,145,1961
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 93 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- MEXPAG Medicina Experimentalis. (Basel, Switzerland) V.1-11, 1959-64; V.18-19, 1968-69. For publisher information, see JNMDBO. Volume(issue)/page/year: 4,145,1961
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 1050 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,51,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 27 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,51,1972 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5553 No. of Facilities: 23 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 722 (estimated) No. of Female Employees: 377 (estimated)
Safety Information
| Hazard Codes | Xi |
|---|
Synonyms
| 2-butenedioate |
| torecandimaleate |
| 2-(Ethylsulfanyl)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine (2Z)-but-2-enedioate (1:2) |
| Thiethylperazinbishydrogenmaleat |
| THIETHYLPERAZINE MALEATE (200 MG) |
| torecanmaleate |
| torecanbimaleate |
| thiethylperazine dimaleate |
| 10H-Phenothiazine, 2-(ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]-, (2Z)-2-butenedioate (1:2) |
| torecan |
| toresten |
| tresten |
| 2-(Ethylsulfanyl)-10-[3-(4-methyl-1-piperazinyl)propyl]-10H-phenothiazine (2Z)-2-butenedioate (1:2) |
| gs-95 |
