Thiethylperazine dimaleate

Modify Date: 2024-01-11 16:26:26

Thiethylperazine dimaleate Structure
Thiethylperazine dimaleate structure
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 N/A Flash Point 292.4ºC

 Use of Thiethylperazine dimaleate


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].

 Names

Name thiethylperazine maleate
Synonym More Synonyms

 Thiethylperazine dimaleate Biological Activity

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
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

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SP0350000
CAS REGISTRY NUMBER :
1179-69-7
LAST UPDATED :
199504
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C22-H29-N3-S2.2C4-H4-O4
MOLECULAR WEIGHT :
631.82
WISWESSER LINE NOTATION :
T C666 BN ISJ ES2 B3- AT6N DNTJ D1 &OV1U1VO

HEALTH HAZARD DATA

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
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  • China
  • Product Name: Toresten
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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