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thiethylperazine

Names

[ CAS No. ]:
1420-55-9

[ Name ]:
thiethylperazine

[Synonym ]:
Ethylthioperazine.
Torecane
Tietylperazine
thietylperazine

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Research Areas >> Infection
Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
Signaling Pathways >> Anti-infection >> Bacterial

[Target]

D2 Receptor

H1 Receptor


[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].

[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.

[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 760mmHg

[ Melting Point ]:
62-64°

[ Molecular Formula ]:
C22H29N3S2

[ Molecular Weight ]:
399.61600

[ Flash Point ]:
292.4ºC

[ Exact Mass ]:
399.18000

[ PSA ]:
60.32000

[ LogP ]:
4.97960

[ Index of Refraction ]:
1.5605 (estimate)

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 DATA

ACUTE 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)

Related Compounds