thiethylperazine

Modify Date: 2024-01-13 12:46:46

thiethylperazine structure	Common Name	thiethylperazine
	CAS Number	1420-55-9	Molecular Weight	399.61600
	Density	1.24g/cm3	Boiling Point	559.8ºC at 760mmHg
	Molecular Formula	C₂₂H₂₉N₃S₂	Melting Point	62-64°
	MSDS	N/A	Flash Point	292.4ºC

Use of thiethylperazine

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].

Name	thiethylperazine
Synonym	More Synonyms

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.

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)

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)

Ethylthioperazine.

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Tietylperazine

thietylperazine

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