Thioproperazine

Names

[ CAS No. ]:
316-81-4

[ Name ]:
Thioproperazine

[Synonym ]:
2-Dimethylsulfamoyl-10-<3-(4-methyl-piperazin-1-yl)-propyl>-phenothiazin
10-[3-(4-methyl-piperazin-1-yl)-propyl]-10H-phenothiazine-2-sulfonic acid dimethylamide
Majeptyl
Megeptil
Thioproperazine
Sulfenazin
N,N-dimethyl-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine-2-sulfonamide
10-<3-(4-Methyl-piperazin-1-yl)-propyl>-phenothiazin-2-sulfonsaeure-dimethylamid
Cephalmin
Thioperazine
Mazeptyl
Thioproperazin
thiproperazine
Vontil
Tioproferazina

Biological Activity

[Description]:

Thioproperazine (RP 7843) is an orally active antipsychotic agent with calming, antiemetic activity. Thioproperazine is effective in promoting the release of dopamine in rat striatum. Thioproperazine can be used in studies of schizophrenia and bipolar disorder[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[In Vivo]

Thioproperazine (5 mg/kg; i.p.; single) increases accumulation of dopamine in rat striatum[1]. Animal Model: Male charles river rats (200-250 g)[1]. Dosage: 5 mg/kg Administration: Intraperitoneal injection; single. Result: Markedly decreased dopamine levels (26%), and accelerated synthesis and utilization of dopamine in the striatum (dopamine specific activity was enhanced 250%).

Chemical & Physical Properties

[ Density]:
1.237g/cm3

[ Boiling Point ]:
612.2ºC at 760mmHg

[ Melting Point ]:
140ºC

[ Molecular Formula ]:
C₂₂H₃₀N₄O₂S₂

[ Molecular Weight ]:
446.62900

[ Flash Point ]:
324ºC

[ Exact Mass ]:
446.18100

[ PSA ]:
80.78000

[ LogP ]:
4.19870

[ Index of Refraction ]:
1.615

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SP5400000

CHEMICAL NAME :: Phenothiazine-2-sulfonamide, N,N-dimethyl-10-(3-(4-methyl-1-piperazinyl)propyl)-

CAS REGISTRY NUMBER :: 316-81-4

LAST UPDATED :: 199806

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C22-H30-N4-O2-S2

MOLECULAR WEIGHT :: 446.68

WISWESSER LINE NOTATION :: T C666 BN ISJ ESWN1&1 B3- AT6N DNTJ D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 830 mg/kg

TOXIC EFFECTS :: Behavioral - antipsychotic

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 130 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 70 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 200 mg/kg

SEX/DURATION :: female 1-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 5 mg/kg

REFERENCE :: CYGEDX Cytology and Genetics (English Translation). Translation of TGANAK. (Allerton Press Inc., 150 Fifth Ave., New York, NY 10011) V.8- 1974- Volume(issue)/page/year: 9(5),14,1975

Safety Information

[ HS Code ]:
2935009090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

Related Compounds

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