Tiapride

Names

[ Name ]:
Tiapride

[Synonym ]:
N-[2-(Diethylamino)ethyl]-5-(methylsulfonyl)-o-anisamide hydrochloride
N-[2-(diethylamino)ethyl]-2-methoxy-5-methylsulfonylbenzamide
EINECS 256-907-9
N-(2-(Diethylamino)ethyl)-2-methoxy-5-(methylsulfonyl)benzamide
MFCD00242730

Biological Activity

[Description]:

Tiapride, an atypical neuroleptic agent, is a selective dopamine D2-receptor antagonist with little propensity for causing catalepsy and sedation. The IC50 values of Tiapride are 1440, 45.8, >100, and 11.7 μM for D1; D2; D3; D4, respectively[1].

[Related Catalog]:

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

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

D2 Receptor:110-320 nM (IC50)

D3 Receptor:180 nM (IC50)

[References]

[1]. D H Peters, et al. Tiapride. A review of its pharmacology and therapeutic potential in the management of alcohol dependence syndrome. Drugs. 1994 Jun;47(6):1010-32.

[2]. T Arima, et al. Comparison of effects of tiapride and sulpiride on D-1, D-2, D-3 and D-4 subtypes of dopamine receptors in rat striatal and bovine caudate nucleus membranes. Jpn J Pharmacol. 1986 Jul;41(3):419-23.

Chemical & Physical Properties

[ Density]:
1.15 g/cm3

[ Boiling Point ]:
498.1ºC at 760 mmHg

[ Melting Point ]:
120ºC

[ Molecular Formula ]:
C₁₅H₂₄N₂O₄S

[ Molecular Weight ]:
328.42700

[ Flash Point ]:
255.1ºC

[ Exact Mass ]:
328.14600

[ PSA ]:
87.58000

[ LogP ]:
2.82590

[ Storage condition ]:
2-8°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV4203700

CHEMICAL NAME :: Benzamide, N-(2-(diethylamino)ethyl)-2-methoxy-5-(methylsulfonyl )-

CAS REGISTRY NUMBER :: 51012-32-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C15-H24-N2-O4-S

MOLECULAR WEIGHT :: 328.47

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1197 mg/kg

SEX/DURATION :: female 38 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 30,231,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 850 mg/kg

SEX/DURATION :: female 27 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 30,231,1975

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
2

[ RTECS ]:
CV4203800

[ HS Code ]:
2924299090

Customs

[ HS Code ]: 2924299090

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

Articles

Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease.

Brain 138 , 3221-37, (2015)

Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is...

German insurer finds a third of people over 65 take five or more drugs a day.

BMJ 346 , f3905, (2013)

Pharmacological treatment of tic disorders and Tourette Syndrome.

Neuropharmacology 68 , 143-9, (2013)

The present review gives an overview of current pharmacological treatment options of tic disorders and Tourette Syndrome (TS). After a short summary on phenomenology, clinical course and comorbid cond...