Remoxipride hydrochloride

Names

[ Name ]:
Remoxipride hydrochloride

[Synonym ]:
Macbecin I
REMOXIPRIDE HYDROCHLORIDE

Biological Activity

[Description]:

(S)-Remoxipride ((-)-Remoxipride) hydrochloride is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride hydrochloride can be used for the research of psychotic disorder[1].

[Related Catalog]:

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

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[In Vitro]

(S)-Remoxipride hydrochloride (1-100 μM; 20 min) shows binding efficiency with IC50s of ＞100, 1.57 and 42 μM for dopamine D1, dopamine D2 and α1-Adrenoccptor, respectively[1].

[In Vivo]

(S)-Remoxipride hydrochloride (0.1-100 μM/kg; i.p. 60 min prior to apomorphine) blockades apomorphine-induced behaviors s in rats and vomiting in dogs[1]. (S)-Remoxipride hydrochloride (0.1-10 mg/kg; i.p. 30 min prior to apomorphine) displaces [3H]spiperone from both striatal and extra-striatal areas[1].

[References]

[1]. Ogren SO, et al. Remoxipride, a new potential antipsychotic compound with selective antidopaminergic actions in the rat brain. Eur J Pharmacol. 1984 Jul 20;102(3-4):459-74.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₂₄BrClN₂O₃

[ Molecular Weight ]:
407.73

[ Exact Mass ]:
406.06600

[ PSA ]:
50.80000

[ LogP ]:
3.81120

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV2369000

CHEMICAL NAME :: Benzamide, 3-bromo-2,6-dimethoxy-N-(1-ethyl-2-pyrrolidinylmethyl )-, hydrochloride, (S)-(-)-

CAS REGISTRY NUMBER :: 73220-03-8

LAST UPDATED :: 199412

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C16-H23-Br-N2-O3

MOLECULAR WEIGHT :: 371.32

WISWESSER LINE NOTATION :: T5NTJ A2 B1MVR CE BO1 FO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 324 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - rigidity (including catalepsy)

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 25,1280,1982

Safety Information

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%