Quinidine sulfate dihydrate

Names

[ Name ]:
Quinidine sulfate dihydrate

[Synonym ]:
Quinidine Sulfate Dihydrate
Cinchonan-9-ol, 6'-methoxy-, (9S)-, sulfate, hydrate (2:1:2) (salt)
EINECS 200-046-3
(9S)-6'-Methoxycinchonan-9-ol sulfate hydrate (2:1:2)
MFCD00149346

Biological Activity

[Description]:

Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo[1]. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia[2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

[Target]

IC50: cytochrome P450db; amphetamine metabolism[1]

[References]

[1]. David E. Moody, et al. Quinidine Inhibits In Vivo Metabolism of Amphetamine in Rats: Impact upon Correlation between GCIMS and Immunoassay Findings in Rat Urine. ournal of Analytical Toxicology, Vol. 14, September/October 1990

[2]. Tsuruo T, et al. Effects of quinidine and related compounds on cytotoxicity and cellular accumulation of vincristine and adriamycin in drug-resistant tumor cells.Cancer Res. 1984 Oct;44(10):4303-7.

Chemical & Physical Properties

[ Boiling Point ]:
992.5ºC at 760 mmHg

[ Melting Point ]:
212-214 °C (dec.)(lit.)

[ Molecular Formula ]:
C₂₀H₂₄N₂O_2.1/₂H₂O₄S_.H₂O

[ Molecular Weight ]:
782.943

[ Flash Point ]:
554ºC

[ Exact Mass ]:
782.356079

[ PSA ]:
192.62000

[ LogP ]:
6.52160

[ Index of Refraction ]:
275 ° (C=2, 0.1mol/L HCl)

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VA5605000

CHEMICAL NAME :: Quinidine, hemisulfate, hydrate

CAS REGISTRY NUMBER :: 6591-63-5

LAST UPDATED :: 198708

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C20-H24-N2-O2.1/2H2-O4-S.H2-O

MOLECULAR WEIGHT :: 391.52

WISWESSER LINE NOTATION :: T66 A B CNTJ A1U1 DYQ- ET66 BNJ HO1 2 &..H2.S-O4 &QH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 59 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - other changes

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 123,269,1958

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
R22

[ Safety Phrases ]:
13-36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
VA5605000

Articles

Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein.

Antimicrob. Agents Chemother. 58(6) , 3168-76, (2014)

Predicting drug-drug interactions (DDIs) related to cytochrome P450 (CYP), such as CYP3A4 and one of the major drug transporters, P-glycoprotein (P-gp), is crucial in the development of future chemoth...

Diurnal variation in P-glycoprotein-mediated transport and cerebrospinal fluid turnover in the brain.

AAPS J. 16(5) , 1029-37, (2014)

Nearly all bodily processes exhibit circadian rhythmicity. As a consequence, the pharmacokinetic and pharmacodynamic properties of a drug may also vary with time of day. The objective of this study wa...

Effects of the inhibition of intestinal P-glycoprotein on aliskiren pharmacokinetics in cynomolgus monkeys.

Biopharm. Drug Dispos. 36(1) , 15-33, (2015)

Aliskiren is a substrate for P-glycoprotein (P-gp) and is metabolized via cytochrome P450 3A4 (CYP3A4). The aim of the present study was to assess whether P-gp influenced the pharmacokinetics of alisk...