Mefloquine hydrochloride

Suppliers

Names

[ CAS No. ]:
51773-92-3

[ Name ]:
Mefloquine hydrochloride

[Synonym ]:
Mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol
EINECS 257-412-0
[2,8-bis(trifluoromethyl)quinolin-4-yl](piperidin-2-yl)methanol
4-quinolinemethanol, a-2-piperidinyl-2,8-bis(trifluoromethyl)-
[2,8-Bis(trifluoromethyl)-4-quinolinyl](2-piperidinyl)methanol
MFCD00797519
(AS)-rel-a-(2R)-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol monohydrochloride
4-Quinolinemethanol, α-2-piperidinyl-2,8-bis(trifluoromethyl)-
α-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol
Mefloquine (hydrochloride)

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
415.7±40.0 °C at 760 mmHg

[ Melting Point ]:
250-254ºC

[ Molecular Formula ]:
C17H17ClF6N2O

[ Molecular Weight ]:
378.312

[ Flash Point ]:
205.2±27.3 °C

[ Exact Mass ]:
378.116669

[ PSA ]:
45.15000

[ LogP ]:
2.87

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.519

[ Storage condition ]:
Refrigerator

[ Water Solubility ]:
DMSO: 38 mg/mL, soluble

MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VC0308000
CHEMICAL NAME :
4-Quinolinemethanol, 2,8-bis(trifluoromethyl)-alpha-2-piperidinyl-, monohydrochloride, (R*,S*)-, (+-)-
CAS REGISTRY NUMBER :
51773-92-3
LAST UPDATED :
199603
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C17-H16-F6-N2-O.Cl-H
MOLECULAR WEIGHT :
414.81
WISWESSER LINE NOTATION :
T66 BNJ CXFFF EYQ- BT6MTJ& JXFFF &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
96 mg/kg/52D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions Behavioral - excitement Behavioral - aggression
REFERENCE :
AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 154,2360,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
15 mg/kg/3W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma
REFERENCE :
MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 161,453,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
11 mg/kg/2W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 114,994,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
18 mg/kg/5W-I
TOXIC EFFECTS :
Peripheral Nerve and Sensation - paresthesis Behavioral - general anesthetic
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 117,1058,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
880 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
130 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980

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: Harmful;

[ Risk Phrases ]:
R22

[ RIDADR ]:
UN 3077 9 / PGIII

[ WGK Germany ]:
3

[ RTECS ]:
VC0308000

Synthetic Route

Precursor & DownStream

Precursor

  • bis[2,8-di(trifluoromethyl)quinolin-4-yl-2-pyridyl] ketone
  • 2,8-Bis(trifluoromethyl)quinolin-4-ol
  • 2-(Chloromethyl)pyridine HCl
  • 4-[(tert-butyldimethylsilyl)(2-pyridyl)methoxy]-2,8-bis(trifluoromethyl)quinoline
  • alpha-2-pyridinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol

DownStream

Articles

Preliminary investigation of the contribution of CYP2A6, CYP2B6, and UGT1A9 polymorphisms on artesunate-mefloquine treatment response in Burmese patients with Plasmodium falciparum malaria.

Am. J. Trop. Med. Hyg. 91(2) , 361-6, (2014)

CYP2A6, CYP2B6, and UGT1A9 genetic polymorphisms and treatment response after a three-day course of artesunate-mefloquine was investigated in 71 Burmese patients with uncomplicated Plasmodium falcipar...

Studying the effect of chloroquine on sporozoite-induced protection and immune responses in Plasmodium berghei malaria.

Malaria Journal 14 , 130, (2015)

Sporozoite immunization of animals and humans under a chemo-prophylactic cover of chloroquine (CPS-CQ) efficiently induces sterile protection against malaria. In humans, CPS-CQ is strikingly more effi...

Comparison between Flow Cytometry, Microscopy, and Lactate Dehydrogenase-Based Enzyme-Linked Immunosorbent Assay for Plasmodium falciparum Drug Susceptibility Testing under Field Conditions.

J. Clin. Microbiol. 53 , 3296-303, (2015)

Flow cytometry is an objective method for conducting in vitro antimalarial sensitivity assays with increasing potential for application in field sites. We examined in vitro susceptibility to seven ant...


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Related Compounds

  • threo-Mefloquine Hydrochloride
  • (-)-syn-mefloquine hydrochloride
  • Mefloquine
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  • 2-Methoxy-6-(pyrazol-1-yl)-benzonitrile
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  • (4-Methyl-tetrahydro-furan-2-yl)-methanol
  • N-(1-cyanocyclopentyl)-2-[4-(4-fluorobenzenesulfonyl)-1,4-diazepan-1-yl]acetamide
  • 4,5,6,7-Tetrahydrobenzo[d]isoxazole-3-carbaldehyde
  • tert-Butyl-DL-alanine
  • 4-amino-N-[2-tert-butyl-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-benzimidazol-5-yl]-N-ethylbenzenesulfonamide
  • N-[3-(Aminooxy)propyl]-N-butyl-1-butanamine