Muzolimine

[Description]:

Muzolimine (BAY-g 282) is a slow and long lasting diuresis agent. Muzolimine produces a diuresis in the loop of Henle and also shows anti-hypertensive effects. Muzolimine can be used for the research of cardiovascular disease[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[In Vitro]

Muzolimine (10 μM-1 mM) dose-dependently inhibits ion transport in Ehrlich cells[2].

[In Vivo]

Muzolimine (0-18 mg/kg; p.o. 7-times per week for 3 months) shows a marked diuresis effect in dogs[1]. Animal Model: 3 male and 3 female dogs[1] Dosage: 0, 2, 6, 8 and 18 mg/kg Administration: Oral gavage; 7 times per week for 3 months Result: Showed significant diuretic results, and increased the water intake of dogs.

[ Density]:
1.51g/cm3

[ Boiling Point ]:
401.4ºC at 760 mmHg

[ Molecular Formula ]:
C₁₁H₁₁Cl₂N₃O

[ Molecular Weight ]:
272.13100

[ Flash Point ]:
196.6ºC

[ Exact Mass ]:
271.02800

[ PSA ]:
56.19000

[ LogP ]:
3.13500

[ Index of Refraction ]:
1.666

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UR0370000

CHEMICAL NAME :: 3H-Pyrazol-3-one, 5-amino-2-(1-(3,4-dichlorophenyl)ethyl)-2,4-dihydro-

CAS REGISTRY NUMBER :: 55294-15-0

LAST UPDATED :: 199703

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C11-H11-Cl2-N3-O

MOLECULAR WEIGHT :: 272.15

WISWESSER LINE NOTATION :: T5NNV DHJ BY1&R CG DG& EZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1559 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory obstruction Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 221 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: CLNHBI Clinical Nephrology. (Dustri-Verlag Dr. Karl Feistle, Postfach 49, D-8024 Munich-Deisenhofen, Fed. Rep. Ger.) V.1- 1973- Volume(issue)/page/year: 19(Suppl 1),20,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1794 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory obstruction Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 310 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: CLNHBI Clinical Nephrology. (Dustri-Verlag Dr. Karl Feistle, Postfach 49, D-8024 Munich-Deisenhofen, Fed. Rep. Ger.) V.1- 1973- Volume(issue)/page/year: 19(Suppl 1),20,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Behavioral - fluid intake Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >200 mg/kg

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

REFERENCE :: CLNHBI Clinical Nephrology. (Dustri-Verlag Dr. Karl Feistle, Postfach 49, D-8024 Munich-Deisenhofen, Fed. Rep. Ger.) V.1- 1973- Volume(issue)/page/year: 19(Suppl 1),20,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1250 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory obstruction Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9 gm/kg/13W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume increased Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1620 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - fluid intake Kidney, Ureter, Bladder - urine volume increased Related to Chronic Data - death

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 84 mg/kg/4W-I

TOXIC EFFECTS :: Behavioral - fluid intake Kidney, Ureter, Bladder - urine volume increased Nutritional and Gross Metabolic - dehydration

REFERENCE :: CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,716,1977

Names

Biological Activity

Chemical & Physical Properties

Toxicological Information

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

Related Compounds