*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : XZ4179000
CHEMICAL NAME : 1H-1,2,4-Triazole-3-carboxamide,
5-(((aminoacetyl)amino)methyl)-1-(4-chloro-2-(2-
chlorobenzoyl)phenyl)-N,N-dimethyl-,
monohydrochloride, dihydrate
CAS REGISTRY NUMBER : 85815-37-8
OTHER CAS REGISTRY NOS. : 89233-59-0
LAST UPDATED : 199506
DATA ITEMS CITED : 16
MOLECULAR FORMULA : C21-H20-Cl2-N6-O3.Cl-H.2H2-O
MOLECULAR WEIGHT : 547.87
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
SYNONYMS/TRADE NAMES :
* Rhythmy
* 450191S
*** 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 : 680 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - ataxia
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 91 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Lungs, Thorax, or Respiration - dyspnea
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 1600 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - ataxia
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 540 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 72 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - somnolence (general depressed activity)
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 620 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
TYPE OF TEST : LD - Lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >1 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - excitement
Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8543,1986
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 5600 mg/kg/35D-C
TOXIC EFFECTS :
Liver - other changes
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
Related to Chronic Data - death
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8557,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 2275 mg/kg/13W-I
TOXIC EFFECTS :
Liver - other changes
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - phosphatases
Biochemical - Metabolism (Intermediary) - lipids including transport
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 21,1561,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 1500 mg/kg/30D-C
TOXIC EFFECTS :
Liver - other changes
Kidney, Ureter, Bladder - other changes in urine composition
Endocrine - other changes
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 20,8597,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 9125 mg/kg/1Y-I
TOXIC EFFECTS :
Liver - changes in liver weight
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
Biochemical - Enzyme inhibition, induction, or change in blood or tissue
levels - phosphatases
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 21,1651,1987
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 4400 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
gain)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,765,1985
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 650 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 20 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4
per # born alive)
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
gain)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,793,1985
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 2600 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 20 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Paternal Effects - testes, epididymis, sperm duct
Reproductive - Maternal Effects - ovaries, fallopian tubes
Reproductive - Effects on Newborn - delayed effects
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,793,1985
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 10400 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 20 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland,
accessory glands
Reproductive - Maternal Effects - uterus, cervix, vagina
Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,793,1985
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 91 mg/kg
SEX/DURATION : female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,819,1985
*** END OF RECORD ***