*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : DE9600000
CHEMICAL NAME : 1H-1,5-Benzodiazepine-2,4(3H,5H)-dione,
7-chloro-1-methyl-5-phenyl-
CAS REGISTRY NUMBER : 22316-47-8
BEILSTEIN REFERENCE NO. : 0758410
REFERENCE : 5-24-08-00034 (Beilstein Handbook Reference)
LAST UPDATED : 199612
DATA ITEMS CITED : 18
MOLECULAR FORMULA : C16-H13-Cl-N2-O2
MOLECULAR WEIGHT : 300.76
WISWESSER LINE NOTATION : T67 GNV JVN IHJ CG G1 KR
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* Chlorepin
* 7-Chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4(3H,5H)-dione
* Clobazam
* Clorepin
* Frisium
* H-4723
* HR 376
* LM-2717
* 1-Phenyl-5-methyl-8-chloro-1,2,4,5-tetrahydro-2,4-dioxo-3H-1,5-benzodiaz
epine
* RU-4723
* Urbanyl
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 104 mg/kg/1Y-C
TOXIC EFFECTS :
Behavioral - wakefulness
Behavioral - withdrawal
Gastrointestinal - nausea or vomiting
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House,
Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year:
282,1931,1981
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 6 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos
540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year:
16,9,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 740 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 8700 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - changes in motor activity (specific assay)
Behavioral - muscle weakness
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,663,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 580 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag,
Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
Volume(issue)/page/year: 35,133,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 289 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 2250 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >100 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 320 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - guinea pig
DOSE/DURATION : 109 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - somnolence (general depressed activity)
Behavioral - tremor
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 18200 mg/kg/26W-C
TOXIC EFFECTS :
Skin and Appendages - hair
Related to Chronic Data - death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,673,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 3650 mg/kg/52W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - withdrawal
Related to Chronic Data - death
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : 7300 mg/kg/52W-I
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - ataxia
Cardiac - pulse rate
REFERENCE :
BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub.
Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year:
7,33S,1979
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 2750 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,1039,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 1575 mg/kg
SEX/DURATION : male 63 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - testes, epididymis, sperm duct
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,907,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 3750 mg/kg
SEX/DURATION : female 17-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,917,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 6500 mg/kg
SEX/DURATION : female 17-21 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - physical
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,917,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 650 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 - sex ratio
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,1055,1983
*** END OF RECORD ***