*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : DE9800000
CHEMICAL NAME : 2H-1,4-Benzodiazepin-2-one,
7-bromo-1,3-dihydro-5-(2-pyridyl)-
CAS REGISTRY NUMBER : 1812-30-2
BEILSTEIN REFERENCE NO. : 0618645
REFERENCE : 5-26-05-00078 (Beilstein Handbook Reference)
LAST UPDATED : 199612
DATA ITEMS CITED : 26
MOLECULAR FORMULA : C14-H10-Br-N3-O
MOLECULAR WEIGHT : 316.18
WISWESSER LINE NOTATION : T67 GMV JN IHJ CE K- BT6NJ
COMPOUND DESCRIPTOR : Drug
Mutagen
Reproductive Effector
Primary Irritant
SYNONYMS/TRADE NAMES :
* 2H-1,4-Benzodiazepin-2-one, 1,3-dihydro-7-bromo-5-(2-pyridyl)-
* Bromazepam
* 7-Bromo-1,3-dihydro-5-(2-pyridyl)-2H-1,4-benzdiazepin-2-one
* 7-Bromo-5-(2-pyridyl)-3H-1,4-benzodiazepin-2(1H)-one
* Compendium
* 1,3-Dihydro-7-bromo-5-(2-pyridyl)-2H-1,4-benzodiazepin-2-one
* KL-001
* LA Xvii
* Lectopam
* Lexomil
* Lexotan
* Lexotanil
* Ro 4-9253
* Ro 5-3350
*** HEALTH HAZARD DATA ***
** SKIN/EYE IRRITATION DATA **
TYPE OF TEST : Standard Draize test
ROUTE OF EXPOSURE : Administration onto the skin
SPECIES OBSERVED : Human
DOSE/DURATION : 3 mg/3D (Intermittent)
REACTION SEVERITY : Moderate
REFERENCE :
85DKA8 "Cutaneous Toxicity, Proceedings of the 3rd Conference, 1976," Drill,
V.A., and P. Lazar, eds., New York, Academic Press, Inc. 1977
Volume(issue)/page/year: -,127,1977
** ACUTE TOXICITY DATA **
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 1950 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - ataxia
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: 7,2413,1973
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 1660 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 17,115,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 8800 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 17,115,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo,
Japan) Volume(issue)/page/year: -,1048,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 879 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 17,115,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 200 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - convulsions or effect on seizure threshold
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
JDGRAX Journal of Drug Research. (National Organization for Drug Research
and Control, POB 29, Cairo, Egypt) V.2- 1969- Volume(issue)/page/year:
16,7,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 6870 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 17,115,1979
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo,
Japan) Volume(issue)/page/year: -,1048,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 1690 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and
D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,158,1972
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 18750 mg/kg/30D-I
TOXIC EFFECTS :
Liver - changes in liver weight
Related to Chronic Data - death
Related to Chronic Data - changes in uterine weight
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo,
Japan) V.1- 1950- Volume(issue)/page/year: 27,1327,1976
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 58240 mg/kg/26W-I
TOXIC EFFECTS :
Liver - changes in liver weight
Nutritional and Gross Metabolic - weight loss or decreased weight gain
Related to Chronic Data - changes in ovarian weight
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo,
Japan) V.1- 1950- Volume(issue)/page/year: 27,1327,1976
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 35 mg/kg
SEX/DURATION : female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 7,2422,1973
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE : 180 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
TOXIC EFFECTS :
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: 26,199,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE : 210 mg/kg
SEX/DURATION : female 14 day(s) pre-mating
female 1-7 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: 26,215,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE : 21 mg/kg
SEX/DURATION : female 14 day(s) pre-mating
female 1-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 26,215,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE : 110 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
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: 26,111,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE : 11 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 26,111,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE : 60 mg/kg
SEX/DURATION : female 17-22 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: 26,199,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE : 875 mg/kg
SEX/DURATION : female 7-13 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
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: 7,2422,1973
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE : 35 mg/kg
SEX/DURATION : female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
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: 7,2422,1973
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 720 mg/kg
SEX/DURATION : female 8-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - extra-embryonic structures
(e.g., placenta, umbilical cord)
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 7,2433,1973
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rabbit
DOSE : 130 mg/kg
SEX/DURATION : female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured
before birth)
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 26,99,1983
** MUTATION DATA **
TYPE OF TEST : Mutation test systems - not otherwise specified
TEST SYSTEM : Rodent - hamster Embryo
DOSE/DURATION : 150 mg/L
REFERENCE :
MUTAEX Mutagenesis. (Oxford Univ. Press, Pinkhill House, Southfield Road,
Eynsham, Oxford OX8 1JJ, UK) V.1- 1986- Volume(issue)/page/year: 3,23,1988
TYPE OF TEST : Cytogenetic analysis
TEST SYSTEM : Rodent - hamster Fibroblast
DOSE/DURATION : 150 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 189,319,1987
TYPE OF TEST : Cytogenetic analysis
TEST SYSTEM : Rodent - hamster Embryo
DOSE/DURATION : 150 mg/L
REFERENCE :
MUTAEX Mutagenesis. (Oxford Univ. Press, Pinkhill House, Southfield Road,
Eynsham, Oxford OX8 1JJ, UK) V.1- 1986- Volume(issue)/page/year: 3,23,1988
*** END OF RECORD ***