*** CHEMICAL IDENTIFICATION ***

RTECS NUMBER            : DL0305000
CHEMICAL NAME           : 1,5-Benzothiazepin-4(5H)-one,
                          2,3-dihydro-3-(acetyloxy)-8-chloro-5-(2-(dimethylamin
                          o)ethyl)- 2-(4-methoxyphenyl)-, (2S-cis)-,
                          (Z)-2-butenedioate (1:1)
CAS REGISTRY NUMBER     : 96128-92-6
LAST UPDATED            : 199512
DATA ITEMS CITED        : 9
MOLECULAR FORMULA       : C22-H25-Cl-N2-O4-S.C4-H4-O4
MOLECULAR WEIGHT        : 565.08
COMPOUND DESCRIPTOR     : Drug
                          Reproductive Effector
SYNONYMS/TRADE NAMES :
   * Clentiazem maleate
   * TA 3090
 
                       *** HEALTH HAZARD DATA ***
 
                        ** ACUTE TOXICITY DATA **
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 800 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   EPXXDW European Patent Application. (U.S. Patent and Trademark Office,
   Foreign Patents, Washington, DC 20231)  Volume(issue)/page/year: #501442
 
                 ** OTHER MULTIPLE DOSE TOXICITY DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 27300 mg/kg/13W-C
TOXIC EFFECTS :
   Liver - changes in liver weight
   Kidney, Ureter, Bladder - urine volume increased
   Biochemical - Enzyme inhibition, induction, or change in blood or tissue
   levels - transaminases
REFERENCE :
   OYYAA2 Oyo Yakuri.  Pharmacometrics.  (Oyo Yakuri Kenkyukai, CPO Box 180,
   Sendai 980-91, Japan) V.1-    1967-  Volume(issue)/page/year: 44,565,1992
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 36400 mg/kg/52W-C
TOXIC EFFECTS :
   Liver - changes in liver weight
   Kidney, Ureter, Bladder - urine volume increased
   Biochemical - Enzyme inhibition, induction, or change in blood or tissue
   levels - transaminases
REFERENCE :
   OYYAA2 Oyo Yakuri.  Pharmacometrics.  (Oyo Yakuri Kenkyukai, CPO Box 180,
   Sendai 980-91, Japan) V.1-    1967-  Volume(issue)/page/year: 44,565,1992
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 910 mg/kg/13W-I
TOXIC EFFECTS :
   Cardiac - EKG changes not diagnostic of specified effects
   Cardiac - pulse rate
   Biochemical - Enzyme inhibition, induction, or change in blood or tissue
   levels - transaminases
REFERENCE :
   OYYAA2 Oyo Yakuri.  Pharmacometrics.  (Oyo Yakuri Kenkyukai, CPO Box 180,
   Sendai 980-91, Japan) V.1-    1967-  Volume(issue)/page/year: 44,585,1992
 
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 :
   Cardiac - pulse rate
   Liver - fatty liver degeneration
   Biochemical - Enzyme inhibition, induction, or change in blood or tissue
   levels - transaminases
REFERENCE :
   OYYAA2 Oyo Yakuri.  Pharmacometrics.  (Oyo Yakuri Kenkyukai, CPO Box 180,
   Sendai 980-91, Japan) V.1-    1967-  Volume(issue)/page/year: 44,585,1992
 
                          ** REPRODUCTIVE DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 880 mg/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
   resorbed implants per total number of implants)
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
   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: 44,511,1992
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 6720 mg/kg
SEX/DURATION            : male 9 week(s) pre-mating
                          female 2 week(s) pre-mating  - 7 day(s) after
                          conception
TOXIC EFFECTS :
   Reproductive - Maternal Effects - menstrual cycle changes or disorders
REFERENCE :
   OYYAA2 Oyo Yakuri.  Pharmacometrics.  (Oyo Yakuri Kenkyukai, CPO Box 180,
   Sendai 980-91, Japan) V.1-    1967-  Volume(issue)/page/year: 47,165,1994
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 650 mg/kg
SEX/DURATION            : female 17-21 day(s) after conception
                          lactating female 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - live birth index (measured after birth)
   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: 47,165,1994
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rabbit
DOSE                    : 390 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 - Effects on Embryo or Fetus - fetal death
   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: 44,511,1992
 
                            *** END OF RECORD ***