*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : CU9390000
CHEMICAL NAME : Benzamide,
4-amino-5-chloro-2-methoxy-N-(1-benzyl-4-piperidyl)-,
malate
CAS REGISTRY NUMBER : 57645-91-7
LAST UPDATED : 199604
DATA ITEMS CITED : 16
MOLECULAR FORMULA : C20-H24-Cl-N3-O2.C4-H6-O5
MOLECULAR WEIGHT : 508.02
WISWESSER LINE NOTATION : T6NTJ A1R& DMVR DZ CG FO1 &QVYQ1VQ
COMPOUND DESCRIPTOR : Reproductive Effector
SYNONYMS/TRADE NAMES :
* 4-Amino-5-chloro-2-methoxy-N-(1-benzyl-4-piperidyl)benzamide malate
* Clebopride hydrogen malate
* Clebopride malate
*** 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 : 2540 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - changes in motor activity (specific assay)
Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 155 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 4850 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 39 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - analgesia
Gastrointestinal - nausea or vomiting
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intramuscular
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 1450 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
Behavioral - ataxia
Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 490 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - antipsychotic
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 145 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
Lungs, Thorax, or Respiration - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 305 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
Lungs, Thorax, or Respiration - respiratory stimulation
Skin and Appendages - hair
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 51 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
Lungs, Thorax, or Respiration - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intramuscular
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 260 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
Lungs, Thorax, or Respiration - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >800 mg/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: -,331,1990
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 2275 mg/kg/13W-C
TOXIC EFFECTS :
Related to Chronic Data - death
Related to Chronic Data - changes in ovarian weight
Related to Chronic Data - changes in uterine weight
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,803,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 4550 mg/kg/26W-C
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
Nutritional and Gross Metabolic - weight loss or decreased weight gain
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: 25,803,1983
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 875 mg/kg/35D-C
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
Related to Chronic Data - death
Related to Chronic Data - changes in uterine weight
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 25,877,1983
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 8 gm/kg
SEX/DURATION : male 9 week(s) pre-mating
female 7 day(s) pre-mating
female 1-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - mating performance (e.g. # sperm positive females
per # females mated; # copulations per # estrus cycles)
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: 16,5670,1982
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 12500 ug/kg
SEX/DURATION : female 17-20 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
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: 16,5661,1982
*** END OF RECORD ***