*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : NL3520500
CHEMICAL NAME : 1H-Indole-3-acetic acid,
1-(4-chlorobenzoyl)-5-methoxy-2-methyl-2-(4-(3-((4-(b
enzoylamino)-
5-(dipropylamino)-1,5-dioxopentyl)oxy)propyl)-1-piper
azinyl)ethyl ester (+-)-, (Z)-2- butenedioate (1:2)
CAS REGISTRY NUMBER : 59209-40-4
OTHER CAS REGISTRY NOS. : 68246-97-9
LAST UPDATED : 199212
DATA ITEMS CITED : 14
MOLECULAR FORMULA : C46-H58-Cl-N5-O8.2C4-H4-O4
MOLECULAR WEIGHT : 1076.70
WISWESSER LINE NOTATION : T56 BNJ BVR DG& C1 D1VO2- AT6N DNTJ D3OV2YMVR&VN3&3
&QV1U1VQ 2
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
SYNONYMS/TRADE NAMES :
* Afloxan
* CR-604
* Proglumetacin maleate
* Proglumetacina
* Protacine
* Proxil
*** 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 : 170 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - ataxia
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1173,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Administration onto the skin
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho
Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
Volume(issue)/page/year: 20,228,1989
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 247 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - ataxia
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1173,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 332 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - ataxia
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1173,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Rectal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >4750 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho
Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970-
Volume(issue)/page/year: 20,228,1989
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 67 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - somnolence (general depressed activity)
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1173,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 243 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - ataxia
Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1173,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 195 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - ataxia
Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1173,1986
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 824 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea
Gastrointestinal - nausea or vomiting
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,403,1986
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 3640 mg/kg/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in bladder weight
Blood - normocytic anemia
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,403,1986
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 132 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 - 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: 32,1017,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 216 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition
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: 32,1039,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 420 mg/kg
SEX/DURATION : male 9 week(s) pre-mating
female 2 week(s) pre-mating - 7 day(s) after
conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1005,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 672 mg/kg
SEX/DURATION : male 9 week(s) pre-mating
female 2 week(s) pre-mating - 7 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 :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180,
Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,1005,1986
*** END OF RECORD ***