*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : KG2955000
CHEMICAL NAME : Estra-4,9-dien-3-one,
11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propyny
l)-, (11-beta, 17-beta)-
CAS REGISTRY NUMBER : 84371-65-3
OTHER CAS REGISTRY NOS. : 83203-42-3
122742-25-0
BEILSTEIN REFERENCE NO. : 5779404
LAST UPDATED : 199709
DATA ITEMS CITED : 26
MOLECULAR FORMULA : C29-H35-N-O2
MOLECULAR WEIGHT : 429.65
COMPOUND DESCRIPTOR : Reproductive Effector
Human
Hormone
SYNONYMS/TRADE NAMES :
* 17-beta-Hydroxy-11-beta-(4-dimethylaminophenyl-1)-17-alpha-(prop-1-ynyl)
oestra-4,9-dien-3-one
* Mifepristone
* R 38486
* RU 486
* RU 486-6
* RU 38486
*** HEALTH HAZARD DATA ***
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE : 12 mg/kg
SEX/DURATION : female 7 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
REFERENCE :
FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S,
Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 56,32,1991
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE : 14 mg/kg
SEX/DURATION : female 7-8 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1-
1970- Volume(issue)/page/year: 35,307,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE : 12 mg/kg
SEX/DURATION : female 6 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
REFERENCE :
EOGRAL European Journal of Obstetrics, Gynecology and Reproductive Biology.
(Elsevier Science Pub. BV, POB 211, 1000 AE Amsterdam, Netherlands) V.3-
1973- Volume(issue)/page/year: 28,249,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE : 12 mg/kg
SEX/DURATION : female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
REFERENCE :
OBGNAS Obstetrics and Gynecology. (Elsevier Science Pub. Co., Inc., 52
Vanderbilt Ave., New York, NY 10017) V.1- 1953- Volume(issue)/page/year:
74,653,1989
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE : 10 mg/kg
SEX/DURATION : female 6 week(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
Reproductive - Fertility - abortion
REFERENCE :
GOBIDS Gynecologic and Obstetric Investigation. (S. Karger Pub., Inc., 79
Fifth Ave., New York, NY 10003) V.9- 1978- Volume(issue)/page/year:
29,13,1990
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 12 mg/kg
SEX/DURATION : female 6-8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant
per # sperm positive females; # females pregnant per # females mated)
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
REFERENCE :
CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal
of Pharmacology. (China International Book Trading Corp., POB 2820,
Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year:
14,437,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 160 mg/kg
SEX/DURATION : female 1-20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
REFERENCE :
BMEMDK Biological Memoirs. (International Publishers, C 131, Mahanagar,
Lucknow 226 006, India) V.1- 1976- Volume(issue)/page/year: 15,107,1989
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 12 mg/kg
SEX/DURATION : female 7-9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant
per # sperm positive females; # females pregnant per # females mated)
REFERENCE :
SCYYDZ Shengzhi Yu Biyun. Reproduction and Contraception. (China
International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) 1980-
Volume(issue)/page/year: 15,47,1995
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 6250 ug/kg
SEX/DURATION : female 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - uterus, cervix, vagina
Reproductive - Fertility - abortion
REFERENCE :
SCYYDZ Shengzhi Yu Biyun. Reproduction and Contraception. (China
International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) 1980-
Volume(issue)/page/year: 14,332,1994
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Administration onto the skin
SPECIES OBSERVED : Rodent - rat
DOSE : 50 mg/kg
SEX/DURATION : female 21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4
per # born alive)
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
gain)
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 79,1,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 2500 ug/kg
SEX/DURATION : female 1 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 :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 80,487,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 10 mg/kg
SEX/DURATION : female 1-2 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 80,487,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 45 mg/kg
SEX/DURATION : female 5-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
Reproductive - Fertility - other measures of fertility
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 83,73,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 30 mg/kg
SEX/DURATION : female 2 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)
Reproductive - Maternal Effects - other effects
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 83,279,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE : 200 mg/kg
SEX/DURATION : female 1-2 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)
Reproductive - Effects on Embryo or Fetus - cytological changes (including
somatic cell genetic material)
Reproductive - Effects on Embryo or Fetus - other effects to embryo
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1-
1970- Volume(issue)/page/year: 41,551,1990
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE : 6 mg/kg
SEX/DURATION : female 6-8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant
per # sperm positive females; # females pregnant per # females mated)
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
number of implants per female; total number of implants per corpora lutea)
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
REFERENCE :
CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal
of Pharmacology. (China International Book Trading Corp., POB 2820,
Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year:
14,437,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE : 3 mg/kg
SEX/DURATION : female 7-9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant
per # sperm positive females; # females pregnant per # females mated)
REFERENCE :
SCYYDZ Shengzhi Yu Biyun. Reproduction and Contraception. (China
International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) 1980-
Volume(issue)/page/year: 15,47,1995
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE : 4 mg/kg
SEX/DURATION : female 1 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 :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1-
1970- Volume(issue)/page/year: 36,549,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 2 mg/kg
SEX/DURATION : female 15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 96,299,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE : 2 mg/kg
SEX/DURATION : female 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant
per # sperm positive females; # females pregnant per # females mated)
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1-
1970- Volume(issue)/page/year: 47,317,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE : 400 ug/kg
SEX/DURATION : female 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1-
1970- Volume(issue)/page/year: 47,317,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE : 22500 ug/kg
SEX/DURATION : female 32-36 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
Endocrine - changes in luteinizing hormone
Reproductive - Fertility - abortion
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 88,99,1990
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE : 70 mg/kg
SEX/DURATION : female 32-39 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
REFERENCE :
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1-
1970- Volume(issue)/page/year: 41,85,1990
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intramuscular
SPECIES OBSERVED : Primate - monkey
DOSE : 10 mg/kg
SEX/DURATION : female 15-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System
Reproductive - Specific Developmental Abnormalities - craniofacial
(including nose and tongue)
REFERENCE :
JMPMAO Journal of Medical Primatology. (Munksgaard International
Publishers, 238 Main St., Cambridge, MA 02142) V.1- 1972-
Volume(issue)/page/year: 23,319,1994
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intramuscular
SPECIES OBSERVED : Mammal - domestic
DOSE : 8 mg/kg
SEX/DURATION : female 21 week(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition
Endocrine - effect on menstrual cycle
REFERENCE :
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot,
POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
Volume(issue)/page/year: 97,233,1993
*** REVIEWS ***
TOXICOLOGY REVIEW
HUREEE Human Reproduction. (IRL Press Inc., POB Q, McLean, VA 22101) V.1-
1986- Volume(issue)/page/year: 1,107,1986
*** END OF RECORD ***