*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : CV5376000
CHEMICAL NAME : Benzamide,
2-hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)am
ino)ethyl)-, monohydrochloride
CAS REGISTRY NUMBER : 32780-64-6
LAST UPDATED : 199612
DATA ITEMS CITED : 27
MOLECULAR FORMULA : C19-H24-N2-O3.Cl-H
MOLECULAR WEIGHT : 364.91
WISWESSER LINE NOTATION : ZVR BQ EYQ1MY1&2R &GH
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* AH 5158A
* Amipress
* 5-(1-Hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)salicylamide
hydrochloride
* Ipolab
* Labelol
* Labetalol hydrochloride
* Labrocol
* Normadate
* Normodyne
* Presdate
* Pressalolo
* Salicylamide, 5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)-,
hydrochloride
* Sch 15719W
* Trandate
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 244 mg/kg/76D-I
TOXIC EFFECTS :
Liver - liver function tests impaired
Lungs, Thorax, or Respiration - other changes
REFERENCE :
AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New
York, NY 10022) V.1- 1946- Volume(issue)/page/year: 87,235,1989
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 360 mg/kg/60D-I
TOXIC EFFECTS :
Liver - jaundice (or hyperbilirubinemia) hepatocellular
Liver - liver function tests impaired
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
113,210,1990
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 1620 mg/kg/27W-I
TOXIC EFFECTS :
Gastrointestinal - other changes
Liver - jaundice (or hyperbilirubinemia) hepatocellular
Kidney, Ureter, Bladder - other changes in urine composition
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
113,210,1990
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 53 mg/kg/53D-I
TOXIC EFFECTS :
Liver - jaundice (or hyperbilirubinemia) hepatocellular
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
113,210,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 2114 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
Behavioral - convulsions or effect on seizure threshold
Nutritional and Gross Metabolic - body temperature decrease
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: 21,6307,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 107 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 53 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 1450 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 114 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 47 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : >1500 mg/kg
TOXIC EFFECTS :
Behavioral - tremor
Behavioral - ataxia
Gastrointestinal - nausea or vomiting
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
6,273,1980
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 1250 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rabbit
DOSE/DURATION : 41 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - ataxia
REFERENCE :
HOIZAK Hokkaido Igaku Zasshi. Hokkaido Journal of Medical Science.
(Hokkaido Daigaku Igakubu, Nishi-7-chome, Kita-15-jo, Kita-ku, Sapporo,
Japan) V.1- 1923- Volume(issue)/page/year: 53,15,1978
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 13500 mg/kg/30D-I
TOXIC EFFECTS :
Liver - changes in liver weight
Kidney, Ureter, Bladder - changes in bladder weight
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 5,353,1980
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 27300 mg/kg/39W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight
Kidney, Ureter, Bladder - other changes in urine composition
Nutritional and Gross Metabolic - changes in potassium
REFERENCE :
JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological
Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku,
Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 6,37,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 21600 mg/kg/13W-I
TOXIC EFFECTS :
Liver - changes in liver weight
Kidney, Ureter, Bladder - urine volume increased
Blood - changes in leukocyte (WBC) count
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: 21,6314,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 2730 mg/kg/13W-I
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands
Gastrointestinal - hypermotility, diarrhea
Gastrointestinal - nausea or vomiting
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental
Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa,
Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year:
6,273,1980
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - woman
DOSE : 600 ug/kg
SEX/DURATION : female 35 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - cardiovascular
(circulatory) system
Reproductive - Specific Developmental Abnormalities - respiratory system
Reproductive - Effects on Newborn - Apgar score (human only)
REFERENCE :
AJPEEK American Journal of Perinatology. (Thieme Medical Publishers, Inc.
381 Park Ave. S., New York, NY 10157-0208) V.1- 1983-
Volume(issue)/page/year: 11,91,1994
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 3150 mg/kg
SEX/DURATION : male 63 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - testes, epididymis, sperm duct
Reproductive - Fertility - mating performance (e.g. # sperm positive females
per # females mated; # copulations per # estrus cycles)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,839,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 1 gm/kg
SEX/DURATION : female 17-22 day(s) after conception
lactating female 14 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
gain)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,879,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 3850 mg/kg
SEX/DURATION : female 7-17 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 - fetal death
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,851,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 1650 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)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,851,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 550 mg/kg
SEX/DURATION : female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,851,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 1800 mg/kg
SEX/DURATION : female 17-22 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,879,1981
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 100 mg/kg
SEX/DURATION : female 7-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - other neonatal measures or effects
Reproductive - Effects on Newborn - biochemical and metabolic
REFERENCE :
AIPBE4 Archives Internationalos de Physiologie, de Biochimie et de
Biophysique. (Vaillant-Carmanne, s.a., Zeven Puttenstraat 20, 3690
Zutendaal, Belgium) V.99- 1991- Volume(issue)/page/year: 100,355,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 650 mg/kg
SEX/DURATION : female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu
Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
Volume(issue)/page/year: 9,869,1981
*** REVIEWS ***
TOXICOLOGY REVIEW
PBPSDY Pharmacological and Biochemical Properties of Drug Substances.
(American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC
20037) V.1- 1977- Volume(issue)/page/year: 2,229,1979
*** END OF RECORD ***