*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : UP0791400
CHEMICAL NAME : 6H-Purin-6-one,
1,9-dihydro-2-amino-9-((2-hydroxyethoxy)methyl)-
CAS REGISTRY NUMBER : 59277-89-3
LAST UPDATED : 199712
DATA ITEMS CITED : 30
MOLECULAR FORMULA : C8-H11-N5-O3
MOLECULAR WEIGHT : 225.24
WISWESSER LINE NOTATION : T56 BN DN FN HNJ D1O2Q GZ IQ &T56 BN DN FVM INJ B1O2Q
HZ
COMPOUND DESCRIPTOR : Drug
Mutagen
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* Aciclovir
* Acycloguanosine
* Acyclovir
* 2-Amino-1,9-dihydro-9-((2-hydroxyethoxy)methyl)-6H-purin-6-one
* BW 248U
* 9-(2-Hydroxyethoxymethyl)guanine
* 6H-Purin-6-one, 2-amino-1,9-dihydro-9-((2-hydroxyethoxy)-methyl)-
* Wellcome-248U
* W-248-U
* Zovirax
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 28 mg/kg/2D-I
TOXIC EFFECTS :
Brain and Coverings - changes in surface EEG
Behavioral - hallucinations, distorted perceptions
Lungs, Thorax, or Respiration - sputum
REFERENCE :
SMJOAV Southern Medical Journal. (Southern Medical Assoc., POB 2446,
Birmingham, AL 35205) V.1- 1908- Volume(issue)/page/year: 87,1227,1994
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 12 mg/kg/1D-I
TOXIC EFFECTS :
Brain and Coverings - meningeal changes
Behavioral - somnolence (general depressed activity)
Behavioral - antipsychotic
REFERENCE :
SMJOAV Southern Medical Journal. (Southern Medical Assoc., POB 2446,
Birmingham, AL 35205) V.1- 1908- Volume(issue)/page/year: 87,1227,1994
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 100 mg/kg/5D-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, allergic (after systemic exposure)
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House,
Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year:
289,1424,1984
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 80 mg/kg/4D-I
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
Behavioral - hallucinations, distorted perceptions
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
111,187,1989
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 486 mg/kg/17D-I
TOXIC EFFECTS :
Gastrointestinal - decreased motility or constipation
Gastrointestinal - other changes
REFERENCE :
AJGAAR American Journal of Gastroenterology. (American College of
Gastroenterology, Inc., 428 E. Preston St., Baltimore, MD 21202) V.21-
1954- Volume(issue)/page/year: 88,2110,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - man
DOSE/DURATION : 134 ug/kg/1D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823-
Volume(issue)/page/year: 2,385,1985
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 101 mg/kg/2D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Behavioral - muscle contraction or spasticity
REFERENCE :
AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New
York, NY 10022) V.1- 1946- Volume(issue)/page/year: 94,212,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Human - man
DOSE/DURATION : 107 mg/kg/4D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
acute tubular necrosis)
REFERENCE :
AJKDDP American Journal of Kidney Diseases. (Grune & Stratton, Inc.,
Journal Subscription Dept., POB 6280, Duluth, MN 55806) V.1- 1981-
Volume(issue)/page/year: 22,611,1993
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Multiple routes
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 36 mg/kg/2D-I
TOXIC EFFECTS :
Brain and Coverings - other degenerative changes
Behavioral - coma
Lungs, Thorax, or Respiration - other changes
REFERENCE :
AJKDDP American Journal of Kidney Diseases. (Grune & Stratton, Inc.,
Journal Subscription Dept., POB 6280, Duluth, MN 55806) V.1- 1981-
Volume(issue)/page/year: 20,647,1992
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >20 gm/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: -,7,1990
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 860 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: 16,866,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 620 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: 16,866,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 750 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: 25,815,1994
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736)
V.1- 1869- Volume(issue)/page/year: 272,583,1978
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 724 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: 25,815,1994
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 1118 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: 16,866,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 1118 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: 16,866,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Mammal - species unspecified
DOSE/DURATION : 400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PHINDQ Pharmacy International. (Elsevier Science Pub. Co., Inc., 52
Vanderbilt Ave., New York, NY 10017) V.1- 1980- Volume(issue)/page/year:
5,191,1984
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 250 mg/kg/5D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes primarily in glomeruli
Kidney, Ureter, Bladder - urine volume increased
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
JASNEU Journal of the American Society of Nephrology. (Williams & Wilkins,
428 E. Preston St., Baltimore, MD 21202) V.1- 1990-
Volume(issue)/page/year: 8,361,1997
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE : 60 mg/kg
SEX/DURATION : female 5-6 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System
REFERENCE :
REPTED Reproductive Toxicology. (Pergamon Press Inc., Maxwell House,
Fairview Park, Elmsford, NY 10523) V.1- 1987- Volume(issue)/page/year:
5,517,1991
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 100 mg/kg
SEX/DURATION : female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
Reproductive - Effects on Newborn - weaning or lactation index (e.g., #
alive at weaning per # alive at day 4)
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan
R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968-
Volume(issue)/page/year: 36,31A,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 200 mg/kg
SEX/DURATION : female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - craniofacial
(including nose and tongue)
REFERENCE :
ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000
Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year:
61,468,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 400 mg/kg
SEX/DURATION : female 9-11 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
REFERENCE :
ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000
Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year:
61,468,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE : 1200 mg/kg
SEX/DURATION : female 1-20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
REFERENCE :
GEPHDP General Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview
Park, Elmsford, NY 10523) V.6- 1975- Volume(issue)/page/year:
26,523,1995
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Unreported
SPECIES OBSERVED : Rodent - rat
DOSE : 300 mg/kg
SEX/DURATION : female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
REFERENCE :
BJMRDK Brazilian Journal of Medical and Biological Research. (Associacao
Brasileira de Divulgacao Cientifica, Faculdade de Medicina de Ribeirao
Preto, USP, 141000 Ribeirao Preto, SP, Brazil) V.14- 1981-
Volume(issue)/page/year: 22,1457,1989
** MUTATION DATA **
TYPE OF TEST : Cytogenetic analysis
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 250 mg/L/48H
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
3,587,1983
TYPE OF TEST : Morphological transformation
TEST SYSTEM : Rodent - mouse Fibroblast
DOSE/DURATION : 50 mg/L/72H
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
3,587,1983
TYPE OF TEST : DNA inhibition
TEST SYSTEM : Rodent - mouse Leukocyte
DOSE/DURATION : 810 mg/L
REFERENCE :
BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House,
Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year:
38,1771,1989
TYPE OF TEST : Mutation in mammalian somatic cells
TEST SYSTEM : Rodent - mouse Lymphocyte
DOSE/DURATION : 400 mg/L/4H
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
3,587,1983
TYPE OF TEST : DNA inhibition
TEST SYSTEM : Rodent - rabbit Kidney
DOSE/DURATION : 6800 ug/L
REFERENCE :
BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House,
Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year:
38,1771,1989
*** END OF RECORD ***