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Pyrimidine, 2,4 - diamino - 5 - (3,4,5 - trimethoxybenzyl) -

RTECS #: UV8225000

CAS #: 738-70-5

UPDATE: May 2009 MW: 290.36 MF: C14H18N4O3


NOTE:

TABLE OF CONTENTS:
  1. SYNONYMS:
  2. MUTATION DATA:
  3. REPRODUCTIVE EFFECTS DATA:
  4. ACUTE TOXICITY DATA:
  5. OTHER MULTIPLE DOSE DATA:
  6. REVIEWS:
  7. STANDARDS AND REGULATIONS:
  8. NIOSH DOCUMENTATION AND SURVEILLANCE:
  9. STATUS IN FEDERAL AGENCIES:
  10. REFERENCES:

SYNONYMS:

  1. 2,4 - Diamino - 5 - (3,4,5 - trimethoxybenzyl) pyrimidine
  2. 2,4 - Pyrimidinediamine, 5 - ( (3,4,5 - trimethoxyphenyl) - methyl) -
  3. 5 - (3,4,5 - Trimethoxybenzyl) - 2,4 - diaminopyrimidine
  4. BW 56 - 72
  5. Monoprim
  6. NIH 204
  7. NSC - 106568
  8. Proloprim
  9. Syraprim
  1. Tiempe
  2. Trimanyl
  3. Trimethoprim
  4. Trimetoprim (Polish)
  5. Trimopan
  6. Trimpex
  7. WR 5949
  8. Wellcoprim


SKIN AND EYE IRRITATION DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
N/R
 N/R N/R N/R


MUTATION DATA AND REFERENCES:

SYSTEM TEST ROUTE/
ORGANISM/
TISSUE 		DOSE REFERENCE
DNA inhibition human lymphocyte 10 µmol/L BCPCA6 26,1593,1977
mutation in microorganisms other microorganisms 50 µg/plate (-enzymatic activation step) AMACCQ 12,84,1977
mutation in microorganisms Salmonella typhimurium 15 µg/plate (+/-enzymatic activation step) MUREAV 188,197,1987
micronucleus test human lymphocyte 5 mg/L MUREAV 440,157,1999
other mutation test systems human lymphocyte 50 µmol/L BCPCA6 26,1593,1977
phage inhibition capacity Escherichia coli 10 µg/plate CNREA8 43,2819,1983
sister chromatid exchange human lymphocyte 5 mg/L MUREAV 440,157,1999
sex chromosome loss and nondisjunction Neurospora crassa 62 mg/L MUREAV 167,35,1986
sperm morphology unreported route
rat 		800 mg/kg/8 day JOURAA 112,348,1974


REPRODUCTIVE EFFECTS DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
oral
rat 		lowest published toxic dose: 2,250 mg/kg (11-13 day pregnant) Reproductive: Effects on 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) 		ANANAU 149,151,1981


TUMORIGENIC DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
N/R
 N/R N/R N/R


ACUTE TOXICITY DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
inhalation
rat 		lowest published toxic concentration: 36.5 mg/m3/4 hour Behavioral: Alteration of classical conditioning

Kidney, Ureter, and Bladder: Proteinuria

Blood: Changes in serum composition (e.g. TP, bilirubin, cholesterol) 		TOVEFN (2),34,1998
inhalation
rat 		lowest published toxic concentration: 36.5 mg/m3/4 hour Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Transaminases TOVEFN (2),34,1998
intraperitoneal
mouse 		lethal dose (50 percent kill): 400 mg/kg N/R TOVEFN (2),34,1998
intraperitoneal
rat 		lethal dose (50 percent kill): 500 mg/kg N/R TOVEFN (2),34,1998
intravenous
dog 		lowest published lethal dose: 90 mg/kg Vascular: BP lowering not characterized in autonomic section CHTHBK 14,37,1969
intravenous
mouse 		lethal dose (50 percent kill): 132 mg/kg N/R JCHEEU 5,400,1993
oral
mouse 		lethal dose (50 percent kill): 2,764 mg/kg N/R USXXAM #4180578
oral
rat 		lethal dose (50 percent kill): >5,300 mg/kg N/R TOVEFN (2),34,1998
oral
woman 		lowest published toxic dose: 56 mg/kg/7 day- intermittent Kidney, Ureter, and Bladder: Hematuria

Blood: Other changes

Musculoskeletal: Joints 		PGMJAO 68,391,1992
oral
woman 		lowest published toxic dose: 60 mg/kg/10 day- intermittent Blood: Thrombocytopenia NZMJAX 106,251,1993
subcutaneous
mouse 		lethal dose (50 percent kill): >5 gm/kg N/R NKRZAZ 21,175,1973
subcutaneous
rat 		lethal dose (50 percent kill): >5 gm/kg N/R NKRZAZ 21,175,1973


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
oral
monkey 		lowest published toxic dose: 27,300 mg/kg/13 week- intermittent Brain and Coverings: Recordings from specific areas of CNS

Nutritional and Gross Metabolic: Weight loss or decreased weight gain

Related to Chronic Data: Death in the "MULTIPLE DOSE" data type field 		JCHEEU 5,400,1993
oral
rat 		lowest published toxic dose: 31,800 mg/kg/30 day- intermittent Blood: Changes in bone marrow not included in above BCTKAG 10,267,1977
oral
rabbit 		lowest published toxic dose: 31,800 mg/kg/30 day- intermittent Blood: Changes in bone marrow not included in above

Related to Chronic Data: Death in the "MULTIPLE DOSE" data type field 		BCTKAG 10,267,1977


REVIEWS:

ORGANIZATION STANDARD
REFERENCE
TOXICOLOGY REVIEW
HFHBAG 29,364,1974
TOXICOLOGY REVIEW
NEJMAG 343,1608,2000
TOXICOLOGY REVIEW
MUREAV 488,151,2001
TOXICOLOGY REVIEW
TOLED5 142,207,2003
TOXICOLOGY REVIEW
TOLED5 144,383,2003
TOXICOLOGY REVIEW
TPHSDY 23,397,2002
TOXICOLOGY REVIEW
EMMUEG 43,143,2004
TOXICOLOGY REVIEW
JAADDB 56,181,2007
TOXICOLOGY REVIEW
HUTOX* -,429,1996


STANDARDS AND REGULATIONS:

ORGANIZATION STANDARD
REFERENCE
Occupational Exposure Limit - RUSSIA short term exposure limit 0.5 mg/m3, JUN2003


NIOSH DOCUMENTATION AND SURVEILLANCE:

ORGANIZATION STANDARD or SURVEY
REFERENCE
National Occupational Exposure Survey 1983 National Occupational Exposure Survey 1983: Hazard Code: X4630;
Number of Industries 4;
Total Number of Facilities 918;
Number of Occupations 9;
Total Number of Employees Exposed 21,309;
Total Number of Female Employees Exposed 16,105


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE
EPA GENETOX PROGRAM 1988, Positive: N crassa-aneuploidy


REFERENCES:

CODEN
REFERENCE
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
ANANAU Anatomischer Anzeiger. (VEB Gustav Fischer Verlag, Postfach 176, Jena DDR-6900, Ger. Dem. Rep.) V.1- 1886-
BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958-
BCTKAG Bromatologia i Chemia Toksykologiczna. (Ars Polona, POB 1001, 00-068 Warsaw 1, Poland) V.4- 1971-
CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968-
CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941-
EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987-
HFHBAG Hartford Hospital Bulletin. (Hartford Hospital, 80 Seymour St., Hartford, CT 06115) V.1- 1938/39-
HUTOX*
JAADDB Journal of the American Academy of Dermatology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63141) 1979-
JCHEEU Journal of Chemotherapy. (Edizioni Riviste Scientifiche, via R. Giuliani, 419, 50141 Florence, Italy) V.1- 1989-
JOURAA Journal of Urology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1917-
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964-
NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928-
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953-
NZMJAX New Zealand Medical Journal. (New Zealand Medical Assoc., P.O. Box 156, Wellington, New Zealand) V.1- 1900-
PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925-
TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977-
TOVEFN Toksikologicheskii Vestnik. (18-20 Vadkovskii per. Moscow, 101479, Russia) History Unknown
TPHSDY Trends in Pharmacological Sciences. (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.1- 1979-
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231)

Used as an immunosuppressant

FDA-proprietary drug

RTECS Compound Description:
   Drug
   Mutagen
   Reproductive Effector
   Human Data

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