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Quinoline, 7 - chloro - 4 - (4 - diethylamino - 1 - methyl - butylamino) - , diphosphate

RTECS #: VB2450000

CAS #: 50-63-5

UPDATE: May 2007 MW: 515.92 MF: C18H26ClN3•2H3O4P


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. NIOSH DOCUMENTATION AND SURVEILLANCE:
  8. REFERENCES:

SYNONYMS:

  1. 3377 RP
  2. 7 - Chlor - 4 - (4 - (diaethylamino) - 1 - methylbutylamino) - chinolindiphosphat (German)
  3. 7 - Chloro - 4 - ( (4' - diethylamino - 1 - methylbutyl) amino) quinoline diphosphate
  4. Alermine
  5. Aralen diphosphate
  6. Aralen phosphate
  7. Arechin
  8. Avloclor
  9. Bemaphate
  10. Chingamin
  11. Chingamin phosphate
  12. Chloroquin diphosphate
  13. Chloroquine diphosphate
  1. Chloroquine phosphate
  2. Delagil
  3. Gontochin phosphate
  4. H - Stadur
  5. Khingamin
  6. Klorokinfosfat
  7. Resochin
  8. Resoquine
  9. SN 7,618
  10. Sanoquin
  11. Tanakan
  12. Tanakan (antimalarial)
  13. WR 1522


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 repair Escherichia coli 2,223 µg/disc MUREAV 188,111,1987
mutation in microorganisms Escherichia coli 200 µg/plate (+enzymatic activation step) MUREAV 192,233,1987
mutation in microorganisms Salmonella typhimurium 250 µg/plate (+enzymatic activation step) MUREAV 192,233,1987
mutation in microorganisms Salmonella typhimurium 5 mg/plate (-enzymatic activation step) CBTOE2 2,379,1986
sister chromatid exchange hamster lung 100 µg/L CBTOE2 2,379,1986
sister chromatid exchange rat liver 100 µg/L CBTOE2 2,379,1986


REPRODUCTIVE EFFECTS DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
intraperitoneal
rat 		lowest published toxic dose: 80 mg/kg (20-21 day pregnant) Reproductive: Specific developmental abnormalities: Respiratory system

Reproductive: Effects on newborn: Physical 		AJMSDC 22,61,1993
oral
rat 		lowest published toxic dose: 1,200 mg/kg (5-16 day pregnant) Reproductive: Effects on embryo or fetus: Fetotoxicity (except death, e.g., stunted fetus) RCOCB8 7,701,1974
oral
rat 		lowest published toxic dose: 550 mg/kg (9 day pregnant) Reproductive: Specific developmental abnormalities: Eye, ear RPTOAN 30,114,1967
oral
rat 		lowest published toxic dose: 750 mg/kg (9 day pregnant) Reproductive: Effects on embryo or fetus: Fetal death RPTOAN 30,114,1967
subcutaneous
rat 		lowest published toxic dose: 475 mg/kg (10-14 day pregnant) Reproductive: Effects on newborn: Physical VAAZA2 39,59,1982


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
intramuscular
rabbit 		lowest published toxic dose: 12.5 mg/kg Blood: Change in clotting factors FATOAO 48,77,1985
intraperitoneal
mouse 		lethal dose (50 percent kill): 68 mg/kg Behavioral: Convulsions or effect on seizure threshold 85GLAQ 1,389,1946
intravenous
domestic bird 		lethal dose (50 percent kill): 64,500 µg/kg N/R ARZNAD 20,1775,1970
intravenous
dog 		lowest published lethal dose: 8 mg/kg Behavioral: Somnolence (general depressed activity) 85GLAQ 1,390,1946
intravenous
rat 		lowest published toxic dose: 121.2 µg/kg/1 hour Kidney, Ureter, and Bladder: Urine volume increased

Kidney, Ureter, and Bladder: Other changes in urine composition

Kidney, Ureter, and Bladder: Other changes 		JPETAB 306,478,2003
intravenous
rabbit 		lowest published toxic dose: 12.5 mg/kg Blood: Change in clotting factors FATOAO 48,77,1985
oral
child 		lowest published lethal dose: 250 mg/kg Behavioral: Coma ATXKA8 23,204,1968
oral
man 		lowest published toxic dose: 8,571 µg/kg Gastrointestinal: Nausea or vomiting

Gastrointestinal: Other changes 		HUTODJ 8,387,1989
oral
man 		lowest published toxic dose: 8,571 µg/kg Gastrointestinal: Ulceration or bleeding from duodeum

Gastrointestinal: Nausea or vomiting

Gastrointestinal: Other changes 		HUTODJ 8,387,1989
oral
man 		lowest published lethal dose: 179 mg/kg N/R ATXKA8 23,204,1968
oral
mouse 		lethal dose (50 percent kill): 500 mg/kg N/R TMPRAD 30,308,1979
oral
rat 		lethal dose (50 percent kill): 623 mg/kg N/R EVHPAZ 106(Suppl 2),497,1998
oral
woman 		lowest published lethal dose: 298 mg/kg Behavioral: Coma

Cardiac: Other changes

Lung, Thorax, or Respiration: Other changes 		JFSCAS 41,1077,1996
oral
woman 		lowest published toxic dose: 138 mg/kg Behavioral: Coma

Vascular: BP lowering not characterized in autonomic section

Lung, Thorax, or Respiration: Other changes 		JJTOEX 12,159,1999
oral
woman 		lowest published toxic dose: 600 mg/kg/17 week- intermittent Peripheral Nerve and Sensation: Spastic paralysis with/without sensory change

Eye: Other eye effects

Behavioral: Change in motor activity (specific assay) 		PGMJAO 55,569,1979
oral
woman 		lowest published toxic dose: 167 mg/kg Cardiac: EKG changes not diagnostic of above

Vascular: BP lowering not characterized in autonomic section

Lung, Thorax, or Respiration: Respiratory depression 		JTCTDW 19,1067,1982/1983
subcutaneous
mouse 		lethal dose (50 percent kill): 200 mg/kg N/R ATMPA2 74,393,1980
subcutaneous
mouse 		lowest published toxic dose: 5.9 mg/kg Peripheral Nerve and Sensation: Paresthesia EJPHAZ 502,233,2004
skin
mouse 		lowest published toxic dose: 25 mg/kg Immunological Including Allergic: Decrease in cellular immune response FATOAO 47,84,1984
skin
rat 		lowest published toxic dose: 25 mg/kg Biochemical: Metabolism (intermediary): Effect on inflammation or mediation of inflammation FATOAO 47,84,1984


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM 		DOSE
EFFECT

 REFERENCE
intramuscular
rabbit 		lowest published toxic dose: 62.5 mg/kg/5 day- intermittent Blood: Change in clotting factors FATOAO 48,77,1985
intraperitoneal
rat 		lowest published toxic dose: 840 mg/kg/21 day- intermittent Behavioral: Food intake (animal)

Kidney, Ureter, and Bladder: Urine volume decreased or anuria

Nutritional and Gross Metabolic: Weight loss or decreased weight gain 		MSCREJ 19,777,1991
intraperitoneal
rat 		lowest published toxic dose: 700 mg/kg/2 week- intermittent Nutritional and Gross Metabolic: Weight loss or decreased weight gain EKFAE9 60,50,1997
intraperitoneal
rat 		lowest published toxic dose: 350 mg/kg/1 week- intermittent Endocrine: Other changes EKFAE9 60,50,1997
intraperitoneal
rat 		lowest published toxic dose: 70 mg/kg/7 day- intermittent Liver: Other changes

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Cytochrome oxidases (indlucing oxidative phosphrylation)

Biochemical: Metabolism (intermediary): Effect on mitochondrial function 		DCTODJ 27,41,2004
ocular
rat 		lowest published toxic dose: 72 µg/kg/12 day- intermittent Eye: Corneal damage ARZNAD 33,827,1983
oral
dog 		lowest published toxic dose: 280 mg/kg/14 day- intermittent Behavioral: Tremor

Related to Chronic Data: Death in the "MULTIPLE DOSE" data type field 		85GLAQ 1,390,1946
oral
monkey 		lowest published toxic dose: 1 gm/kg/10 day- intermittent Liver: Fatty liver degeneration

Nutritional and Gross Metabolic: Weight loss or decreased weight gain

Related to Chronic Data: Death in the "MULTIPLE DOSE" data type field 		85GLAQ 1,390,1946
oral
rat 		lowest published toxic dose: 8,820 mg/kg/21 week- continuous Cardiac: Other changes

Liver: Hepatitis (hepatocellular necrosis), diffuse

Related to Chronic Data: Death in the "MULTIPLE DOSE" data type field 		85GLAQ 1,389,1946
oral
rat 		lowest published toxic dose: 875 mg/kg/7 day- intermittent Peripheral Nerve and Sensation: Spastic paralysis with/without sensory change

Behavioral: Ataxia

Related to Chronic Data: Death in the "MULTIPLE DOSE" data type field 		TOXID9 42,55,1998
oral
rabbit 		lowest published toxic dose: 87.5 mg/kg/7 day- intermittent Blood: Change in clotting factors FATOAO 48,77,1985
oral
woman 		lowest published toxic dose: 25 mg/kg/3 day- intermittent Behavioral: Toxic psychosis

Behavioral: Headache 		APHRER 39,551,2005
oral
woman 		lowest published toxic dose: 65.57 mg/kg/2 day- intermittent Skin: After systemic exposure: Dermatitis, other

Nutritional and Gross Metabolic: Body temperature increase 		INJPD2 36,101,2004
subcutaneous
rat 		lowest published toxic dose: 400 mg/kg/10 day- intermittent Kidney, Ureter, and Bladder: Proteinuria

Kidney, Ureter, and Bladder: Other changes in urine composition

Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Phosphatases 		TOLED5 10,145,1982
skin
mouse 		lowest published toxic dose: 250 mg/kg/10 day- intermittent Biochemical: Metabolism (intermediary): Effect on inflammation or mediation of inflammation FATOAO 47,84,1984


REVIEWS:

ORGANIZATION STANDARD
REFERENCE
TOXICOLOGY REVIEW
INTEAG 15,7,1974
TOXICOLOGY REVIEW
ARPTDI 43,441,2003
TOXICOLOGY REVIEW
MUREAV 578,88,2005


STANDARDS AND REGULATIONS:

ORGANIZATION STANDARD
REFERENCE
N/R N/R N/R


NIOSH DOCUMENTATION AND SURVEILLANCE:

ORGANIZATION STANDARD or SURVEY
REFERENCE
National Occupational Exposure Survey 1983 National Occupational Exposure Survey 1983: Hazard Code: X4486;
Number of Industries 2;
Total Number of Facilities 40;
Number of Occupations 3;
Total Number of Employees Exposed 644;
Total Number of Female Employees Exposed 238


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE
N/R


REFERENCES:

CODEN
REFERENCE
85GLAQ "A Survey of Antimalarial Drugs, 1941-1945," Wiselogle, F.Y., 2 vols., Ann Arbor, MI, J.W. Edwards, 1946
AJMSDC African Journal of Medicine and Medical Sciences. (Blackwell Scientific Publications, 238 Main St., Cambridge, MA 02142) V.5- 1976-
APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992-
ARPTDI Annual Review of Pharmacology and Toxicology. (Annual Reviews, Inc., POB 10139, Palo Alto, CA 94303) V.16- 1976-
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951-
ATMPA2 Annals of Tropical Medicine and Parasitology. (Grune & Stratton, Inc., POB 6280, Duluth, MN 55806) V.1- 1907-
ATXKA8 Archiv fuer Toxikologie. (Berlin, Fed. Rep. Ger.) V.15-31, 1954-74. For publisher information, see ARTODN.
CBTOE2 Cell Biology and Toxicology. (Princeton Scientific Pub., Inc., 301 N. Harrison St., CN 5279, Princeton, NJ 08540) V.1- 1984-
DCTODJ Drug and Chemical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.1- 1977/78-
EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967-
EKFAE9 Eksperimental'naya i Klinicheskaya Farmakologiya. Experimental and Clinical Pharmacology. (Mezhdunarodnaya Kniga, ul. B. Yakimanka, 39, 117049 Moscow, Russia) V.55- 1992-
EVHPAZ EHP, Environmental Health Perspectives. (U.S. Government Printing Office, Supt of Documents, Washington, DC 20402) No.1- 1972-
FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939-
HUTODJ Human Toxicology. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants., RG 21 2XS, UK) V.1- 1981-
INJPD2 Indian Journal of Pharmacology. (Dept. of Pharmacology, Baranas Hindu Univ., Varanasi 221 005, India) V.1- 1968(?)-
INTEAG Internist. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1960-
JFSCAS Journal of Forensic Sciences. (American Soc. for Testing and Materials, 1916 Race St., Philadelphia, PA 19103) V.1- 1956-
JJTOEX Japanese Journal of Toxicology. (Yakugyo Jihosha, Hokushin Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo, 101, Japan) V.1- 1988-
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982-
MSCREJ Medical Science Research. (Elsevier Applied Science Pub. Ltd., Crown House, Linton Rd., Barking, Essex IG11 8JU, UK) V.15- 1987-
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964-
PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925-
RCOCB8 Research Communications in Chemical Pathology and Pharmacology. (PJD Pub. Ltd., P.O. Box 966, Westbury, NY 11590) V.1- 1970-
RPTOAN Russian Pharmacology and Toxicology (English Translation). Translation of FATOAO. (Euromed Pub., 33, Woodlands Rd., Surbiton, Surrey, UK) V.30- 1967-
TMPRAD Tropenmedizin und Parasitologie. (Georg Thieme Verlag, Postfach 732, D-7000 Stuttgart 1, Fed. Rep. Ger.) V.25- 1974-
TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977-
TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981-
VAAZA2 Virchows Archiv, Abteilung B: Cell Pathology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.1- 1968-

Used for the treatment of malaria

FDA-proprietary drug

RTECS Compound Description:
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   Mutagen
   Reproductive Effector
   Human Data

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