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2 - Benzimidazolinone, 1 - (1 - (3 - (p - fluorobenzoyl) propyl) - 1,2,3,6 - tetrahydro - 4 - pyridyl) -

RTECS #: DE2100000

CAS #: 548-73-2


UPDATE: February 2009 MW: 379.47 MF: C22H22FN3O2


NOTE:

TABLE OF CONTENTS:
  1. SYNONYMS:
  2. REPRODUCTIVE EFFECTS DATA:
  3. ACUTE TOXICITY DATA:
  4. REVIEWS:
  5. NIOSH DOCUMENTATION AND SURVEILLANCE:
  6. STATUS IN FEDERAL AGENCIES:
  7. REFERENCES:

SYNONYMS:

  1. 1 - (1 - (3 - (p - Fluorobenzoyl) propyl) - 1,2,3,6 - tetrahydro - 4 - pyridyl) - 2 - benzimidazolinone
  2. 1 - (1 - (4 - (p - Fluorophenyl) - 4 - oxobutyl) - 1,2,3,6 - tetrahydro - 4 - pyridyl) - 2 - benzimidazolinone
  3. Dehydrobenzperidol
  4. Deidrobenzperidolo
  5. Dridol
  6. Droleptan
  7. Droperidol
  8. Halkan
  9. Inapsin
  1. Inapsine
  2. Inopsin
  3. Inoval
  4. McN - JR - 4749
  5. Properidol
  6. R 4749
  7. Sintosian
  8. Thalamonal
  9. Vetkalm


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
N/R N/R N/R N/R


REPRODUCTIVE EFFECTS DATA AND REFERENCES:

ROUTE/
ORGANISM
DOSE
EFFECT

REFERENCE
intravenous
rat
lowest published toxic dose: 0.88 mg/kg (1 day after birth) Reproductive: Maternal effects: Uterus, cervix, vagina

Reproductive: Maternal effects: Postpartum
LIFSAK 72,1093,2003


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
human
lowest published toxic dose: 41.7 µg/kg Behavioral: Somnolence (general depressed activity)

Behavioral: Analgesia
AJEMEN 20,39,2002
intramuscular
human
lowest published toxic dose: 0.7 mg/kg Behavioral: Analgesia AEMME* 8,873,2001
intramuscular
human
lowest published lethal dose: 0.7 mg/kg Cardiac: Arrythmias (indlucing changes in conduction)

Cardiac: EKG changes not diagnostic of above
AEMED3 41,546,2003
intraperitoneal
mouse
lethal dose (50 percent kill): 72 mg/kg Behavioral: Somnolence (general depressed activity)

Behavioral: Convulsions or effect on seizure threshold

Lung, Thorax, or Respiration: Dyspnea
ZMZADD 5(2),65,1985
intravenous
human
lowest published toxic dose: 0.3 mg/kg Behavioral: Analgesia AEMME* 8,873,2001
intravenous
human
lowest published toxic dose: 0.1 mg/kg Cardiac: Arrythmias (indlucing changes in conduction) AEMED3 41,546,2003
intravenous
human
lowest published toxic dose: 0.1 mg/kg Cardiac: EKG changes not diagnostic of above AEMED3 41,546,2003
intravenous
human
lowest published toxic dose: 0.9 mg/kg Cardiac: Arrythmias (indlucing changes in conduction)

Cardiac: Pulse rate increased without fall in BP

Lung, Thorax, or Respiration: Dyspnea
AEMED3 41,546,2003
intravenous
human
lowest published toxic dose: 0.9 mg/kg Biochemical: Enzyme inhibition, induction, or change in blood or tissue levels: Other enzymes AEMED3 41,546,2003
intravenous
man
lowest published toxic dose: 133 µg/kg Behavioral: Coma JCLPDE 47,94,1986
intravenous
man
lowest published toxic dose: 80 µg/kg Behavioral: Rigidity (includes catalepsy)

Lung, Thorax, or Respiration: Dyspnea

Skin and Appendages: Other: Sweating
JKMSEH 17,715,2002
intravenous
man
lowest published toxic dose: 0.36 mg/kg Behavioral: Convulsions or effect on seizure threshold

Cardiac: Change in rate

Lung, Thorax, or Respiration: Respiratory obstruction
AEMED3 41,546,2003
intravenous
mouse
lethal dose (50 percent kill): 20 mg/kg Behavioral: Convulsions or effect on seizure threshold

Lung, Thorax, or Respiration: Dyspnea
ARZNAD 13,205,1963
intravenous
rat
lethal dose (50 percent kill): 30 mg/kg Behavioral: Convulsions or effect on seizure threshold

Lung, Thorax, or Respiration: Dyspnea
ARZNAD 13,205,1963
intravenous
woman
lowest published toxic dose: 20 µg/kg Gastrointestinal: Other changes AANEAB 45,501,2001
intravenous
woman
lowest published toxic dose: 12.5 mg/kg Cardiac: Arrythmias (indlucing changes in conduction) AEMED3 41,546,2003
oral
human
lowest published toxic dose: 223 µg/kg/12 day- intermittent Behavioral: Wakefulness

Behavioral: Tremor

Behavioral: Muscle weakness
ARZNAD 22,93,1972
oral
mouse
lethal dose : >160 mg/kg N/R ARZNAD 13,205,1963
oral
rat
lethal dose (50 percent kill): 750 mg/kg N/R TXAPA9 18,185,1971
parenteral
human
lowest published lethal dose: 0.36 mg/kg N/R AJEMEN 22,27,2004
subcutaneous
mammal (species unspecified)
lowest published toxic dose: 1 mg/kg Gastrointestinal: Decreased motility or constipation EJPHAZ 544,153,2006
subcutaneous
mouse
lethal dose (50 percent kill): 125 mg/kg N/R TXAPA9 6,63,1964
subcutaneous
rat
lethal dose (50 percent kill): >100 mg/kg N/R NIIRDN 6,533,1982
unreported route
mammal (species unspecified)
lowest published toxic dose: 1 mg/kg Blood: Change in clotting factors FATOAO 49,46,1986


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM
DOSE
EFFECT

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


REVIEWS:

ORGANIZATION STANDARD
REFERENCE

TOXICOLOGY REVIEW
IDPYAK 1,203,1974
TOXICOLOGY REVIEW
MDCHAG 4(2),199,1967
TOXICOLOGY REVIEW
ARPTDI 43,441,2003
TOXICOLOGY REVIEW
CMAJAX 166,932,2002
TOXICOLOGY REVIEW
AEMED3 41,546,2003
TOXICOLOGY REVIEW
TPHSDY 24,619,2003
TOXICOLOGY REVIEW
ENTOX* -,372,2005
TOXICOLOGY REVIEW
AJEMEN 22,28,2004
TOXICOLOGY REVIEW
PSBUL* 35,66,2001
TOXICOLOGY REVIEW
PSBUL* 36,91,2002


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: X4644;
Number of Industries 2;
Total Number of Facilities 310;
Number of Occupations 5;
Total Number of Employees Exposed 3,340;
Total Number of Female Employees Exposed 2,588


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE

EPA TSCA TEST SUBMISSION (TSCATS) DATA BASE, JANUARY 2001


REFERENCES:

CODEN
REFERENCE

AANEAB Acta Anaesthesiologica Scandinavica. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.1- 1957-
AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038)
AEMME* Academic emergency medicine: official journal of the Society for Academic Emergency Medicine (Philadelphia Pa Hanley And Belfus) V.1- 1994-
AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983-
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-
CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911-
EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967-
ENTOX* Encyclopedia of Toxicology: Reference Book, Elsevier, 2005
FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939-
IDPYAK Industrial Pharmacology. (Mount Kisco, NY) V.1-3, 1974-79. Discontinued.
JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978-
JKMSEH Journal of Korean Medical Science. (Korean Academy of Medical Science, C.P.O. Box 2062, Seoul, S. Korea) V.1- 1986-
LIFSAK Life Sciences. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1-8, 1962-69; V.14- 1974-
MDCHAG Medicinal Chemistry: A Series of Monographs. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1963-
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan)
PSBUL*
TPHSDY Trends in Pharmacological Sciences. (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.1- 1979-
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959-
ZMZADD Zhonghua Mazuixue Zazhi. Chinese Journal of Anesthesiology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1981-

Used as an antipsychotic agent

FDA-proprietary drug

RTECS Compound Description:
   Drug
   Human Data

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