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Quinazoline, 4 - amino - 6,7 - dimethoxy - 2 - (4 - (2 - furoyl) piperazin - 1 - yl) - , hydrochloride

RTECS #: VA1350000

CAS #: 19237-84-4


UPDATE: February 2009 MW: 419.91 MF: C19H21N5O4•ClH


NOTE:

TABLE OF CONTENTS:
  1. SYNONYMS:
  2. REPRODUCTIVE EFFECTS DATA:
  3. ACUTE TOXICITY DATA:
  4. OTHER MULTIPLE DOSE DATA:
  5. NIOSH DOCUMENTATION AND SURVEILLANCE:
  6. REFERENCES:

SYNONYMS:

  1. 1 - (4 - Amino - 6,7 - dimethoxy - 2 - quinazolinyl) - 4 - (2 - furanylcarbonyl) piperazine hydrochloride
  2. 1 - (4 - Amino - 6,7 - dimethoxy - 2 - quinazolinyl) - 4 - (2 - furoyl) piperazine monohydrochloride
  3. 2 - (4 - (2 - Furoyl) piperazin - 1 - yl) - 4 - amino - 6,7 - dimethoxyquinazoline hydrochloride
  4. CP - 12299 - 1
  5. Deprazolin
  6. Furazosin hydrochloride
  7. Hypovase
  8. Hypovasole
  1. Minipress
  2. Peripress
  3. Piperazine, 1 - (4 - amino - 6,7 - dimethoxy - 2 - quinazolinyl) - 4 - (2 - furoyl) - , monohydrochloride
  4. Pratsiol
  5. Prazosin clorhidrato (Spanish)
  6. Prazosin hydrochloride
  7. Sinetens


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
implant
rat
lowest published toxic dose: 30 mg/kg (3 day male) Reproductive: Paternal effects: Spermatogenesis (including genetic material, sperm morphology, motility, and count)

Reproductive: Effects on fertility: Male fertility index (e.g., # males impregnating females per # males exposed to fertile nonpregnant females)
JRPFA4 70,643,1984
oral
rat
lowest published toxic dose: 4,150 mg/kg (8 week male/2 week prior to copulation-9 day pregnant) Reproductive: Effects on embryo or fetus: Fetotoxicity (except death, e.g., stunted fetus) OYYAA2 17,57,1979
oral
rat
lowest published toxic dose: 300 mg/kg (9-14 day pregnant) Reproductive: Effects on embryo or fetus: Fetal death OYYAA2 17,57,1979
oral
rat
lowest published toxic dose: 8,700 mg/kg (14-22 day pregnant/20 day after birth) Reproductive: Effects on newborn: Viability index (e.g., # alive at day 4 per # born alive) OYYAA2 17,57,1979
oral
rat
lowest published toxic dose: 1,450 mg/kg (14-22 day pregnant/20 day after birth) Reproductive: Effects on newborn: Weaning or lactation index (e.g., # alive at weaning per # alive at day 4) OYYAA2 17,57,1979
oral
rabbit
lowest published toxic dose: 90 mg/kg (9-14 day pregnant) Reproductive: Effects on embryo or fetus: Fetal death OYYAA2 17,57,1979
oral
rabbit
lowest published toxic dose: 450 mg/kg (9-14 day pregnant) Reproductive: Effects on embryo or fetus: Fetotoxicity (except death, e.g., stunted fetus) OYYAA2 17,57,1979
subcutaneous
rat
lowest published toxic dose: 4 mg/kg (22 day pregnant) Reproductive: Maternal effects: Parturition JRPFA4 76,415,1986
subcutaneous
rat
lowest published toxic dose: 12 mg/kg (4-5 day pregnant) Reproductive: Maternal effects: Uterus, cervix, vagina

Reproductive: Other effects on female
JRPFA4 81,51,1987
subcutaneous
rat
lowest published toxic dose: 1,400 mg/kg (1 day male) Reproductive: Paternal effects: Testes, epididymis, sperm duct

Reproductive: Effects on fertility: Male fertility index (e.g., # males impregnating females per # males exposed to fertile nonpregnant females)

Reproductive: Effects on fertility: Pre- implantation mortality (e.g., reduction in number of implants per female; total number of implants per corpora lutea)
CCPTAY 41,441,1990
unreported route
dog
lowest published toxic dose: 9,125 mg/kg (52 week male) Reproductive: Paternal effects: Testes, epididymis, sperm duct YHTPAD 18,343,1983
unreported route
rat
lowest published toxic dose: 9,125 mg/kg (52 week male) Reproductive: Paternal effects: Testes, epididymis, sperm duct YHTPAD 18,343,1983


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
intraperitoneal
mouse
lethal dose (50 percent kill): 60 mg/kg Behavioral: Somnolence (general depressed activity)

Behavioral: Ataxia

Gastrointestinal: Hypermotility, diarrhea
OYYAA2 17,39,1979
intraperitoneal
mouse
lowest published toxic dose: 1 mg/kg Nutritional and Gross Metabolic: Body temperature decrease PHTOEH 93,48,2003
intraperitoneal
mouse
lowest published toxic dose: 0.125 mg/kg Behavioral: Analgesia PHMCAA 68,154,2003
intraperitoneal
mouse
lowest published toxic dose: 0.25 mg/kg Eye: Ptosis

Behavioral: Tremor

Behavioral: Change in motor activity (specific assay)
AEPPAE 369,338,2004
intraperitoneal
rat
lethal dose (50 percent kill): 102 mg/kg Eye: Lacrimation

Behavioral: Somnolence (general depressed activity)

Lung, Thorax, or Respiration: Respiratory depression
OYYAA2 17,39,1979
intraperitoneal
rat
lowest published toxic dose: 0.3 mg/kg Behavioral: Change in motor activity (specific assay) PSCHDL 169,176,2003
intraperitoneal
rat
lowest published toxic dose: 8 mg/kg Behavioral: Alteration of operant conditioning PSCHDL 171,212,2004
intravenous
dog
lowest published toxic dose: 2,981 ng/kg Vascular: BP lowering not characterized in autonomic section EJPHAZ 497,327,2004
intravenous
dog
lowest published toxic dose: 4,031 ng/kg Autonomic Nervous System: Central sympatholytic

Kidney, Ureter, and Bladder: Other changes
EJPHAZ 497,327,2004
intravenous
dog
lowest published toxic dose: 5.3 µg/kg Reproductive: Paternal effects: Testes, epididymis, sperm duct EJPHAZ 580,256,2008
intravenous
dog
lowest published toxic dose: 13 µg/kg Kidney, Ureter, and Bladder: Structural or functional change in ureter

Reproductive: Paternal effects: Testes, epididymis, sperm duct
EJPHAZ 580,256,2008
intravenous
guinea pig
lowest published toxic dose: 0.1 mg/kg Vascular: BP lowering not characterized in autonomic section EJPHAZ 452,97,2002
intravenous
mouse
lethal dose (50 percent kill): 92 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Ataxia

Lung, Thorax, or Respiration: Dyspnea
NCDREP 4,1,1986
intravenous
rat
lethal dose (50 percent kill): 73 mg/kg Behavioral: Convulsions or effect on seizure threshold

Behavioral: Ataxia

Lung, Thorax, or Respiration: Dyspnea
NCDREP 4,1,1986
intravenous
rat
lowest published toxic dose: 0.3 mg/kg Peripheral Nerve and Sensation: Recording from afferent nerve EJPHAZ 489,207,2004
intravenous
rat
lowest published toxic dose: 1 µg/kg Vascular: BP lowering not characterized in autonomic section BJPCBM 145,567,2005
intravenous
rabbit
lowest published toxic dose: 3,000 µg/kg Eye: Miosis (pupilliary constriction) AEPPAE 372,346,2006
oral
dog
lethal dose (50 percent kill): >700 mg/kg Gastrointestinal: Changes in structure or function of salivary glands

Gastrointestinal: Nausea or vomiting

Kidney, Ureter, and Bladder: Other changes
OYYAA2 17,39,1979
oral
human
lowest published toxic dose: 285 µg/kg Vascular: BP lowering not characterized in autonomic section JAMAAP 238,157,1977
oral
man
lowest published toxic dose: 1,714 µg/kg Behavioral: Coma

Lung, Thorax, or Respiration: Dyspnea
HUTODJ 4,53,1985
oral
mouse
lethal dose (50 percent kill): 5 gm/kg N/R MDACAP 11,64,1975
oral
rat
lethal dose (50 percent kill): 1,950 mg/kg Gastrointestinal: Changes in structure or function of salivary glands

Gastrointestinal: Nausea or vomiting

Kidney, Ureter, and Bladder: Other changes
OYYAA2 17,39,1979
oral
woman
lowest published toxic dose: 13 mg/kg/6 week- intermittent Brain and Coverings: Encephalitis

Behavioral: Somnolence (general depressed activity)

Behavioral: Toxic psychosis
BMJOAE 293,1347,1986
oral
woman
lowest published toxic dose: 10 µg/kg Behavioral: Coma

Vascular: BP lowering not characterized in autonomic section

Skin and Appendages: Other: Sweating
DICPBB 21,723,1987
subcutaneous
mouse
lethal dose (50 percent kill): 3,100 mg/kg Behavioral: Somnolence (general depressed activity)

Behavioral: Ataxia

Lung, Thorax, or Respiration: Respiratory depression
OYYAA2 17,39,1979
subcutaneous
rat
lethal dose (50 percent kill): 3,750 mg/kg Eye: Lacrimation

Behavioral: Somnolence (general depressed activity)

Lung, Thorax, or Respiration: Respiratory depression
OYYAA2 17,39,1979
subcutaneous
rat
lowest published toxic dose: 0.5 mg/kg Behavioral: Alteration of classical conditioning

Behavioral: Change in psychophysiological tests
PSCHDL 177,438,2005


OTHER MULTIPLE DOSE DATA AND REFERENCES:

ROUTE/
ORGANISM
DOSE
EFFECT

REFERENCE
intraperitoneal
rat
lowest published toxic dose: 2.6 mg/kg/7 day- intermittent Brain and Coverings: Other degenerative changes PHREP* 57,850,2005
oral
rat
lowest published toxic dose: 19,840 mg/kg/31 day- intermittent Cardiac: Changes in heart weight

Blood: Changes in serum composition (e.g. TP, bilirubin, cholesterol)

Related to Chronic Data: Changes in ovarian weight
OYYAA2 17,39,1979
oral
rat
lowest published toxic dose: 582 gm/kg/5 week- intermittent Kidney, Ureter, and Bladder: Other changes

Endocrine: Changes in spleen weight

Blood: Changes in serum composition (e.g. TP, bilirubin, cholesterol)
OYYAA2 17,39,1979


REVIEWS:

ORGANIZATION STANDARD
REFERENCE

N/R N/R N/R


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: X4879;
Number of Industries 1;
Total Number of Facilities 70;
Number of Occupations 1;
Total Number of Employees Exposed 1,092;
Total Number of Female Employees Exposed 700


STATUS IN FEDERAL AGENCIES:

ORGANIZATION
REFERENCE

N/R


REFERENCES:

CODEN
REFERENCE

AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC.
BJPCBM British Journal of Pharmacology. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.34- 1968-
BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857-
CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970-
DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969-
EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967-
HUTODJ Human Toxicology. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants., RG 21 2XS, UK) V.1- 1981-
JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883-
JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960-
MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965-
NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985-
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967-
PHMCAA Pharmacologist. (American Soc. for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20014) V.1- 1959-
PHREP*
PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987-
PSCHDL Psychopharmacology (Berlin). (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.47- 1976-
YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU.

Used as an antihypertensive drug

FDA-proprietary drug

RTECS Compound Description:
   Drug
   Reproductive Effector
   Human Data

ALT CAS #: 86126-06-9
Click Here for Additional Information about RTECS

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