*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : UV1164800
CHEMICAL NAME : 4H-Pyrido(1,2-a)pyrimidin-4-one,
6,7,8,9-tetrahydro-3-(2-(4-(6-fluoro-1,2-benzisoxazol
-3-yl)- 1-piperidinyl)ethyl)-2-methyl-
CAS REGISTRY NUMBER : 106266-06-2
BEILSTEIN REFERENCE NO. : 4891881
LAST UPDATED : 199712
DATA ITEMS CITED : 13
MOLECULAR FORMULA : C23-H27-F-N4-O2
MOLECULAR WEIGHT : 410.54
COMPOUND DESCRIPTOR : Drug
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* R 64766
* Risperidone
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 3428 ug/kg
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions
Cardiac - EKG changes not diagnostic of specified effects
Nutritional and Gross Metabolic - changes in sodium
REFERENCE :
AEMED3 Annals of Emergency Medicine. (American College of Emergency
Physicians, 1125 Executive Circle, Irving, TX 75038)
Volume(issue)/page/year: 22,1908,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 429 ug/kg/15D-I
TOXIC EFFECTS :
Brain and Coverings - changes in surface EEG
Behavioral - anorexia (human)
Behavioral - alteration of operant conditioning
REFERENCE :
JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press,
Inc., POB 240008, Memphis, TN 38124) V.39- 1978-
Volume(issue)/page/year: 58,323,1997
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 114 ug/kg/2D-I
TOXIC EFFECTS :
Behavioral - wakefulness
Behavioral - euphoria
Behavioral - excitement
REFERENCE :
AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc.,
Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921-
Volume(issue)/page/year: 153,1234,1996
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 56600 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams &
Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
Volume(issue)/page/year: 244,685,1988
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Subcutaneous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 98 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - somnolence (general depressed activity)
Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 27,2991,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 34300 ug/kg
TOXIC EFFECTS :
Behavioral - tremor
Behavioral - convulsions or effect on seizure threshold
Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 27,2991,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 63100 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams &
Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
Volume(issue)/page/year: 244,685,1988
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 26900 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams &
Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
Volume(issue)/page/year: 244,685,1988
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 18300 ug/kg
TOXIC EFFECTS :
Behavioral - muscle weakness
Lungs, Thorax, or Respiration - respiratory stimulation
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 27,2991,1993
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 14100 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams &
Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10-
Volume(issue)/page/year: 244,685,1988
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 228 mg/kg/13W-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in erythrocyte (RBC) count
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 27,2991,1993
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 2738 mg/kg/1Y-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes
Endocrine - other changes
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 27,2991,1993
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 110 mg/kg
SEX/DURATION : female 8-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda
Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960-
Volume(issue)/page/year: 27,3023,1993
*** END OF RECORD ***