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Substance Name: Risperidone [USAN:USP:INN:BAN]
RN: 106266-06-2
UNII: L6UH7ZF8HC
InChIKey: RAPZEAPATHNIPO-UHFFFAOYSA-N

Note

  • A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.

Molecular Formula

  • C23-H27-F-N4-O2

Molecular Weight

  • 410.4903
 

Classification Codes

  • Antipsychotic Agents
  • Central Nervous System Agents
  • Central Nervous System Depressants
  • Dopamine Agents
  • Dopamine Antagonists
  • Drug / Therapeutic Agent
  • Human Data
  • Neuroleptic
  • Neurotransmitter Agents
  • Psychotropic Drugs
  • Reproductive Effect
  • Serotonin Agents
  • Serotonin Antagonists
  • Tranquilizing Agents

Names and Synonyms

Name of Substance

  • Risperidone
  • Risperidone [USAN:USP:INN:BAN]

MeSH Heading

  • Risperidone

Synonyms

  • 3-(2-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino)ethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido(1,2-a)pyrimidin-4-one
  • Apexidone
  • BRN 4891881
  • HSDB 7580
  • Psychodal
  • R 64 766
  • R 64,766
  • R 64766
  • Risperdal
  • Risperdal Consta
  • Risperidal M-Tab
  • Risperidona
  • Risperidona [Spanish]
  • Risperidone
  • Risperidonum
  • Risperidonum [Latin]
  • Risperin
  • Rispolept
  • Rispolin
  • Sequinan
  • Spiron
  • UNII-L6UH7ZF8HC
  • Zophrenal

Systematic Names

  • 4H-Pyrido(1,2-a)pyrimidin-4-one, 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-
  • 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-

Registry Numbers

CAS Registry Number

  • 106266-06-2

FDA UNII

  • L6UH7ZF8HC

System Generated Number

  • 0106266062

Structure Descriptors

InChI

1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3

InChIKey

RAPZEAPATHNIPO-UHFFFAOYSA-N

Smiles

Cc1c(c(=O)n2c(n1)CCCC2)CCN3CCC(CC3)c4c5ccc(cc5on4)F

Toxicity

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
child TDLo oral 268ug/kg (0.268mg/kg) BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

BEHAVIORAL: TREMOR

SENSE ORGANS AND SPECIAL SENSES: OTHER: EYE		 Annals of Pharmacotherpy. Vol. 30, Pg. 360, 1996.
dog LD50 intravenous 14100ug/kg (14.1mg/kg)   Journal of Pharmacology and Experimental Therapeutics. Vol. 244, Pg. 685, 1988.
dog LD50 oral 18300ug/kg (18.3mg/kg) GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"

BEHAVIORAL: MUSCLE WEAKNESS

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY STIMULATION		 Kiso to Rinsho. Clinical Report. Vol. 27, Pg. 2991, 1993.
man TDLo oral 114ug/kg/2D-I (0.114mg/kg) BEHAVIORAL: EUPHORIA

BEHAVIORAL: EXCITEMENT

BEHAVIORAL: WAKEFULNESS		 American Journal of Psychiatry. Vol. 153, Pg. 1234, 1996.
man TDLo oral 429ug/kg (0.429mg/kg) CARDIAC: EKG CHANGES NOT DIAGNOSTIC OF ABOVE

CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP

SENSE ORGANS AND SPECIAL SENSES: MIOSIS (PUPILLARY CONSTRICTION): EYE		 American Journal of Emergency Medicine. Vol. 16, Pg. 498, 1998.
man TDLo oral 429ug/kg/15D- (0.429mg/kg) BEHAVIORAL: ANOREXIA (HUMAN

BEHAVIORAL: ALTERATION OF OPERANT CONDITIONING

BRAIN AND COVERINGS: CHANGES IN SURFACE EEG		 Journal of Clinical Psychiatry. Vol. 58, Pg. 323, 1997.
man TDLo oral 3428ug/kg (3.428mg/kg) BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"

CARDIAC: EKG CHANGES NOT DIAGNOSTIC OF ABOVE		 Annals of Emergency Medicine. Vol. 22, Pg. 1908, 1993.
man TDLo oral 3857ug/kg (3.857mg/kg) CARDIAC: EKG CHANGES NOT DIAGNOSTIC OF ABOVE

CARDIAC: PULSE RATE

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Journal of Toxicology, Clinical Toxicology. Vol. 37, Pg. 893, 1999.
mouse LD50 intravenous 26900ug/kg (26.9mg/kg)   Journal of Pharmacology and Experimental Therapeutics. Vol. 244, Pg. 685, 1988.
mouse LD50 oral 63100ug/kg (63.1mg/kg)   Journal of Pharmacology and Experimental Therapeutics. Vol. 244, Pg. 685, 1988.
rat LD50 intravenous 34300ug/kg (34.3mg/kg)   Kiso to Rinsho. Clinical Report. Vol. 27, Pg. 2991, 1993.
rat LD50 intravenous 34300ug/kg (34.3mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: TREMOR		 Kiso to Rinsho. Clinical Report. Vol. 27, Pg. 2991, 1993.
rat LD50 oral 56600ug/kg (56.6mg/kg)   Journal of Pharmacology and Experimental Therapeutics. Vol. 244, Pg. 685, 1988.
rat LD50 subcutaneous 98mg/kg (98mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

LUNGS, THORAX, OR RESPIRATION: DYSPNEA

SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE		 Kiso to Rinsho. Clinical Report. Vol. 27, Pg. 2991, 1993.
women TDLo oral 400ug/kg (0.4mg/kg) CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP

BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY)		 American Journal of Emergency Medicine. Vol. 16, Pg. 498, 1998.
women TDLo oral 880ug/kg (0.88mg/kg) CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION)

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)		 American Journal of Emergency Medicine. Vol. 16, Pg. 498, 1998.
women TDLo oral 1840ug/kg (1.84mg/kg) BEHAVIORAL: HEADACHE

VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION

BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"		 Journal of Clinical Psychiatry. Vol. 56, Pg. 514, 1995.
women TDLo oral 2mg/kg (2mg/kg) VASCULAR: BP ELEVATION NOT CHARACTERIZED IN AUTONOMIC SECTION

CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION)

CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP		 Journal of Clinical Pyschopharmacology. Vol. 17, Pg. 325, 1997.
women TDLo oral 2200ug/kg (2.2mg/kg) VASCULAR: BP ELEVATION NOT CHARACTERIZED IN AUTONOMIC SECTION

CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION)		 Therapie. Vol. 52, Pg. 155, 1997.
women TDLo oral 648mg/kg/77W- (648mg/kg) BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY)

BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

BEHAVIORAL: ATAXIA		 Journal of Clinical Psychiatry. Vol. 59, Pg. 478, 1998.

Physical Properties

Physical Property Value Units Temp (deg C) Source
Melting Point 170 deg C   EXP
log P (octanol-water) 3.490 (none)   EST
Atmospheric OH Rate Constant 1.53E-10 cm3/molecule-sec 25 EST

Physical property data is provided to ChemIDplus by SRC, Inc.