PALIPERIDONE

Details

Stereochemistry	RACEMIC
Molecular Formula	C23H27FN4O3
Molecular Weight	426.4839
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=C(CCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)C(=O)N5CCCC(O)C5=N1

InChI

InChIKey=PMXMIIMHBWHSKN-UHFFFAOYSA-N

InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3

HIDE SMILES / InChI

Molecular Formula	C23H27FN4O3
Molecular Weight	426.4839
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021999s030lbl.pdf
Curator's Comment: description was created based on several sources, including http://dx.doi.org/10.4172/2161-1459.1000117

Paliperidone (9-OH-risperidone) is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. Very common adverse effects are: headache, tachycardia, somnolence and insomnia.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7520908	Antagonist 2760
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7542676	Antagonist 2760
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022264s006lbl.pdf \| https://www.ema.europa.eu/en/documents/assessment-report/xeplion-epar-public-assessment-report_en.pdf	Antagonist 2760
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL224 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022264s006lbl.pdf \| https://www.ema.europa.eu/en/documents/assessment-report/xeplion-epar-public-assessment-report_en.pdf	Antagonist 2760
HERG 91 Target ID: CHEMBL240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28265686	Blocker 534	0.57 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 295 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021999s030lbl.pdf	Primary		Approved 8360	INVEGA Approved Use INVEGA SUSTENNA® (paliperidone palmitate) is indicated for the treatment of: Schizophrenia [see Clinical Studies 14.1 Launch Date 1.16648641E12

C_max

Value	Dose	Co-administered	Analyte	Population
10.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26189570/	75 mg × eq single, intramuscular dose: 75 mg × eq route of administration: Intramuscular experiment type: SINGLE co-administered:		PALIPERIDONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20589922/	3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered:		PALIPERIDONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
22.214 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26189570/	75 mg × eq single, intramuscular dose: 75 mg × eq route of administration: Intramuscular experiment type: SINGLE co-administered:	PALIPERIDONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
410 ng × h/mL EXPERIMENT https://www.researchgate.net/profile/An_Vermeulen/publication/267692020_Population_Pharmacokinetics_of_Paliperidone_ER_in_Healthy_Subjects_and_Patients_With_Schizophrenia/links/5493e2b40cf22d7925da3fa6/Population-Pharmacokinetics-of-Paliperidone-ER-in-Healthy-Subjects-and-Patients-With-Schizophrenia.pdf	6 mg 1 times / day steady-state, oral dose: 6 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PALIPERIDONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
257.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20589922/	3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered:	PALIPERIDONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
44.9 day EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26189570/	75 mg × eq single, intramuscular dose: 75 mg × eq route of administration: Intramuscular experiment type: SINGLE co-administered:	PALIPERIDONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
22.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20589922/	3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered:	PALIPERIDONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
23 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021999s018lbl.pdf	single, oral	PALIPERIDONE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
26% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021999s018lbl.pdf	single, oral		PALIPERIDONE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
180 mg single, oral Overdose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24580061 Page: p.210	unhealthy, 12 n = 1 Health Status: unhealthy Condition: Developmental delay Age Group: 12 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/24580061 Page: p.210	Disc. AE: Lethargy, Tachycardia... AEs leading to discontinuation/dose reduction: Lethargy Tachycardia Hypokalemia Dyskinesia Dystonia Sources: https://pubmed.ncbi.nlm.nih.gov/24580061 Page: p.210
252 mg single, oral Overdose Dose: 252 mg Route: oral Route: single Dose: 252 mg Sources: https://pubmed.ncbi.nlm.nih.gov/31308582 Page: p.47	unhealthy, 16 n = 1 Health Status: unhealthy Condition: Conduct disorder Age Group: 16 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/31308582 Page: p.47	Disc. AE: Loss of consciousness... AEs leading to discontinuation/dose reduction: Loss of consciousness Sources: https://pubmed.ncbi.nlm.nih.gov/31308582 Page: p.47
15 mg 1 times / day multiple, oral Studied dose Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24556260	unhealthy, 30 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 30 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/24556260	DLT: Motor tic... Dose limiting toxicities: Motor tic Sources: https://pubmed.ncbi.nlm.nih.gov/24556260
234 mg 2 times / month multiple, intramuscular Recommended Dose: 234 mg, 2 times / month Route: intramuscular Route: multiple Dose: 234 mg, 2 times / month Sources: https://pubmed.ncbi.nlm.nih.gov/25938474 Page: p.565	unhealthy, 37.7 n = 226 Health Status: unhealthy Condition: Schizophrenia Age Group: 37.7 Sex: M+F Population Size: 226 Sources: https://pubmed.ncbi.nlm.nih.gov/25938474 Page: p.565	Disc. AE: Depressive symptom, Psychotic disorder... AEs leading to discontinuation/dose reduction: Depressive symptom (0.9%) Psychotic disorder (0.9%) Anxiety (0.4%) Insomnia (0.4%) Agitation (0.4%) Abnormal dreams (0.4%) Libido decreased (0.4%) Substance abuse (0.4%) Suicidal ideation (0.4%) Paranoid schizophrenia (0.4%) Akathisia (0.9%) Headache (0.9%) Dystonia (0.4%) Dizziness (0.4%) Tardive dyskinesia (0.4%) Dyskinesia (0.4%) Oromandibular dystonia (0.4%) Extrapyramidal disorder (0.4%) Erectile dysfunction (0.9%) Amenorrhea (0.4%) Ejaculation failure (0.4%) Galactorrhea (0.4%) Gynecomastia (0.4%) Injection site pain (0.9%) Chest discomfort (0.4%) Weight increased (0.9%) Semen volume decreased (0.4%) Sources: https://pubmed.ncbi.nlm.nih.gov/25938474 Page: p.565
9 mg 1 times / day multiple, oral Recommended Dose: 9 mg, 1 times / day Route: oral Route: multiple Dose: 9 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24580061 Page: p.210	unhealthy, 38 n = 1 Health Status: unhealthy Condition: Schizophrenia Age Group: 38 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/24580061 Page: p.210	Disc. AE: Dyskinesia, Dystonia... AEs leading to discontinuation/dose reduction: Dyskinesia Dystonia Tremor Diaphoresis Tachycardia Sources: https://pubmed.ncbi.nlm.nih.gov/24580061 Page: p.210
12 mg 1 times / day multiple, oral Recommended Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf Page: p.1	Disc. AE: Cerebrovascular disorder (NOS), Stroke... AEs leading to discontinuation/dose reduction: Cerebrovascular disorder (NOS) Stroke Transient ischemic attack (grade 3-5) Neuroleptic malignant syndrome QT interval prolonged Tardive dyskinesia Hyperglycemia Dyslipidemia Weight gain Hyperprolactinemia Intestinal stricture NOS Orthostatic hypotension Syncope Leukopenia Neutropenia Agranulocytosis Cognitive impairment Motor dysfunction NOS Seizures Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf Page: p.1
234 mg 2 times / month multiple, intramuscular Recommended Dose: 234 mg, 2 times / month Route: intramuscular Route: multiple Dose: 234 mg, 2 times / month Sources: https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: Schizophrenia\|Schizoaffective disorder Sources: https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf Page: p.1	Disc. AE: Cerebrovascular disorder (NOS), Stroke... AEs leading to discontinuation/dose reduction: Cerebrovascular disorder (NOS) Stroke Transient ischemic attack Neuroleptic malignant syndrome QT interval prolonged Tardive dyskinesia Hyperglycemia Dyslipidemia Weight gain Hyperprolactinemia Seizures Orthostatic hypotension Syncope Leukopenia Neutropenia Agranulocytosis Cognitive impairment Motor dysfunction NOS Sources: https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf Page: p.1

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709 inhibitor 1579	inhibitor 1752	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 CYP2A6 704 CYP2C8 901 CYP4A 19 CYP2E1 876 P-gp 1437	UGT1A1 418 UGT1A6 307 BCRP 555 P-gp 1527

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [IC50 61.9 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe detromethorphan Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP2A6 736	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >30 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe coumarin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP2E1 964	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >30 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe chlorzoxazone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP4A 33	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >30 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe lauric acid Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >60 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe Caffeine Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >60 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe phenytoin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >60 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe phenytoin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81	no [Inhibition >60 uM]	no (co-administration study) Comment: examination of inhibition by paliperidone using CYP isozyme probe testosterone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 41, 81
P-gp 1626	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/16936711/	weak [IC50 63.26 uM]

Drug as victim

Target	Modality	Activity
BCRP 555	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/30542502/	yes
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 40.0	yes
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part1.pdf Page: 40.0	yes
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_PharmR_Part1.pdf Page: 41, 67	yes
UGT1A1 418	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part3.pdf Page: 19.0	yes
UGT1A6 307	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_ClinPharmR_Part3.pdf Page: 19.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021999s000_PharmR_Part1.pdf Page: 8, 17, 24

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY10226	https://www.001chemical.com/chem/144598-75-4
3B Scientific (Wuhan) Corp	3B3-032531	http://www.3bsc.com/index/pro_info.php?id=53795
AA Blocks	AA001JQR	https://www.aablocks.com/goods/Goods/detail?id=AA001JQR
AHH Chemical co.,ltd	MT-01921	http://www.ahhchemical.com/product/MT-01921.html
AK Scientific, Inc. (AKSCI)	J10457	http://www.aksci.com/item_detail.php?cat=J10457
AK Scientific, Inc. (AKSCI)	S451	http://www.aksci.com/item_detail.php?cat=S451
Aaron Chemicals	AR001KIJ	http://www.aaronchem.com/144598-75-4
AbMole Bioscience	M5848	http://www.abmole.com/products/paliperidone.html
Acadechem	ACDC-030009	http://acadechemical.com/product/1779
Aceschem	ACF023126	https://www.aceschem.com/catalog/144598-75-4.html
Achemo Scientific Limited	AC-64208	http://www.achemo.com/search/?Keyword= 144598-75-4
Achemtek	0102-022120	http://www.achemtek.com/144598-75-4
Acorn PharmaTech	ACN-050765	http://www.acornpharmatech.com/
Acros Organics	AC456250010	https://www.fishersci.com/shop/products/9-hydroxyrisperidone-98-acros-organics/AC456250010
Active Biopharma	ABP000395	http://www.activebiopharma.com/144598-75-4
Alfa Chemistry	AP1020719554	https://reagents.alfa-chemistry.com/product/9-hydroxyrisperidone-d4-solution-cas-1020719-55-4-756.html
Alsachim	1560	http://www.alsachim.com/product-C2633-glo.bal-view.html
Ambinter	Amb19132718	http://www.ambinter.com/reference/19132718
Angel Pharmatech	AG-11540	http://www.angelpharmatech.com/144598-75-4.html
Angene	AGN-PC-04XSV9	http://www.angenechemical.com/productshow/AGN-PC-04XSV9.html
Anward	ANW-42875	http://www.anward.com/pro_result/28250
Ark Pharm	AK-77508	http://www.arkpharminc.com/products/144598-75-4.html
Aurora Fine Chemicals LLC	A13.105.665	http://online.aurorafinechemicals.com/info?ID=A13.105.665
Aurum Pharmatech LLC	Q-4343	http://www.Aurumpharmatech.com/Product/ProductDetails/Q_4343
AvaChem Scientific	2244	http://www.avachem.com/productSearch.asp?2244
BLD Pharm	BD111798	http://www.bldpharm.com/products/144598-75-4.html
BOC Sciences	130049-85-3	https://www.bocsci.com/r-9-hydroxy-risperidone-r-paliperidone-cas-130049-85-3-item-262137.html
BOC Sciences	147663-01-2	https://www.bocsci.com/s-9-hydroxy-risperidone-s-paliperidone-cas-147663-01-2-item-262138.html
BioChemPartner	BCP02338	http://www.biochempartner.com/144598-75-4-BCP02338
BioCrick	BCC3834	http://www.biocrick.com/Paliperidone-BCC3834.html
BioSynth	Q-101425	https://www.biosynth.com/en/products/life-science/other-biochemicals/products/Q-101425.html
Boerchem	BC228519	http://www.boerchem.com/?product_38518.html
Boerchem	BC677689	http://www.boerchem.com/?product_42087.html
CSNpharm	CSN10189	https://www.csnpharm.com/products/paliperidone.html
Chem Scene	CS-0386	http://www.chemscene.com/144598-75-4.html
ChemMol	30108656	http://www.chemmol.com/chemmol/30108656.html
ChemMol	44008670	http://www.chemmol.com/chemmol/44008670.html
ChemMol	44009994	http://www.chemmol.com/chemmol/44009994.html
ChemMol	49400035	http://www.chemmol.com/chemmol/49400035.html
ChemMol	81412039	http://www.chemmol.com/chemmol/81412039.html
Chemenu	CM110058	http://www.chemenu.com/products/CM110058
Chemspace	CSSB00000693926	https://chem-space.com/CSSB00000693926
Clearsynth	CS-EB-01587	https://www.clearsynth.com/en/CSEB01587.html
Clearsynth	CS-ER-01579	https://www.clearsynth.com/en/CSER01579.html
Clearsynth	CS-O-02070	https://www.clearsynth.com/en/CSO02070.html
Combi-Blocks	OR-2275	http://www.combi-blocks.com/cgi-bin/find.cgi?OR-2275
Coresyn	CM14424	http://www.coresyn.com/Cas144598-75-4.html
DAOGE BIOPHARMA	DG21-12007	https://www.daogechem.com/product/144598-75-4.html
Finetech	FT-0670101	http://www.finetechnology-ind.com/prod/detail/pub/1020719-55-4.html
Finetech	FT-0670102	http://www.finetechnology-ind.com/prod/detail/pub/130049-85-3.html
Finetech	FT-0600425	http://www.finetechnology-ind.com/prod/detail/pub/144598-75-4.html
Fluoropharm	YF10040	http://www.fluoropharm.com/product/YF10040.html
Glentham Life Sciences	GP3914	http://www.glentham.com/products/product/GP3914/
Hello Bio	HB1798	https://www.hellobio.com/paliperidone.html
LGC Standards	LGCAMP0491.03-01	https://www.lgcstandards.com/US/en/p/LGCAMP0491.03-01
LGC Standards	LGCFOR0491.03	https://www.lgcstandards.com/US/en/p/LGCFOR0491.03
LGC Standards	MM0491.03	https://www.lgcstandards.com/US/en/p/MM0491.03
Lab Network	LN00188652	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00188652
Matrix Scientific	125342	https://www.matrixscientific.com/125342.html
MedChem Express	HY-A0019	https://www.medchemexpress.com/Paliperidone.html
MolPort	MolPort-020-313-413	https://www.molport.com/shop/molecule-link/MolPort-020-313-413
Molcore	MC10226	https://www.molcore.com/product/144598-75-4
MuseChem	A000313	https://www.musechem.com/product/A000313.html
OChem	22777	http://www.ocheminc.com/index.php?act=psearch&pid=598P754
Renno Tech	RL01805	http://www.rennotech.com/product_show.asp?id=2054
Shanghai Send Pharmaceutical Technology Co., Ltd	send21033	http://shsendpharm.com/
Sigma-Aldrich	H-076_CERILLIAN	https://www.sigmaaldrich.com/catalog/product/cerillian/h076?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	P0099_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/p0099?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	1491809_USP	https://www.sigmaaldrich.com/catalog/product/usp/1491809?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S538546	http://www.smolecule.com/products/s538546
Synblock Inc	PB27526	http://www.synblock.com/product/144598-75-4.html
TCI (Tokyo Chemical Industry)	P1897	http://www.tcichemicals.com/eshop/en/us/commodity/P1897/index.html
THE BioTek	bt-278646	https://www.thebiotek.com/product/inhibitors/bt-278646
THE BioTek	bt-318627	https://www.thebiotek.com/product/others/bt-318627
Tocris	4493	https://www.tocris.com/products/paliperidone_4493
VladaChem	VL281908-10MG	https://www.vladachem.com/product.php?products=144598-75-4
Yuhao Chemical	M0403394	http://www.chemyuhao.com/144598-75-4.html
abcr GmbH	AB457979	http://www.abcr.com/shop/en/AB457979
eNovation Chemicals	D522284	http://www.enovationchem.com/productDetails.asp?productID=D522284
iChemical	EBD54215	http://www.ichemical.com/products/144598-75-4.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
mcule	MCULE-5597043685	https://mcule.com/MCULE-5597043685/

PubMed

Title	Date	PubMed
Possible relationship between combined plasma concentrations of risperidone plus 9-hydroxyrisperidone and extrapyramidal symptoms. Preliminary study.	2001	11586052
Effects of two atypical neuroleptics, olanzapine and risperidone, on the function of the urinary bladder and the external urethral sphincter in anesthetized rats.	2001	11580866
Long-term treatment of chronic schizophrenia with risperidone: a study with plasma levels.	2001 Feb	11246293
Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia.	2001 Jan 1	11205425
Plasma concentrations of risperidone and 9-hydroxyrisperidone during combined treatment with paroxetine.	2001 Jun	11360029
Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes.	2001 Oct	11560868
The effect of fluoxetine on the pharmacokinetics and safety of risperidone in psychotic patients.	2002 Mar	11985287
Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel.	2002 May	11961040
Relationship between risperidone and 9-hydroxy-risperidone plasma concentrations and CYP2D6 enzyme activity in psychiatric patients.	2002 Nov	12518271
Sequential changes in the plasma concentration of risperidone following intentional overdose.	2002 Nov-Dec	12469003
Prediction and assessment of extrapyramidal side effects induced by risperidone based on dopamine D(2) receptor occupancy.	2002 Oct	12211096
Risperidone and 9-hydroxyrisperidone concentrations are not dependent on age or creatinine clearance among elderly subjects.	2002 Summer	12083597
Effects of CYP2D6 genotypes on plasma concentrations of risperidone and enantiomers of 9-hydroxyrisperidone in Japanese patients with schizophrenia.	2003 Feb	12616663
Pharmacokinetic comparison of fast-disintegrating and conventional tablet formulations of risperidone in healthy volunteers.	2003 Jun	12860492
Correlation between scores on Continuous Performance Test and plasma concentration for schizophrenic patients on risperidone.	2004 Apr	15009822
In vitro effects of risperidone and 9-hydroxy-risperidone on human platelet function, plasma coagulation, and fibrinolysis.	2004 Aug	15476907
Plasma risperidone concentrations during combined treatment with sertraline.	2004 Aug	15257068
Effects of various factors on steady-state plasma concentrations of risperidone and 9-hydroxyrisperidone: lack of impact of MDR-1 genotypes.	2004 May	15089809
Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition.	2005 Jul	16003291
Cytochrome P450 3A inhibitor itraconazole affects plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients.	2005 Nov	16321618
Pharmacokinetic profile of long-acting injectable risperidone at steady-state: comparison with oral administration.	2005 Sep-Oct	16598965
Serum concentrations of risperidone and 9-OH risperidone following intramuscular injection of long-acting risperidone compared with oral risperidone medication.	2006 Jul	16774657
Positive modulation of glutamatergic receptors potentiates the suppressive effects of antipsychotics on conditioned avoidance responding in rats.	2006 Jun	16782180
A PET study evaluating dopamine D2 receptor occupancy for long-acting injectable risperidone.	2006 Mar	16513859
Multiple dose pharmacokinetics of risperidone and 9-hydroxyrisperidone in Chinese female patients with schizophrenia.	2006 Mar	16490177
Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein.	2006 Sep	16810505
Forty years of antipsychotic Drug research--from haloperidol to paliperidone--with Dr. Paul Janssen.	2007	18074755
Paliperidone extended release.	2007	17447829
Paliperidone: quo vadis?	2007 Apr	17343660
Efficacy and safety of paliperidone extended-release tablets: results of a 6-week, randomized, placebo-controlled study.	2007 Dec 15	17601495
Rapidly disintegrating risperidone in subjects with schizophrenia or schizoaffective disorder: a summary of ten phase I clinical trials assessing taste, tablet disintegration time, bioequivalence, and tolerability.	2007 Feb	17472821
Treatment of schizophrenia with paliperidone extended-release tablets: a 6-week placebo-controlled trial.	2007 Feb	17092691
Maintenance therapy with once-monthly administration of long-acting injectable risperidone in patients with schizophrenia or schizoaffective disorder: a pilot study of an extended dosing interval.	2007 Jan 29	17261186
Paliperidone (Invega) for schizophrenia.	2007 Mar 12	17351558
Effect of topiramate on plasma concentrations of clozapine, olanzapine, risperidone, and quetiapine in patients with psychotic disorders.	2007 Mar-Apr	17414943
A double-blind, placebo-controlled, randomized study evaluating the effect of paliperidone extended-release tablets on sleep architecture in patients with schizophrenia.	2007 Sep	17690599
Upcoming agents for the treatment of schizophrenia: mechanism of action, efficacy and tolerability.	2008	18973393
New drug update: 2007.	2008 Apr	18454587
Paliperidone extended-release tablets for the acute and maintenance treatment of schizophrenia.	2008 Feb	18343262
Paliperidone-ER: first atypical antipsychotic with oral extended release formulation.	2008 Feb	18271706
Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone.	2008 Jan	18094221
Validated LC-MS/MS methods for the determination of risperidone and the enantiomers of 9-hydroxyrisperidone in human plasma and urine.	2008 Jul 1	18571483
Gateways to clinical trials. July-August 2008.	2008 Jul-Aug	18850047
Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions.	2008 Jun	18537577
Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week, placebo-controlled studies.	2008 May	18466043
Paliperidone for treatment of schizophrenia.	2008 May	18375569
Efficacy and safety of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 52-week open-label studies.	2008 Nov	18854723
Antipsychotic drugs inhibit the function of breast cancer resistance protein.	2008 Oct	18834354
ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety.	2008 Oct	18708991
Effects of quetiapine, risperidone, 9-hydroxyrisperidone and ziprasidone on the survival of human neuronal and immune cells in vitro.	2010 Mar	18755815

Patents

Sample Use Guides

In Vivo Use Guide

In adults is 6 mg administered once daily In adolescents 12-17 years of age is 3 mg administered once daily

Route of Administration: Oral

In Vitro Use Guide

Paliperidone has dual hyperprolactinemic actions in lactotrophs i) by preserving the coupling of spontaneous electrical activity and prolactin secretion in the presence of dopamine and ii) by inhibiting intrinsic dopamine receptor activity in the absence of dopamine, leading to enhanced calcium signaling and secretion.

Substance Class	Chemical Created by `admin` on `Wed Jul 05 23:44:28 UTC 2023` Edited by `admin` on `Wed Jul 05 23:44:28 UTC 2023`
Record UNII	838F01T721
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PALIPERIDONE

Official Name

English

PALIPERIDONE [USAN]

Common Name

English

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-9-HYDROXY-2-METHYL-

Systematic Name

English

3-(2-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE

Systematic Name

English

PALIPERIDONE [USP MONOGRAPH]

Common Name

English

PALIPERIDONE [MART.]

Common Name

English

PALIPERIDONE [EMA EPAR]

Common Name

English

RISPERIDONE IMPURITY C [EP IMPURITY]

Common Name

English

9-HYDROXYRISPERIDONE

Common Name

English

RO76477

Code

English

paliperidone [INN]

Common Name

English

PALIPERIDONE [VANDF]

Common Name

English

(9RS)-3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one

Common Name

English

NSC-759623

Code

English

PALIPERIDONE [ORANGE BOOK]

Common Name

English

RISPERIDONE IMPURITY, 9-HYDROXYRISPERIDONE- [USP IMPURITY]

Common Name

English

PALIPERIDONE [USP-RS]

Common Name

English

PALIPERIDONE [MI]

Common Name

English

Paliperidone [WHO-DD]

Common Name

English

R-76477

Code

English

RO-76477

Code

English

PALIPERIDONE [JAN]

Common Name

English

INVEGA

Brand Name

English

Classification Tree Code System Code

WHO-ATC

N05AX13