Paliperidone
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MedKoo CAT#: 318451

CAS#: 144598-75-4 (free base)

Description: Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class of medications. It is developed by Janssen Pharmaceutica. Invega is an extended release formulation of paliperidone that uses the OROS extended release system to allow for once-daily dosing.Paliperidone has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors. It does not bind to muscarinic acetylcholine receptors. In addition, it binds with dopamine and serotonin receptors.


Price and Availability

Size
Price

50mg
USD 250
500mg
USD 1050
Size
Price

100mg
USD 450
1g
USD 1650
Size
Price

200mg
USD 650
2g
USD 2450

Paliperidone, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 318451
Name: Paliperidone
CAS#: 144598-75-4 (free base)
Chemical Formula: C23H27FN4O3
Exact Mass: 426.20672
Molecular Weight: 426.48
Elemental Analysis: C, 64.77; H, 6.38; F, 4.45; N, 13.14; O, 11.25


Related CAS #: 144598-75-4 (free base)   199739-10-1 (palmitate)  

Synonym: Paliperidone; 9-Hydroxyrisperidone; Invega; 9-OH-risperidone; Invega Sustenna; Invega Sustenna; paliperidone;

IUPAC/Chemical Name: 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

InChi Key: PMXMIIMHBWHSKN-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: MacDowell KS, Sayd A, García-Bueno B, Caso JR, Madrigal JL, Leza JC. Effects
of the antipsychotic paliperidone on stress-induced changes in the
endocannabinoid system in rat prefrontal cortex. World J Biol Psychiatry. 2016
Mar 18:1-14. [Epub ahead of print] PubMed PMID: 26987678.

2: Tsai MC, Chang PT, Yang CH, Liu ME. The Delirium Related to Oral Paliperidone
in Dementia: A Case Report. J Clin Psychopharmacol. 2016 Apr;36(2):184-5. doi:
10.1097/JCP.0000000000000472. PubMed PMID: 26872118.

3: Xiao Y, Muser E, Fu DJ, Lafeuille MH, Pilon D, Emond B, Wu A, Duh MS, Lefebvre
P. Comparison of Medicaid spending in schizoaffective patients treated with once
monthly paliperidone palmitate or oral atypical antipsychotics. Curr Med Res
Opin. 2016 Apr;32(4):759-769. Epub 2016 Feb 2. PubMed PMID: 26750639.

4: Yang CH, Juang KD, Chou PH, Chan CH. A Case Report of Probable Paliperidone
ER-Induced Serotonin Syndrome in a 17-Year-Old Taiwanese Female With New Onset
Psychosis. Medicine (Baltimore). 2016 Mar;95(9):e2930. doi:
10.1097/MD.0000000000002930. PubMed PMID: 26945397.

5: Alphs L, Fu DJ, Turkoz I. Paliperidone for the Treatment of Schizoaffective
Disorder. Expert Opin Pharmacother. 2016 Mar 2. [Epub ahead of print] PubMed
PMID: 26934062.

6: Qiao Y, Yang F, Li C, Guo Q, Wen H, Zhu S, Ouyang Q, Shen W, Sheng J. Add-on
effects of a low-dose aripiprazole in resolving hyperprolactinemia induced by
risperidone or paliperidone. Psychiatry Res. 2016 Mar 30;237:83-9. doi:
10.1016/j.psychres.2015.12.033. Epub 2015 Dec 28. PubMed PMID: 26921057.

7: Druais S, Doutriaux A, Cognet M, Godet A, Lançon C, Levy P, Samalin L, Guillon
P. Cost Effectiveness of Paliperidone Long-Acting Injectable Versus Other
Antipsychotics for the Maintenance Treatment of Schizophrenia in France.
Pharmacoeconomics. 2016 Apr;34(4):363-91. doi: 10.1007/s40273-015-0348-x. PubMed
PMID: 26883132.

8: Fu DJ, Turkoz I, Bossie CA, Patel H, Alphs L. Rapid onset of treatment effects
on psychosis, depression, and mania in patients with acute exacerbation of
schizoaffective disorder following treatment with oral extended-release
paliperidone. J Affect Disord. 2016 Mar 15;193:381-90. doi:
10.1016/j.jad.2015.12.060. Epub 2015 Dec 31. PubMed PMID: 26802315.

9: Kim MK, Kim B, Lee KS, Kim CM, Bang SY, Choi TK, Lee SH. White-matter
connectivity related to paliperidone treatment response in patients with
schizophrenia. J Psychopharmacol. 2016 Mar;30(3):294-302. doi:
10.1177/0269881115625114. Epub 2016 Jan 11. PubMed PMID: 26755544.

10: Ravenstijn P, Remmerie B, Savitz A, Samtani MN, Nuamah I, Chang CT, De
Meulder M, Hough D, Gopal S. Pharmacokinetics, safety, and tolerability of
paliperidone palmitate 3-month formulation in patients with schizophrenia: A
phase-1, single-dose, randomized, open-label study. J Clin Pharmacol. 2016
Mar;56(3):330-9. doi: 10.1002/jcph.597. Epub 2015 Oct 5. PubMed PMID: 26189570.

11: Cordiner M, Shajahan P, McAvoy S, Bashir M, Taylor M. Effectiveness of
long-acting antipsychotics in clinical practice : 1. A retrospective, 18-month
follow up and comparison between paliperidone palmitate, risperidone long-acting
injection and zuclopenthixol decanoate. Ther Adv Psychopharmacol. 2016
Feb;6(1):22-32. doi: 10.1177/2045125315623168. PubMed PMID: 26913175; PubMed
Central PMCID: PMC4749742.

12: Karslıoǧlu EH, Özalp E, Çayköylü A. Paliperidone Palmitate-induced Urinary
Incontinence: A Case Report. Clin Psychopharmacol Neurosci. 2016 Feb
29;14(1):96-100. doi: 10.9758/cpn.2016.14.1.96. PubMed PMID: 26792046; PubMed
Central PMCID: PMC4730936.

13: Struye A, Depuydt C, Abdel Sater E, Dubois V. Toxic Epidermal Necrolysis
Related to Paliperidone Palmitate: First Case Report. J Clin Psychopharmacol.
2016 Feb 26. [Epub ahead of print] PubMed PMID: 26928057.

14: Savitz AJ, Xu H, Gopal S, Nuamah I, Ravenstijn P, Janik A, Schotte A, Hough
D, Fleischhacker WW. Efficacy and Safety of Paliperidone Palmitate 3-Month
Formulation for Patients with Schizophrenia: A Randomized, Multicenter,
Double-Blind, Noninferiority Study. Int J Neuropsychopharmacol. 2016 Feb 22. pii:
pyw018. doi: 10.1093/ijnp/pyw018. [Epub ahead of print] PubMed PMID: 26902950.

15: Gomeni R, Bressolle F, Fava M. Response Surface Analysis and Non-Linear
Optimization Algorithm For Maximization of Clinical Drug Performance: Application
to Extended Release and Long-Acting-Injectable Paliperidone. J Clin Pharmacol.
2016 Feb 22. doi: 10.1002/jcph.724. [Epub ahead of print] PubMed PMID: 26899406.

16: Alphs L, Mao L, Lynn Starr H, Benson C. A pragmatic analysis comparing
once-monthly paliperidone palmitate versus daily oral antipsychotic treatment in
patients with schizophrenia. Schizophr Res. 2016 Feb;170(2-3):259-64. doi:
10.1016/j.schres.2015.12.012. Epub 2015 Dec 29. PubMed PMID: 26742509.

17: Darville N, van Heerden M, Erkens T, De Jonghe S, Vynckier A, De Meulder M,
Vermeulen A, Sterkens P, Annaert P, Van den Mooter G. Modeling the Time Course of
the Tissue Responses to Intramuscular Long-acting Paliperidone Palmitate
Nano-/Microcrystals and Polystyrene Microspheres in the Rat. Toxicol Pathol. 2016
Feb;44(2):189-210. doi: 10.1177/0192623315618291. Epub 2015 Dec 23. PubMed PMID:
26698322.

18: Lisbeth P, Vincent H, Kristof M, Bernard S, Manuel M, Hugo N. Genotype and
co-medication dependent CYP2D6 metabolic activity: effects on serum
concentrations of aripiprazole, haloperidol, risperidone, paliperidone and
zuclopenthixol. Eur J Clin Pharmacol. 2016 Feb;72(2):175-84. doi:
10.1007/s00228-015-1965-1. Epub 2015 Oct 30. PubMed PMID: 26514968.

19: Chue P, Chue J. A critical appraisal of paliperidone long-acting injection in
the treatment of schizoaffective disorder. Ther Clin Risk Manag. 2016 Jan
27;12:109-16. doi: 10.2147/TCRM.S81581. eCollection 2016. Review. PubMed PMID:
26869795; PubMed Central PMCID: PMC4737499.

20: Koshikawa Y, Takekita Y, Kato M, Sakai S, Onohara A, Sunada N, Nishida K,
Yoshimura M, Fabbri C, Serretti A, Kinoshita T. The Comparative Effects of
Risperidone Long-Acting Injection and Paliperidone Palmitate on Social
Functioning in Schizophrenia: A 6-Month, Open-Label, Randomized Controlled Pilot
Trial. Neuropsychobiology. 2016;73(1):35-42. doi: 10.1159/000442209. Epub 2016
Jan 27. PubMed PMID: 26812618.