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MedKoo Cat#: 318451 | Name: Paliperidone
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

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

Theoretical Analysis

MedKoo Cat#: 318451

Name: Paliperidone

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

Chemical Formula: C23H27FN4O3

Exact Mass: 426.2067

Molecular Weight: 426.49

Elemental Analysis: C, 64.77; H, 6.38; F, 4.45; N, 13.14; O, 11.25

Price and Availability

Size Price Availability Quantity
100mg USD 250.00 2 weeks
200mg USD 400.00 2 weeks
500mg USD 750.00 2 weeks
1g USD 1,150.00 2 weeks
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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
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).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Paliperidone (9-Hydroxyrisperidone) is a dopamine D2 antagonist and 5-HT2A antagonist.
In vitro activity:
In the present study, this study used mouse embryonic prefrontal cortical neurons to examine the neuroprotection of paliperidone against the neuronal damage induced by exposure to the NMDA receptor antagonist, MK-801. Paliperidone inhibited MK-801 induced neurotoxicity both in MTT metabolism assay (p<0.01) and in lactate dehydrogenase (LDH) activity assay (p<0.01). Time course studies revealed that paliperidone effectively attenuated the elevation of intracellular free calcium concentration ([Ca(2+)]i) induced by exposure to MK-801 (p<0.01). Reference: Schizophr Res. 2013 Jun;147(1):14-23. https://pubmed.ncbi.nlm.nih.gov/23583326/
In vivo activity:
The data showed that MK-801 caused stereotyped behavior in mice and induced synaptic damage and dendritic spine impairment compared with the control, whereas paliperidone ameliorated these changes. Moreover, paliperidone reversed MK-801-induced decreases in PP2A and PTEN levels in prefrontal cortical neurons. Furthermore, in primary cultured cortical neurons and HT-22 cells, paliperidone inhibited cell apoptosis caused by MK-801. Reference: J Affect Disord. 2022 Nov 15;317:265-277. https://pubmed.ncbi.nlm.nih.gov/36031001/
Solvent mg/mL mM comments
Solubility
DMSO 4.8 11.15
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 426.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Peng L, Zhu D, Feng X, Dong H, Yue Q, Zhang J, Gao Q, Hao J, Zhang X, Liu Z, Sun J. Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3β signaling pathway. Schizophr Res. 2013 Jun;147(1):14-23. doi: 10.1016/j.schres.2013.03.006. Epub 2013 Apr 9. PMID: 23583326. 2. Yang MC, Lung FW. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl). 2011 Oct;217(3):397-410. doi: 10.1007/s00213-011-2291-7. Epub 2011 Apr 27. PMID: 21523348. 3. Wang J, Li M, Zhang J, Gao Q, Ding Z, Sun J. Paliperidone alleviates MK-801-induced damage to prefrontal cortical neurons via the PP2A/PTEN pathway. J Affect Disord. 2022 Nov 15;317:265-277. doi: 10.1016/j.jad.2022.08.071. Epub 2022 Aug 27. PMID: 36031001. 4. Schwartzer JJ, Morrison RL, Ricci LA, Melloni RH Jr. Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression. Psychopharmacology (Berl). 2009 May;203(4):653-63. doi: 10.1007/s00213-008-1412-4. Epub 2008 Dec 6. PMID: 19066856.
In vitro protocol:
1. Peng L, Zhu D, Feng X, Dong H, Yue Q, Zhang J, Gao Q, Hao J, Zhang X, Liu Z, Sun J. Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3β signaling pathway. Schizophr Res. 2013 Jun;147(1):14-23. doi: 10.1016/j.schres.2013.03.006. Epub 2013 Apr 9. PMID: 23583326. 2. Yang MC, Lung FW. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl). 2011 Oct;217(3):397-410. doi: 10.1007/s00213-011-2291-7. Epub 2011 Apr 27. PMID: 21523348.
In vivo protocol:
1. Wang J, Li M, Zhang J, Gao Q, Ding Z, Sun J. Paliperidone alleviates MK-801-induced damage to prefrontal cortical neurons via the PP2A/PTEN pathway. J Affect Disord. 2022 Nov 15;317:265-277. doi: 10.1016/j.jad.2022.08.071. Epub 2022 Aug 27. PMID: 36031001. 2. Schwartzer JJ, Morrison RL, Ricci LA, Melloni RH Jr. Paliperidone suppresses the development of the aggressive phenotype in a developmentally sensitive animal model of escalated aggression. Psychopharmacology (Berl). 2009 May;203(4):653-63. doi: 10.1007/s00213-008-1412-4. Epub 2008 Dec 6. PMID: 19066856.
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.

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