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Submit ReviewPaliperidone
Description: 5-HT2A antagonist; also D2 antagonist; atypical antipsychotic
Alternative Names: 9-Hydroxyrisperidone,9-OH-risperidone
Chemical Name: 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
Purity: ≥98% (HPLC)
Biological Activity for Paliperidone
Paliperidone is an atypical antipsychotic; metabolite of risperidone (Cat. No. 2865). Exhibits high affinity for 5-HT2A receptors (Ki = 0.4 nM for cloned human 5-HT2A receptors). Also displays nanomolar affinity for human D2 receptors.
Technical Data for Paliperidone
| M. Wt | 426.48 |
| Formula | C23H27FN4O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 144598-75-4 |
| PubChem ID | 115237 |
| InChI Key | PMXMIIMHBWHSKN-UHFFFAOYSA-N |
| Smiles | FC1=CC2=C(C(C3CCN(CCC4=C(C)N=C(C(O)CCC5)N5C4=O)CC3)=NO2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Paliperidone
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.26 | 10 |
Preparing Stock Solutions for Paliperidone
The following data is based on the product molecular weight 426.48. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 23.45 mL | 117.24 mL | 234.48 mL |
| 0.5 mM | 4.69 mL | 23.45 mL | 46.9 mL |
| 1 mM | 2.34 mL | 11.72 mL | 23.45 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.69 mL |
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Product Datasheets for Paliperidone
References for Paliperidone
References are publications that support the biological activity of the product.
Schotte et al (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology 124 57 PMID: 8935801
Dremencov et al (2007) Distinct electrophysiological effects of paliper. and risper. on the firing activity of rat serotonin and NE neurons. Psychopharmacology 194 63 PMID: 17530476
Megens and Awouters et al (1994) In vivo pharmacological profile of 9-hydroxyrisperidone, the major metabolite of the novel antipsychotic risper. 33 399
Leysen et al (1994) Risperidone: a novel antipsychotic with balanced serotonin-DA antagonism, receptor occupancy profile, and pharmacologic activity. J.Clin.Psychiatry 55 5 PMID: 7520908
If you know of a relevant reference for Paliperidone, please let us know.
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Citations for Paliperidone
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.