2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor
  4. Paliperidone palmitate

Paliperidone palmitate  (Synonyms: 9-Hydroxyrisperidone palmitate)

Cat. No.: HY-A0019A Purity: 98.41%
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Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia.

For research use only. We do not sell to patients.

Paliperidone palmitate Chemical Structure

Paliperidone palmitate Chemical Structure

CAS No. : 199739-10-1

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Based on 1 publication(s) in Google Scholar

Paliperidone palmitate Related Antibodies

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Description

Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia[1][2][3].

IC50 & Target[1]

D2 Receptor

 

5-HT2A Receptor

 

In Vivo

Co-administration of paliperidone palmitate (62.4 mg/kg in mice and 20 mg/kg in rats; intramuscular injection; single dose) with hyaluronidase (HY-172442) altered the depot release of paliperidone palmitate in the first 4 days after injection and increased plasma exposure in both BALB/c mice and Sprague Dawley rat models, but did not affect the long-acting release characteristics of paliperidone palmitate. In mice, hyaluronidase altered the tissue morphology at the injection site, resulting in infiltration of macrophages between myocytes, and in rats, granulomas with central cavities and necrosis formed at the injection site[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (female, about 20 g, 6-8 weeks old)+Sprague Dawley rats (male, about 250 g, 6-8 weeks old)[2]
Dosage: Mice: 62.4 mg/kg of Paliperidone palmitate, 5 U or 15 U of hyaluronidase (dissolved in normal saline)
Rats: 20 mg/kg of Paliperidone palmitate, 5 U or 15 U of Hyaluronidase (dissolved in phosphate buffered saline)
Administration: Intramuscular injection, single dose; for mice, 4-week study period; for rats, 21-28-day study period
Result: In mice, co-administration of hyaluronidase increased paliperidone plasma exposures in the first week after injection. The overall long-acting release nature of the formulation was maintained. Macrophages showed infiltration between individual myocytes when paliperidone palmitate was co-administered with hyaluronidase.
In rats, co-administration of hyaluronidase also increased exposure in the first 4 days, but the effect was less than that in mice. The long-acting exposure was still maintained for about 20 days. Co-administration of hyaluronidase did not discernably affect the granulomas or the surrounding myocytes in rats. The lymph node retention of paliperidone palmitate was diminished upon treatment with hyaluronidase in both mice and rats. The biphasic plasma concentration-time profiles of paliperidone in both species could be described by an open first-order disposition model with parallel fast and slow absorption processes.
The macrophage infiltration and angiogenesis at the injection site affected the drug release and absorption, and the effect of hyaluronidase on these processes was different between mice and rats.
Clinical Trial
Molecular Weight

664.89

Formula

C39H57FN4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC1CCCN(C1=NC(C)=C2CCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)C2=O)CCCCCCCCCCCCCCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

Ethanol : 2 mg/mL (3.01 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5040 mL 7.5200 mL 15.0401 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 98.41%

SDS (392 KB)

COA (245 KB) HNMR (295 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 1.5040 mL 7.5200 mL 15.0401 mL 37.6002 mL
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Paliperidone palmitate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Paliperidone199739-10-19-HydroxyrisperidoneDopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantipsychoticesterprodrugschizophreniaatypicallong-actingInhibitorinhibitorinhibit

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