1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. Ocaperidone

Ocaperidone  (Synonyms: R79598)

Cat. No.: HY-101094 Purity: 99.93%
COA Handling Instructions

Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.

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

Ocaperidone Chemical Structure

Ocaperidone Chemical Structure

CAS No. : 129029-23-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 52 In-stock
5 mg USD 110 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ocaperidone

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.

IC50 & Target

5-HT2 Receptor

0.14 nM (Ki)

a1-adrenergic receptor

0.46 nM (Ki)

D2 Receptor

0.75 nM (Ki)

Histamine H1

1.6 nM (Ki)

a2-adrenergic receptor

5.4 nM (Ki)

5-HT1A Receptor

7.6 (pEC50, h5-HT1A)

5-HT1A Receptor

8.08 (pKi, h5-HT1A)

In Vitro

Ocaperidone has high affinify at 5-HT2 and dopamine D2, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5HT2, a1-adrenergic, dopamine D2, histamine H1 and a2-adrenergic, respectively[1]. Ocaperidone shows 5-HT1A receptor agonist activity, with a pEC50 and pKi of 7.60 and 8.08[2].

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

In Vivo

Ocaperidone shows a potent occupation of 5HT2 receptor via in vivo binding in the frontal cortex of rats with an ED50 of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D2 receptor in the striatum and the nucleus accumbens[1]. Ocaperidone (R 79598) antagonizes dopamine D2 and 5-HT2, and shows a a partial generalization to buspirone with an ED50 of 0.163 mg/kg[3].

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

Molecular Weight

420.48

Formula

C24H25FN4O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(CCN2CCC(C3=NOC4=C3C=CC(F)=C4)CC2)=C(C)N=C5N1C=CC=C5C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (39.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3782 mL 11.8912 mL 23.7823 mL
5 mM 0.4756 mL 2.3782 mL 4.7565 mL
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.67 mg/mL (3.97 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[3]

The membranes are prepared from frozen HA7 cells. Cells are harvested in ice-cold Tris-HCl pH 7.4, homogenized and centrifuged at 40 000×g, 4°C for 10 min. The pellet is suspended in the same buffer and centrifuged again. After the second centrifugation, the pellet is suspended in an assay buffer consisting of pargyline (10 μM) and CaCl2 (4 mM) in Tris-HCl (50 mM, pH 7.4). Membrane protein, 0.031-0.084 mg/tube, is incubated with [3H] 8-OH-DPAT (1 nM final concentration) and Ocaperidone at seven concentrations, for 30 min, room temperature. The reaction is terminated by filtration through Whatman filters, and radioactivity is counted by liquid scintillation spectrometry. The experiments are performed in triplicate. Data are analyzed using the non-linear curve fitting program EBDA/LIGAND. Results expressed as pKi values are means of three determinations[3].

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

Animal Administration
[1]

Rats[1]
Male Wistar rats (200 g)
are treated subcutaneously with various dosages (0.01-10 or 2.5-40 mg/kg) of Ocaperidone dissolved in saline (injection of 1 mL of drug solution/100 g of body weight) or with saline (control); 1 hr thereafter the rats receive 1 μg/kg (5-10 μCi) [3H]spiperone by intravenous injection in the tail vein. The rats are sacrificed by decapitation 1 hr after the [3H]spiperone injection; the striatum, the nucleus accumbens, the tuberculum olfactorium, the frontal cortex, and the cerebellum are immediately dissected. The tissues are cooled on ice, weighed, and dissolved in 10 mL of Instagel II, in plastic counting vials. After 48 hr the radioactivity is counted; data are expressed in dpm, using external standard counting and referring to a quenched standard curve. The counted radioactivity is converted to pg of [3H]spiperone/mg of tissue. Four to six animals are treated at each drug dosage. For each drug and brain area, the values are averaged and graphically plotted versus the logarithm of the drug dosages. On each graph, values measured in the cerebellum are plotted; labeling in the cerebellum is taken as an indication of nonspecific tissue labeling[1].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3782 mL 11.8912 mL 23.7823 mL 59.4559 mL
5 mM 0.4756 mL 2.3782 mL 4.7565 mL 11.8912 mL
10 mM 0.2378 mL 1.1891 mL 2.3782 mL 5.9456 mL
15 mM 0.1585 mL 0.7927 mL 1.5855 mL 3.9637 mL
20 mM 0.1189 mL 0.5946 mL 1.1891 mL 2.9728 mL
25 mM 0.0951 mL 0.4756 mL 0.9513 mL 2.3782 mL
30 mM 0.0793 mL 0.3964 mL 0.7927 mL 1.9819 mL
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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.

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