2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Pridopidine

Pridopidine  (Synonyms: ACR16; ASP2314; FR310826)

Cat. No.: HY-10684 Purity: 99.85%
COA Handling Instructions

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Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.

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

Pridopidine Chemical Structure

Pridopidine Chemical Structure

CAS No. : 346688-38-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 94 In-stock
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid
2 mg USD 45 In-stock
5 mg USD 85 In-stock
10 mg USD 160 In-stock
25 mg USD 320 In-stock
50 mg USD 500 In-stock
100 mg USD 780 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

Pridopidine Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.

IC50 & Target

D2 Receptor

 

In Vitro

Pridopidine, a dopamine (DA) stabilizer, Pridopidine may be a neuromodulatory agent with neuroprotective properties in Huntington disease (HD). To clarify the neuroprotective efficacy of Pridopidine and to explore the potential underling molecular mechanism, the ability of Pridopidine is evaluated to protect cells from apoptosis and to eventually activate pro-survival targets. Administration of Pridopidine (150 μM), the most effective dose, significantly reduces apoptosis in immortalized striatal knock-in cells expressing endogenous levels of mutant Htt (STHdh111/111) and markedly enhances phosphorylation state of prosurvival kinase ERK[2].

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

Pridopidine Related Antibodies
In Vivo

Pridopidine is known to act as a low affinity D2R antagonist. Pridopidine’s activity may be attributed to binding the sigma 1 receptor (S1R), an endoplasmic reticulum (ER). To strengthen the hypothesis that the BDNF pathway is upregulated due to activation of the S1R, SD rats are treated with lower doses of Pridopidine (range 0.3-60?mg/kg), and analysed the expression of seven selected genes in the BDNF pathway by qPCR. Pridopidine doses of 3 and 15?mg/kg in rats occupy 57±2% and 85±2% of S1R, respectively, and both do not show occupancy of the D2R, as determined by in vivo PET imaging. The significant occupancy proportion of the D2R (44-66%) is observed only at a dose of 60?mg/kg. This PET study supports the conclusion that the upregulation of genes in rats treated with 15?mg/kg Pridopidine are a result of specific activation of the S1R. At 30?mg/kg, partial/low occupancy of the D2R is at levels of 22-33% (assuming linearity), and S1R is saturated. Indeed, qPCR analysis reveals that the upregulation of EGR1 (already up at 3?mg/kg), EGR2, HOMER1A, KLF5, and ARC expression are upregulated at the low 15?mg/kg dose and expression of CDNK1A and CEBPB are significantly upregulated from a low dose of 30?mg/kg (CEBPB is significantly increased at 3?mg/kg but not at 15?mg/kg)[1]. To further confirm the beneficial effect of Pridopidine on HD motor phenotype and to elucidate whether Pridopidine may act also as neuroprotective agent, preclinical studies in R6/2 mice have been undertaken. Daily administration of Pridopidine at a dose of 5 mg/kg, the most effective dose with no adverse effects, starting at the pre-symptomatic stage at 5 weeks for 6 weeks, significantly preserves motor function and prevents the progressive and dramatic motor worsening commonly observed in R6/2 mice. The beneficial effects of Pridopidine are maintained for about 4 weeks, after which mice show a slight worsening in performing both the horizontal ladder task and the open field. In addition, according to a Kaplan-Meier survival curve analysis, Pridopidine efficiently extends lifespan in the same mice[2].

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

281.41

Formula

C15H23NO2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC(C2CCN(CCC)CC2)=CC=C1)(C)=O
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 : 100 mg/mL (355.35 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 3.5535 mL 17.7677 mL 35.5353 mL
5 mM 0.7107 mL 3.5535 mL 7.1071 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: ≥ 2.5 mg/mL (8.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (8.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

Purity: 99.85%

COA (245 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

Conditionally immortalized mouse striatal knock-in cells expressing endogenous levels of wild-type (STHdh7/7) or mHtt (STHdh111/111) are used. Different concentrations of Pridopidine (100, 150, 200 and 300 μM) are tested to investigate the anti-apoptotic effect of the molecule on immortalized cells cultured in serum-free medium at 39°C for six hours. In NE100 experiments, cells are pre-incubated with the compound (10 μM) for 2 hrs before culturing them in apoptotic conditions. At the end of each treatment, cells are collected and incubated with FITC-conjugated Annexin V. Fluorescence Activated Cell Sorting (FACS) analysis is performed[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Rats[1]
Sprague Dawley (SD) male rats (n=6 per group) are treated daily by oral gavage with Pridopidine at a dose of 60 mg/kg or vehicle (water) over the course of 10 days. On day 10, 90 min following last drug/water administration, brains are removed, and quickly rinsed with cold physiological saline. The striatum of the left hemisphere is gently extracted and immediately immerged in 1000 µL of RNAlater Solution in pre-labelled polypropylene vials and stored at 4°C overnight (to allow the solution to thoroughly penetrate the tissue), then moved to -20°C until analysis. RNA is isolated from the striatum of each rat and analysed[1].
Mice[2]
All in vivo experiments are conducted in R6/2 transgenic mice expressing exon 1 of human Htt with approximately 160±10 (CAG) repeats and manifesting first symptoms around week 7, and in wild-type (WT) littermates maintained on the B6CBA strain. Animals are housed singly and maintained under a 12-hr light/dark cycle environment in a clean facility and given free access to food pellets and water. Pridopidine is dissolved in saline (vehicle), and administered daily by intraperitoneal (i.p.) injection at a dose of 5 or 6 mg/kg per bodyweight during the light phase of the circadian rhythm. Control mice (WT and R6/2) are injected daily with the same volume of vehicle. All the mice are singly housed in home cage. Pridopidine (5 mg/kg) is administered to pre-symptomatic mice starting at week 5 to week 11 (6 week duration) and for symptomatic animals starting from week 7 to week 9 (3 weeks duration) and 1 week of daily administration (6 mg/kg) at week 10[2].

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 3.5535 mL 17.7677 mL 35.5353 mL 88.8383 mL
5 mM 0.7107 mL 3.5535 mL 7.1071 mL 17.7677 mL
10 mM 0.3554 mL 1.7768 mL 3.5535 mL 8.8838 mL
15 mM 0.2369 mL 1.1845 mL 2.3690 mL 5.9226 mL
20 mM 0.1777 mL 0.8884 mL 1.7768 mL 4.4419 mL
25 mM 0.1421 mL 0.7107 mL 1.4214 mL 3.5535 mL
30 mM 0.1185 mL 0.5923 mL 1.1845 mL 2.9613 mL
40 mM 0.0888 mL 0.4442 mL 0.8884 mL 2.2210 mL
50 mM 0.0711 mL 0.3554 mL 0.7107 mL 1.7768 mL
60 mM 0.0592 mL 0.2961 mL 0.5923 mL 1.4806 mL
80 mM 0.0444 mL 0.2221 mL 0.4442 mL 1.1105 mL
100 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8884 mL
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Pridopidine 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:

Pridopidine346688-38-8ACR16 ASP2314 FR310826ACR 16ACR-16ASP2314ASP 2314ASP-2314FR310826FR 310826FR-310826Dopamine ReceptorInhibitorinhibitorinhibit

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