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

Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics.

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Adoprazine Chemical Structure

Adoprazine Chemical Structure

CAS No. : 222551-17-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics[1].

IC50 & Target[1]

5-HT1A Receptor

9 (pEC50)

D2 Receptor

9.3 (pA2)

D3 Receptor

8.9 (pA2)

D4 Receptor

8.0 (pKi)

5-HT7 Receptor

7.2 (pKi)

5-HT1A Receptor

9.1 (pKi)

D2 Receptor

8.4 (pKi)

D3 Receptor

8.4 (pKi)

In Vitro

Adoprazine has high affinity at human recombinant D2, D3, D4, 5-HT2B, and 5-HT1A receptors, with pKis of 8.4, 8.4, 8.0, 7.9 and 9.1, respectively[1].
Adoprazine acts as a high potency dopamine D2 receptor antagonist and an efficacious serotonin 5-HT1A receptor agonist, with Emax value (% effect of 10 μM 5-HT) of 73 and pKB value of 8.5 [2].

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

In Vivo

Adoprazine (SLV313) (0.1-10 mg/kg; p.o.; single) is sufficient to reduce extracellular 5-HT and increase dopamine levels in the nucleus accumbens in a dose- and time-dependent manner[1].

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

Animal Model: Male Wistar rats (275-350 g) [1]
Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: p.o.; single
Result: Led to a dose- and time-dependent increase in extracellular levels of DA, DOPAC, and HVA. In contrast, led to a reduction in 5-HT levels and no change in 5-HIAA levels.
Clinical Trial
Molecular Weight

405.46

Formula

C24H24FN3O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1=CC=C(C2=CN=CC(CN3CCN(C4=C5OCCOC5=CC=C4)CC3)=C2)C=C1

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 : 50 mg/mL (123.32 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 2.4663 mL 12.3317 mL 24.6633 mL
5 mM 0.4933 mL 2.4663 mL 4.9327 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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    90% Corn Oil

    Solubility: ≥ 30 mg/mL (73.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 30 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (300.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

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

    Solubility: ≥ 3 mg/mL (7.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
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

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 2.4663 mL 12.3317 mL 24.6633 mL 61.6584 mL
5 mM 0.4933 mL 2.4663 mL 4.9327 mL 12.3317 mL
10 mM 0.2466 mL 1.2332 mL 2.4663 mL 6.1658 mL
15 mM 0.1644 mL 0.8221 mL 1.6442 mL 4.1106 mL
20 mM 0.1233 mL 0.6166 mL 1.2332 mL 3.0829 mL
25 mM 0.0987 mL 0.4933 mL 0.9865 mL 2.4663 mL
30 mM 0.0822 mL 0.4111 mL 0.8221 mL 2.0553 mL
40 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5415 mL
50 mM 0.0493 mL 0.2466 mL 0.4933 mL 1.2332 mL
60 mM 0.0411 mL 0.2055 mL 0.4111 mL 1.0276 mL
80 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
100 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6166 mL
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  • 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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Adoprazine
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