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

Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.

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Azaperone

Azaperone 화학구조

CAS No. : 1649-18-9

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
500 mg 해외재고보유
1 g   견적 받기  
5 g   견적 받기  

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent[1][2][3].

In Vivo

Azaperone (0.4-0.8 mg/kg; i.m.; single administration) induces dose-dependent sedation in healthy Welsh mountain ponies; the 0.8 mg/kg dose causes a sustained 30%-38% reduction in mean arterial pressure, which persists for at least 4 h, accompanied by decreased peripheral resistance, transient tachycardia, and reduced packed red blood cell volume and hemoglobin concentration[1].
Co-administration of Azaperone (0.03-0.0375 mg/kg; i.m.) with Etorphine reduces the median induction time of white rhinoceroses to 6.25 min while maintaining a median immobilization quality score of 2[2].
Azaperone (2-4 mg/kg; i.m., intranasal administration; single dose) exerts sedative effects on healthy weaned piglets[3].

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

Animal Model: Welsh Mountain ponies (either sex, 3-5 years old, 202-300 kg)[1]
Dosage: 0.4 mg/kg; 0.8 mg/kg
Administration: i.m.; single dose
Result: Produced a moderate blood pressure-lowering effect that lasts for at least 4 hours, with an average systolic blood pressure reduction of 30-38% at 0.8 mg/kg.
Animal Model: Ceratotherium simum (male, 5-6 years old, 1000-1500 kg)[2]
Dosage: 0.03 mg/kg (for 1000-1250 kg rhinoceros); 0.0375 mg/kg (for 1250-1500 kg rhinoceros)
Administration: i.m.; single dose
Result: Reduced median induction time to 6.25 minutes (range 5.35-6.9 minutes), a ~30% reduction compared to etorphine alone.
Maintained median immobilization quality score at 2 (range 2-3), identical to etorphine alone.
Animal Model: gilts (weaned, ~28 days old, mean body weight 8.10-8.80 kg)[3]
Dosage: 2 mg/kg (i.m.); 2 mg/kg (intranasal); 4 mg/kg (intranasal)
Administration: i.m.; single dose; intranasal; single dose via LMA MAD Nasal applicator
Result: To achieve a sedative level comparable to that of standard intramuscular injection (2 mg/kg), a dose of 4 mg/kg via nasal administration is required.
Nasal administration of 2 mg/kg took longer to take effect (60 minutes) and Had a weaker effect than intramuscular injection.
분자량

327.40

화학식

C19H22FN3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(F)C=C1)CCCN2CCN(C3=NC=CC=C3)CC2
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

DMSO : 50 mg/mL (152.72 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 3.0544 mL 15.2718 mL 30.5437 mL
5 mM 0.6109 mL 3.0544 mL 6.1087 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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 (7.64 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 (7.64 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.
순도&문서
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 3.0544 mL 15.2718 mL 30.5437 mL 76.3592 mL
5 mM 0.6109 mL 3.0544 mL 6.1087 mL 15.2718 mL
10 mM 0.3054 mL 1.5272 mL 3.0544 mL 7.6359 mL
15 mM 0.2036 mL 1.0181 mL 2.0362 mL 5.0906 mL
20 mM 0.1527 mL 0.7636 mL 1.5272 mL 3.8180 mL
25 mM 0.1222 mL 0.6109 mL 1.2217 mL 3.0544 mL
30 mM 0.1018 mL 0.5091 mL 1.0181 mL 2.5453 mL
40 mM 0.0764 mL 0.3818 mL 0.7636 mL 1.9090 mL
50 mM 0.0611 mL 0.3054 mL 0.6109 mL 1.5272 mL
60 mM 0.0509 mL 0.2545 mL 0.5091 mL 1.2727 mL
80 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9545 mL
100 mM 0.0305 mL 0.1527 mL 0.3054 mL 0.7636 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.

Keywords:

Azaperone1649-18-9R-1929R1929R 1929Dopamine ReceptorAdrenergic ReceptorBeta Receptordopamine receptorerythrocyte splenic uptakewhite rhinocerosponiesWelsh Mountain poniesanimal behavior modificationweaned pigletsα-adrenoceptorsedationimmobilizationInhibitorinhibitorinhibit

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상품명:
Azaperone
Cat. No.:
HY-B1470
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