2. Neuronal Signaling
  3. Serotonin Transporter
  4. Azaphen dihydrochloride monohydrate

Azaphen dihydrochloride monohydrate  (Synonyms: Azafen dihydrochloride monohydrate; Pipofezin dihydrochloride monohydrate; Pipofezine dihydrochloride monohydrate; Azaphenonxazine dihydrochloride monohydrate)

Cat. No.: HY-A0022A Purity: 99.94%
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Azaphen (Pipofezin) dihydrochloride monohydrate is an orally active serotonin reuptake inhibitor. Azaphen dihydrochloride monohydrate potentiates sympathomimetic compound effects. Azaphen dihydrochloride monohydrate can be used for the research of depressive states.

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

Azaphen dihydrochloride monohydrate

Azaphen dihydrochloride monohydrate Chemical Structure

CAS No. : 63302-99-8

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

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Azaphen dihydrochloride monohydrate Related Antibodies

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1 Publications Citing Use of MCE Azaphen dihydrochloride monohydrate

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Azaphen (Pipofezin) dihydrochloride monohydrate is an orally active serotonin reuptake inhibitor. Azaphen dihydrochloride monohydrate potentiates sympathomimetic compound effects. Azaphen dihydrochloride monohydrate can be used for the research of depressive states[1][2].

In Vivo

Azaphen (10-25 mg/kg; single dose) dihydrochloride monohydrate significantly prolongs Phenamine (HY-W016477)-induced stereotypic behavioral reactions in white rats, with mean durations increased to 105 min and 147 min, respectively[1].
Azaphen (25-50 mg/kg; s.c.; single dose) dihydrochloride monohydrate significantly increases the group toxicity of Phenamine in white mice, inducing up to 95% mortality when combined with 10 mg/kg Phenamine, while also enhancing Phenamine-induced motor activity and hyperthermia[1].
Azaphen (25-50 mg/kg; s.c.; single dose) dihydrochloride monohydrate antagonizes Reserpine (HY-N0480)-induced depression effects in white mice, reducing blepharoptosis to 2.6 points and 2.3 points, respectively, while decreasing hypothermia[1].
Azaphen (25-50 mg/kg; s.c.; single dose) dihydrochloride monohydrate antagonizes Tetrabenazine (HY-B0590)-induced depression effects in white mice, reducing blepharoptosis to 2.3 points and 1.1 points, respectively, while decreasing hypothermia and catalepsy[1].
Azaphen (25 mg/kg; p.o.; single dose) dihydrochloride monohydrate significantly increases active escape attempts in the mouse water escape test, with a mean of 48 water wheel rotations per mouse over 6 minutes[2].
Azaphen (10-25 mg/kg; p.o.; single dose) dihydrochloride monohydrate exhibits antireserpine activity in mice, with a statistically significant reduction in Reserpine-induced blepharoptosis at 25 mg/kg to a rate of 2.7[2].
Azaphen (25 mg/kg; p.o.; single dose) dihydrochloride monohydrate significantly reduces anxiety-related inhibition in mice exposed to electric irritation, increasing plate crossings to 10.5 over 2 minutes[2].
Azaphen (25 mg/kg; p.o.; single dose) dihydrochloride monohydrate significantly reduces aggressive behavior in mice, decreasing fight counts to 8 (isolation-induced) and 9 (electric irritation-induced)[2].
Azaphen (10 mg/kg; p.o.; single dose) dihydrochloride monohydrate significantly reduces amnesia in rats, increasing passive avoidance conditioned reflex retention to 30% (electroshock-induced) and 50% (Scopolamine (HY-N0296)-induced)[2].
Azaphen (10 mg/kg; p.o.; daily; 4 days) dihydrochloride monohydrate does not produce a statistically significant restoration of ethanol-impaired active avoidance conditioned reflex learning in rats[2].
Azaphen (25-100 mg/kg; p.o.; single dose) dihydrochloride monohydrate exhibits dose-dependent antihypoxic activity in mice, significantly increasing survival time in hypoxic hypoxia at 50 mg/kg (37 min) and 100 mg/kg (44 min), and in hemic hypoxia at 25 mg/kg (22 min) and 50 mg/kg (21 min)[2].
Azaphen (25 mg/kg; p.o.; daily; 5 days) dihydrochloride monohydrate produces a pronounced protective effect in rats with circulatory hypoxia, resulting in 100% survival over 5 days[2].
Azaphen (5-25 mg/kg; p.o.; single dose) dihydrochloride monohydrate increases physical endurance in mice swimming with a load[2].
Azaphen (25 mg/kg; p.o.; single dose) dihydrochloride monohydrate does not produce a statistically significant change in mouse motor activity[2].

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

Animal Model: White mice[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: s.c.; single dose
Result: Caused 35% mortality when combined with Phenamine (5 mg/kg).
Caused 65% mortality when combined with Phenamine (5 mg/kg).
Caused 60% mortality when combined with Phenamine (10 mg/kg).
Caused 95% mortality when combined with Phenamine (10 mg/kg).
Enhanced Phenamine-induced motor activity and hyperthermia.
Animal Model: White mice[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: s.c.; single dose
Result: Reduced Reserpine-induced blepharoptosis from a control of 3.7 points to 2.6 points.
Reduced Reserpine-induced blepharoptosis from a control of 3.7 points to 2.3 points.
Decreased Reserpine-induced hypothermia.
Animal Model: White mice[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: s.c.; single dose
Result: Reduced Tetrabenazine-induced blepharoptosis from a control of 3.2 points to 2.3 points.
Reduced Tetrabenazine-induced blepharoptosis from a control of 3.2 points to 1.1 points.
Decreased Tetrabenazine-induced hypothermia and catalepsy.
Animal Model: white mice (male and female, 18-20 g)[2]
Dosage: 25 mg/kg
Administration: p.o.; single dose
Result: Increased the number of water wheel rotations to 48 per mouse.
Animal Model: white mice (male and female, 18-20 g)[2]
Dosage: 10 mg/kg; 25 mg/kg
Administration: p.o.; single dose
Result: Resulted in a blepharoptosis rate of 3.0 per mouse at 10 mg/kg.
Resulted in a blepharoptosis rate of 2.7 per mouse at 25 mg/kg, which was statistically significant compared to control.
Animal Model: white mice (male and female, 18-20 g)[2]
Dosage: 25 mg/kg
Administration: p.o.; single dose
Result: Increased the number of plate crossings to 10.5 per mouse, a statistically significant increase compared to the irritated control group.
Animal Model: white mice (male, 22-25 g)[2]
Dosage: 25 mg/kg
Administration: p.o.; single dose
Result: Reduced the number of fights to 8 in isolation-induced aggression, statistically significant compared to control.
Reduced the number of fights to 9 in electric irritation-induced aggression, statistically significant compared to control.
Animal Model: white mongrel rats (male, 180-200 g)[2]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Increased the percentage of rats retaining PACR from 3% to 30% in electroshock-induced amnesia, statistically significant compared to control.
Increased the percentage of rats retaining PACR from 20% to 50% in Scopolamine-induced amnesia, statistically significant compared to control.
Animal Model: white mongrel rats (male, 180-200 g)[2]
Dosage: 10 mg/kg
Administration: p.o.; daily; 4 days
Result: Resulted in 2, 7, 13, and 14 AACR events over 10 runs in 10 rats on days 1-4 of training, with no statistically significant difference compared to the ethanol-only control group.
Animal Model: white mice (male and female, 18-20 g)[2]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Increased survival time to 34 min in hypoxic hypoxia at 25 mg/kg.
Increased survival time to 37 min in hypoxic hypoxia at 50 mg/kg, statistically significant.
Increased survival time to 44 min in hypoxic hypoxia at 100 mg/kg, statistically significant.
Increased survival time to 22 min in hemic hypoxia at 25 mg/kg, statistically significant.
Increased survival time to 21 min in hemic hypoxia at 50 mg/kg, statistically significant.
Animal Model: white mongrel rats (male, 180-200 g)[2]
Dosage: 25 mg/kg
Administration: p.o.; daily; 5 days
Result: Resulted in 100% survival on both day 1 and day 5 post-ligation, a statistically significant increase compared to control.
Animal Model: white mice (male and female, 18-20 g)[2]
Dosage: 5 mg/kg; 10 mg/kg; 25 mg/kg
Administration: p.o.; single dose
Result: Increased swimming duration to 8.3 min at 5 mg/kg, statistically significant.
Increased swimming duration to 11.8 min at 10 mg/kg, statistically significant.
Increased swimming duration to 12.1 min at 25 mg/kg, statistically significant.
Animal Model: white mice[2]
Dosage: 25 mg/kg
Administration: p.o.; single dose
Result: Resulted in 508 runs per group of 3 mice, with no statistically significant difference compared to control.
Molecular Weight

388.29

Formula

C16H23Cl2N5O2
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

[H]Cl.[H]Cl.CN1C2=CC=CC=C2OC3=C1C=C(N4CCN(C)CC4)N=N3.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (257.54 mM)

DMSO : 1 mg/mL (2.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5754 mL 12.8770 mL 25.7539 mL
5 mM 0.5151 mL 2.5754 mL 5.1508 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (128.77 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.94%

SDS (252 KB)

COA (251 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). 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
DMSO / H2O 1 mM 2.5754 mL 12.8770 mL 25.7539 mL 64.3849 mL
H2O 5 mM 0.5151 mL 2.5754 mL 5.1508 mL 12.8770 mL
10 mM 0.2575 mL 1.2877 mL 2.5754 mL 6.4385 mL
15 mM 0.1717 mL 0.8585 mL 1.7169 mL 4.2923 mL
20 mM 0.1288 mL 0.6438 mL 1.2877 mL 3.2192 mL
25 mM 0.1030 mL 0.5151 mL 1.0302 mL 2.5754 mL
30 mM 0.0858 mL 0.4292 mL 0.8585 mL 2.1462 mL
40 mM 0.0644 mL 0.3219 mL 0.6438 mL 1.6096 mL
50 mM 0.0515 mL 0.2575 mL 0.5151 mL 1.2877 mL
60 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0731 mL
80 mM 0.0322 mL 0.1610 mL 0.3219 mL 0.8048 mL
100 mM 0.0258 mL 0.1288 mL 0.2575 mL 0.6438 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Keywords:

Azaphen dihydrochloride63302-99-8Azafen dihydrochloridePipofezin dihydrochloridePipofezine dihydrochlorideAzaphenonxazine dihydrochlorideSerotonin Transporter5-HTTSERTSLC6A4scopolaminewhite ratsPhenaminewhite miceantihypoxicdepressive statesreserpineanxiolytictetrabenazineantidepressantInhibitorinhibitorinhibit

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