2. Neuronal Signaling
  3. Serotonin Transporter
  4. Azaphen

Azaphen  (Synonyms: Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride)

Cat. No.: HY-A0022
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Azaphen (Pipofezin) is an orally active serotonin reuptake inhibitor. Azaphen potentiates sympathomimetic compound effects. Azaphen can be used for the research of depressive states.

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Azaphen

Azaphen Chemical Structure

CAS No. : 24853-80-3

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Description

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

In Vivo

Azaphen (10-25 mg/kg; single dose) 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) 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) 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) 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) 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) 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) 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) 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) 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) 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) 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) 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) increases physical endurance in mice swimming with a load[2].
Azaphen (25 mg/kg; p.o.; single dose) 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 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[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 and female, 18-20 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

370.28

Formula

C16H21Cl2N5O
CAS No.
SMILES

[H]Cl.[H]Cl.CN1C2=CC=CC=C2OC3=C1C=C(N4CCN(C)CC4)N=N3
Structure Classification
Initial Source

from the cadaveric material
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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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:

Azaphen24853-80-3AzafenPipofezinPipofezineSerotonin Transporter5-HTTSERTSLC6A4scopolaminewhite ratsPhenaminewhite miceantihypoxicdepressive statesreserpineanxiolytictetrabenazineantidepressantInhibitorinhibitorinhibit

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