Azaphen
(Synonyms: Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride)
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Based on 1 publication(s) in Google Scholar
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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- No. CAS: 24853-80-3
- Fòrmula: C16H21Cl2N5O
- Peso molecular:370.28
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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].
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.
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Animal Model:White mice[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:s.c.; single dose
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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.
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Animal Model:White mice[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:s.c.; single dose
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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.
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Animal Model:White mice[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:s.c.; single dose
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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.
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Animal Model:white mice (male and female, 18-20 g)[2]
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Dosage:25 mg/kg
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Administration:p.o.; single dose
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Result:Increased the number of water wheel rotations to 48 per mouse.
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Animal Model:white mice (male and female, 18-20 g)[2]
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Dosage:10 mg/kg; 25 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:white mice (male and female, 18-20 g)[2]
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Dosage:25 mg/kg
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Administration:p.o.; single dose
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Result:Increased the number of plate crossings to 10.5 per mouse, a statistically significant increase compared to the irritated control group.
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Animal Model:white mice (male and female, 18-20 g)[2]
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Dosage:25 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:white mongrel rats (male, 180-200 g)[2]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:white mongrel rats (male, 180-200 g)[2]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 4 days
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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.
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Animal Model:white mice (male and female, 18-20 g)[2]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:white mongrel rats (male, 180-200 g)[2]
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Dosage:25 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Resulted in 100% survival on both day 1 and day 5 post-ligation, a statistically significant increase compared to control.
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Animal Model:white mice (male and female, 18-20 g)[2]
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Dosage:5 mg/kg; 10 mg/kg; 25 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:white mice[2]
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Dosage:25 mg/kg
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Administration:p.o.; single dose
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Result:Resulted in 508 runs per group of 3 mice, with no statistically significant difference compared to control.
Chemical Information
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No. CAS 24853-80-3
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Peso molecular 370.28
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Fòrmula C16H21Cl2N5O
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SMILES
[H]Cl.[H]Cl.CN1C2=CC=CC=C2OC3=C1C=C(N4CCN(C)CC4)N=N3
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Synonyms
Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride
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Structure Classification
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Initial Source
from the cadaveric material
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Most Recent
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Biochim Biophys Acta Gen Subj
5-Hydroxytryptamine activates a 5-HT/c-Myc/SLC6A4 signaling loop in non-small cell lung cancer. [Abstract]2022 Apr;1866(4):130093. PMID: 35066124
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Azaphen Related Classifications
HY-A0022 Related Classifications
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