2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Adrenergic Receptor
  4. Enciprazine dihydrochloride

Enciprazine dihydrochloride is an orally active non-benzodiazepine anxiolytic. Enciprazine dihydrochloride acts as an agonist of 5-HT1A receptor (5-HT1AR) and an antagonist of α1-adrenergic receptor (α1-adrenergic receptor) . Enciprazine dihydrochloride induces drug-related electroencephalogram changes by reducing the average power of δ waves and θ waves, and increasing the average power of α waves and fast β waves. Enciprazine dihydrochloride exhibits anti-aggressive activity, with only weak sedative and ataxic effects. Enciprazine dihydrochloride regulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis. Enciprazine dihydrochloride can be used in research related to anxiety disorders, generalized anxiety syndrome and psychosis.

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Enciprazine dihydrochloride

Enciprazine dihydrochloride Chemical Structure

CAS No. : 68576-88-5

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Enciprazine dihydrochloride Related Antibodies

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Description

Enciprazine dihydrochloride is an orally active non-benzodiazepine anxiolytic. Enciprazine dihydrochloride acts as an agonist of 5-HT1A receptor (5-HT1AR) and an antagonist of α1-adrenergic receptor (α1-adrenergic receptor) . Enciprazine dihydrochloride induces drug-related electroencephalogram changes by reducing the average power of δ waves and θ waves, and increasing the average power of α waves and fast β waves. Enciprazine dihydrochloride exhibits anti-aggressive activity, with only weak sedative and ataxic effects. Enciprazine dihydrochloride regulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis. Enciprazine dihydrochloride can be used in research related to anxiety disorders, generalized anxiety syndrome and psychosis[1][2][3].

IC50 & Target[3]

5-HT1 Receptor

 

α1-adrenergic receptor

 

In Vivo

Enciprazine (p.o.) dihydrochloride exhibits anti-aggression and anxiolytic activities in male mice, with an oral ED50 of 1.4 mg/kg in the electroshock-induced fighting test[1].
Enciprazine (0.3-1.25 mg/kg; i.p.; single administration) dihydrochloride mildly prolongs the time female rats spend in the open arms in the elevated plus maze test, with a maximum increase of up to 32%; however, no activity is observed at oral doses of 1.5 to 20 mg/kg in the elevated radial arm maze test[1].
Enciprazine (p.o.) dihydrochloride exhibits ataxic sedative effects in mice, with an oral ED50 of 120 mg/kg and a therapeutic index of 86 relative to its anxiolytic and anti-aggressive activities[1].
Enciprazine (p.o.) dihydrochloride potentiates hexobarbital-induced sedation in mice, with an oral ED50 of 46.4 mg/kg, and its therapeutic index reaches 33 relative to its anxiolytic and anti-aggressive activities[1].
Enciprazine (p.o.) dihydrochloride potentiates ethanol-induced sedation in mice, with an oral ED50 of 45.5 mg/kg and a therapeutic index of 32.5 relative to its anxiolytic and anti-aggressive activities[1].
Enciprazine (25-50 mg/kg; p.o.; twice daily; administered 6 days per week for 45 days) dihydrochloride shows no tendency toward physical dependence in rats at oral doses up to 2 × 50 mg/kg per day, as evidenced by the absence of withdrawal symptoms following 45 days of chronic administration[1].
Enciprazine (5 mg/kg; i.p.; single administration) dihydrochloride induces statistically significant, time-dependent electroencephalogram (EEG) changes in freely moving male Sprague-Dawley rats, characterized by decreased δ and θ wave activities and increased α and β2 wave activities, with the peak effect occurring 30-45 minutes after injection[2].

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

Animal Model: unspecified strain (male)[1]
Dosage: unspecified (used to generate dose-response curves)
Administration: p.o.
Result: Determined an oral ED50 of 1.4 mg/kg (95% confidence interval: 0.71-2.77 mg/kg) for inhibition of fighting activity.
Animal Model: unspecified strain (female)[1]
Dosage: 0.3 mg/kg (i.p.); 1.25 mg/kg (i.p.); 1.5 mg/kg (p.o.); 20 mg/kg (p.o.)
Administration: i.p. (single dose); p.o. (single dose)
Result: Caused a weak prolongation of time spent on open arms, reaching up to 32% above baseline, at intraperitoneal doses of 0.3 to 1.25 mg/kg.
Showed no effect on time spent on open arms at oral doses of 1.5 to 20 mg/kg.
Animal Model: unspecified strain (6 mice per dose)[1]
Dosage: unspecified (used to generate dose-response curves)
Administration: p.o.
Result: Determined an oral ED50 of 120 mg/kg (95% confidence interval: 89.6-160.6 mg/kg) for induction of ataxic activity.
Calculated a therapeutic index (ED50 rotarod / ED50 fighting test) of 86.
Animal Model: unspecified strain[1]
Dosage: unspecified (used to generate dose-response curves)
Administration: p.o.
Result: Determined an oral ED50 of 46.4 mg/kg (95% confidence interval: 36.0-59.6 mg/kg) for potentiation of hexobarbital-induced sleep.
Calculated a therapeutic index (ED50 hexobarbital potentiation / ED50 fighting test) of 33.\nDetermined an oral ED50 of 45.5 mg/kg (95% confidence interval: 26.6-77.9 mg/kg) for potentiation of ethanol-induced sleep.
Calculated a therapeutic index (ED50 ethanol potentiation / ED50 fighting test) of 32.5.
Animal Model: unspecified strain (6 rats per group)[1]
Dosage: 2 × 25 mg/kg; 2 × 50 mg/kg
Administration: p.o.; twice daily; 6 days/week for 45 days
Result: Observed no withdrawal symptoms (diarrhea, tremor, jumping, piloerection, restlessness, salivation) in rats treated with either dose after compound withdrawal.
Detected no weight loss post-withdrawal.
Animal Model: Sprague-Dawley (male, 160-210 g, SIV 50)[2]
Dosage: 5 mg/kg
Administration: i.p.; single injection
Result: Induced statistically significant EEG changes first observed 15 minutes post-injection, peaked between 30-45 minutes, and persisted for 75 minutes.
Molecular Weight

505.43

Formula

C23H34Cl2N2O6
CAS No.
SMILES

OC(CN1CCN(CC1)C2=C(OC)C=CC=C2)COC3=CC(OC)=C(OC)C(OC)=C3.Cl.Cl
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Purity & Documentation
References
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Keywords:

Enciprazine68576-88-55-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptordexamethasonegeneralised anxiety syndromesmale Sprague-Dawley ratsmale miceα1-adrenergic binding siteshypothalamic-pituitary-adrenocortical axisanxietycorticosterone5-HT1ApsychosisInhibitorinhibitorinhibit

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