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

Enciprazine dihydrochloride 是一种口服有效的非苯二氮䓬类抗焦虑剂。Enciprazine dihydrochloride 是一种 5-HT1A 受体 (5-HT1AR) 激动剂和 α1-肾上腺素能受体 (α1-adrenergic receptor) 拮抗剂。Enciprazine dihydrochloride 可通过降低 δ 波和 θ 波平均功率、升高 α 波和快 β 波平均功率来诱发药物脑电图改变。Enciprazine dihydrochloride 具有抗攻击活性，仅表现出微弱的镇静和共济失调作用。Enciprazine dihydrochloride 可调节血浆皮质酮水平并激活下丘脑-垂体-肾上腺皮质轴。Enciprazine dihydrochloride 可用于焦虑症、广泛性焦虑综合征及精神病的相关研究。

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Enciprazine dihydrochloride

Enciprazine dihydrochloride Chemical Structure

CAS No. : 68576-88-5

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Enciprazine dihydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体内研究
(In Vivo)

Enciprazine (口服) dihydrochloride 在雄性小鼠中表现出抗攻击抗焦虑活性，在电休克诱导打斗试验中的口服 ED50 为 1.4 mg/kg[1]。
Enciprazine (0.3-1.25 mg/kg；腹腔注射；单次给药) dihydrochloride 可使雌性大鼠在高架十字迷宫实验中在开放臂停留的时间轻度延长，最高可达 32%；而在高架放射臂迷宫实验中，1.5 至 20 mg/kg 的口服剂量未观察到活性[1]。
Enciprazine (口服) dihydrochloride 在小鼠中表现出共济失调镇静作用，口服 ED50 为 120 mg/kg，相较于其抗焦虑抗攻击活性，治疗指数为 86[1]。
Enciprazine (口服) dihydrochloride 可增强小鼠中己巴比妥诱导的镇静作用，其口服 ED50 为 46.4 mg/kg，相对于其抗焦虑抗攻击活性，治疗指数达 33[1]。
Enciprazine (口服) dihydrochloride 可增强乙醇诱导的小鼠镇静作用，其口服 ED50 为 45.5 mg/kg，相较于其抗焦虑抗攻击活性，治疗指数为 32.5[1]。
Enciprazine (25-50 mg/kg；口服；每日 2 次；每周给药 6 天，持续 45 天) dihydrochloride 在大鼠中每日口服剂量高达 2 × 50 mg/kg 时，未表现出躯体依赖性倾向，这一点可由长期给药 45 天后未出现戒断症状得到证实[1]。
Enciprazine (5 mg/kg；腹腔注射；单次给药) dihydrochloride 可在自由活动的雄性 Sprague-Dawley 大鼠中诱导具有统计学意义、时间依赖性的脑电图 (EEG) 变化，表现为 δ 波和 θ 波活动减弱，α 波和 β2 波活动增强，且注射后 30-45 分钟达到作用峰值[2]。

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.
分子量

505.43

Formula

C23H34Cl2N2O6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Enciprazine dihydrochloride 相关分类

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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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