2. Neuronal Signaling GPCR/G Protein
  3. Imidazoline Receptor 5-HT Receptor Adrenergic Receptor
  4. Tracizoline

Tracizoline 是一种口服有效的 I2-imidazoline 受体激动剂。Tracizoline 可对 I2-imidazoline 受体进行功能性调节，调控海马区 FADD 细胞命运衔接蛋白，减轻机械性和热痛觉过敏，以极弱的部分激动作用激活 α2A-adrenergic 受体，并通过激活 5-HT1A 受体诱导类抗抑郁活性。Tracizoline 可用于炎性疼痛、神经性疼痛及抑郁症的相关研究。

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Tracizoline

Tracizoline Chemical Structure

CAS No. : 65248-90-0

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Tracizoline 相关抗体

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tracizoline is an orally active I2-imidazoline receptor agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α2A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT1A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression[1][2][3].

IC50 & Target[1]

5-HT1A Receptor

 

α2-adrenergic receptor

 

体内研究
(In Vivo)

Tracizoline (10 mg/kg；腹腔注射；每日一次；连续 7 天) 可使 6 月龄和 12 月龄雄性 Sprague-Dawley 大鼠的海马 FADD 蛋白含量显著升高 19%[1]。
Tracizoline (10 mg/kg；腹腔注射；每日 1 次，连续 7 天或 24 小时内给药 3 次) 不会改变 9~10 月龄雄性 Sprague-Dawley 大鼠的体重、体温、认知表现或类情感行为[1]。
Tracizoline (3.2-32 mg/kg；腹腔注射) 可在 CFA 诱导的炎性疼痛大鼠中产生剂量依赖性的抗痛觉过敏作用，对机械性痛觉过敏的最大 MPE 达 62.1%，对热痛觉过敏的最大 MPE 达 72.0%，其 ED50 值分别约为 10.3 mg/kg 和 10.4 mg/kg[2]。

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

Animal Model: Sprague-Dawley (male, 6 or 12 months old)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; 7 days
Result: Increased hippocampal FADD protein content by 19% compared to saline-treated control rats.
Did not significantly alter hippocampal FADD levels compared to saline-treated control rats.
Animal Model: Sprague-Dawley (male, 9-10 months old)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily for 7 days or three doses over 24 hours
Result: Did not alter body weight over the 7-day treatment period.
Did not induce hypothermia (no significant change in core body temperature compared to controls).
Did not change the time needed to complete the 8-arm radial maze or the number of errors committed on day 1 or day 8.
Did not significantly alter the time spent immobile or climbing in the forced-swim test compared to saline-treated control rats.
Animal Model: Sprague-Dawley (adult male, CFA-induced inflammatory pain)[2]
Dosage: 3.2 mg/kg; 10 mg/kg; 32 mg/kg
Administration: i.p.
Result: Increased paw withdrawal threshold (mechanical hyperalgesia) and paw withdrawal latency (thermal hyperalgesia) dose-dependently in the CFA-treated paw, with no effect on the non-injured paw.
Significantly increased both paw withdrawal threshold and paw withdrawal latency in the CFA-treated paw at 10 mg/kg and 32 mg/kg (P < 0.05).
Produced a maximum of 62.1% maximal possible effect (MPE) in the von Frey test (mechanical hyperalgesia) and 72.0% MPE in the plantar test (thermal hyperalgesia).
Reached ED50 values of 10 mg/kg in the von Frey test and 10 mg/kg in the plantar test.
分子量

172.23

Formula

C11H12N2
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

Tracizoline 相关分类

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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:

Tracizoline65248-90-0Imidazoline Receptor5-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorI2-imidazoline receptorhippocampal FADD cell fateα2A-adrenergic receptors5-HT1A receptorinflammatory painneuropathic paindepressionInhibitorinhibitorinhibit

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