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

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.

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Tracizoline

Tracizoline Chemical Structure

CAS No. : 65248-90-0

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Description

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

 

In Vivo

Tracizoline (10 mg/kg; i.p.; daily; 7 days) significantly increases hippocampal FADD protein content by 19% in 6- and 12-month-old male Sprague-Dawley rats[1].
Tracizoline (10 mg/kg; i.p.; daily for 7 days or three doses over 24 hours) does not alter body weight, body temperature, cognitive performance, or affective-like behavior in 9-10-month-old male Sprague-Dawley rats[1].
Tracizoline (10-32 mg/kg; i.p.) produces dose-dependent antihyperalgesic effects in rats with CFA-induced inflammatory pain, reaching a maximum 62.1% MPE for mechanical hyperalgesia and 72.0% MPE for thermal hyperalgesia, with ED50 values of ~10.3 mg/kg and ~10.4 mg/kg respectively[2].

MedChemExpress (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.
Molecular Weight

172.23

Formula

C11H12N2

CAS No.
SMILES

C1(/C=C/C2=CC=CC=C2)=NCCN1

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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.

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