2. Membrane Transporter/Ion Channel
  3. Monoamine Transporter
  4. Thionisoxetine

Thionisoxetine is a norepinephrine transporter inhibitor with a Ki value of 0.2 nM in rats, and exhibits anti-hyperalgesic and analgesic activities. Thionisoxetine reverses thermal hyperalgesia and mechanical allodynia in rats. Thionisoxetine can be used in studies related to persistent inflammatory pain.

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Thionisoxetine

Thionisoxetine Chemical Structure

CAS No. : 155273-01-1

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Description

Thionisoxetine is a norepinephrine transporter inhibitor with a Ki value of 0.2 nM in rats, and exhibits anti-hyperalgesic and analgesic activities. Thionisoxetine reverses thermal hyperalgesia and mechanical allodynia in rats. Thionisoxetine can be used in studies related to persistent inflammatory pain[1].

In Vivo

Thionisoxetine (0.03-10 mg/kg; i.p.; single administration) completely reverses carrageenan-induced thermal hyperalgesia in male Sprague-Dawley rats, reverses over 80% of carrageenan-induced mechanical allodynia, and potentiates the effects of Fluoxetine (HY-B0102) on thermal hyperalgesia and mechanical allodynia[1].

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

Animal Model: Sprague-Dawley (male, 70-90 g, inflammatory pain model induced by s.c. λ-carrageenan injection)[1]
Dosage: 0.03, 0.1, 0.3, 1, 3, 10 mg/kg; 0.01, 0.03, 0.1, 0.3, 1, 3, 10 mg/kg (co-administered with 10 mg/kg fluoxetine i.p.)
Administration: i.p.; single dose
Result: Produced a complete, dose-dependent reversal of carrageenan-induced thermal hyperalgesia, significant at doses of 0.3, 1, 3, and 10 mg/kg.
Produced a greater than 80% reversal of carrageenan-induced mechanical allodynia, significant at doses of 3 and 10 mg/kg.
Produced a significant leftward shift in relative potency for reversing carrageenan-induced thermal hyperalgesia.
Produced a significant leftward shift in relative potency for reversing carrageenan-induced mechanical allodynia.
Increased brain concentrations of thionisoxetine 1.09- to 5.1-fold, with analgesic potentiation exceeding pharmacokinetic changes alone, confirming pharmacodynamic synergism.
Molecular Weight

287.42

Formula

C17H21NOS
CAS No.
SMILES

O(C=1C=CC=CC1SC)C(C=2C=CC=CC2)CCNC
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Keywords:

Thionisoxetine155273-01-1Monoamine TransporterNorepinephrine transporter inhibitorSprague-Dawley ratInflammatory painInhibitorinhibitorinhibit

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