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Thionisoxetine

Thionisoxetine is a norepinephrine transporter inhibitor with a K_i 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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CAS No.: 155273-01-1
Formule: C₁₇H₂₁NOS
Masse moléculaire:287.42

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Please store the product under the recommended conditions in the Certificate of Analysis.

Thionisoxetine Chemical Structure

CAS No.: 155273-01-1

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Activité biologique
- Description
- In Vivo
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

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.

Chemical Information

CAS No. 155273-01-1
Masse moléculaire 287.42
Formule C₁₇H₂₁NOS
SMILES

O(C=1C=CC=CC1SC)C(C=2C=CC=CC2)CCNC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Jones CK, et al. Analgesic effects of serotonergic, noradrenergic or dual reuptake inhibitors in the carrageenan test in rats: evidence for synergism between serotonergic and noradrenergic reuptake inhibition. Neuropharmacology. 2006;51(7-8):1172-1180. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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