Title : Relationship between serotonin transporter occupancies and analgesic effects of AS1069562, the (+)-isomer of indeloxazine, and duloxetine in reserpine-induced myalgia rats.

Pub. Date : 2015 Mar 19

PMID : 25595980






5 Functional Relationships(s)
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1 Here, we investigated the relationship between SERT occupancies and the analgesic effects of AS1069562, the (+)-isomer of indeloxazine, and duloxetine, which are both 5-HT and NE reuptake inhibitors (SNRIs), on muscular pain in reserpine-induced myalgia (RIM) rats, an animal model of FM-like chronic pain. Duloxetine Hydrochloride solute carrier family 6 member 4 Rattus norvegicus
2 We also investigated the SERT occupancy level necessary for AS1069562 and duloxetine to exert analgesic effects on muscular pain. Duloxetine Hydrochloride solute carrier family 6 member 4 Rattus norvegicus
3 SERT occupancy levels of AS1069562 and duloxetine increased in both dose- and plasma and brain concentration-dependent manners. Duloxetine Hydrochloride solute carrier family 6 member 4 Rattus norvegicus
4 SERT occupancy levels of AS1069562 and duloxetine were significantly correlated with efficacy on muscular pain thresholds in RIM rats. Duloxetine Hydrochloride solute carrier family 6 member 4 Rattus norvegicus
5 SERT occupancy level above 70% was necessary for AS1069562 and duloxetine to exert significant analgesic effects on muscular pain. Duloxetine Hydrochloride solute carrier family 6 member 4 Rattus norvegicus