Duloxetine-d3 (hydrochloride) (Synonyms: LY248686-d3)

Duloxetine-d₃ is intended for use as an internal standard for the quantification of duloxetine by GC- or LC-MS. (S)-Duloxetine is a potent inhibitor of serotonin and norepinephrine reuptake (K_is = 4.6 and 15.6 nM, respectively, for rat synaptosomes).¹ It also inhibits dopamine reuptake (K_i = 369 nM). (S)-Duloxetine suppresses spontaneous firing activity in vivo in the dorsal raphe and locus coeruleus (ED₅₀s = 99 and 475 µg/kg, respectively).² It also decreases immobility time and increases latency to first immobility in the forced swim test in mice when administered at doses of 16 and 32 mg/kg.³ Formulations containing (S)-duloxetine have been used in the treatment of major depressive disorder, generalized anxiety disorder, chronic neuropathic and musculoskeletal pain, and fibromyalgia.

1.Wong, D.T., Bymaster, F.P., Mayle, D.A., et al.LY248686, a new inhibitor of serotonin and norepinephrine uptakeNeuropsychopharmacology8(1)23-33(1993) 2.Kasamo, K., Blier, P., and De Montigny, C.Blockade of the serotonin and norepinephrine uptake processes by duloxetine: In vitro and in vivo studies in the rat brainJ. Pharmacol. Exp. Ther.277(1)278-286(1996) 3.CastagnÉ, V., Porsolt, R.D., and Moser, P.Use of latency to immobility improves detection of antidepressant-like activity in the behavioral despair test in the mouseEur. J. Pharmacol.616(1-3)128-133(2009)