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Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.

Ansofaxine rapidly penetrates the rat striatum, converts into desvenlafaxine and exhibits larger total exposure compared with the administration of desvenlafaxine. Acute and chronic administration of oral suspension of ansofaxine increases the 5-HT, dopamine and norepinephrine levels more than the relative administration of desvenlafaxine. Unlike desvenlafaxine, acute administration of an intravenous ansofaxine solution does not induce the undesirable 90% decrease in extracellular 5-HT levels. The acute administration of ansofaxine shows a capped increase in extracellular 5-HT levels when combined with WAY-100635. Acute and chronic administration of ansofaxine reduces the immobility time more than the relative administration of desvenlafaxine[1].

[1]. Zhang R, et al. The effects of LPM570065, a novel triple reuptake inhibitor, on extracellular serotonin, dopamineand norepinephrine levels in rats. PLoS One. 2014 Mar 10;9(3):e91775.

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