Ansofaxine hydrochloride

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.

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

IC50: 723 nM (serotonin), 491 nM (dopamine), 763 nM (norepinephrine)[1]

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].

Rats: Acute administration to examine the effects of ansofaxine and desvenlafaxine on extracellular 5-HT, DA and NE levels is performed by administering oral solutions, oral suspensions and intravenous solutions of ansofaxine and desvenlafaxine. An equal number of animals are used to examine the acute effects of ansofaxine and desvenlafaxine on extracellular 5-HT levels under the blockade of 5-HT1A receptors by pretreatment with WAY-100635. For the 14-day chronic administration, animals are randomly divided into three groups. Oral suspensions of ansofaxine, desvenlafaxine and vehicle are administered daily for 14 days. On the 14th day of chronic administration, the effects of ansofaxine and desvenlafaxine on the extracellular 5-HT, DA and NE levels are examined[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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