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Ansofaxine Other names LY03005; LPM570065; 4-Methylbenzoate desvenlafaxine hydrochloride Routes of administration By mouth
4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate
CAS Number PubChem CID ChemSpider UNII Formula C 24 H 31 N O 3 Molar mass 381.516 g·mol−1 3D model (JSmol )
Cc1ccc(cc1)C(=O)Oc2ccc(cc2)C(CN(C)C)C3(CCCCC3)O
InChI=1S/C24H31NO3/c1-18-7-9-20(10-8-18)23(26)28-21-13-11-19(12-14-21)22(17-25(2)3)24(27)15-5-4-6-16-24/h7-14,22,27H,4-6,15-17H2,1-3H3
Key:QKYBZJLEMOZFFU-UHFFFAOYSA-N
Ansofaxine hydrochloride (INN Tooltip International Nonproprietary Name ) (former developmental code names LY03005 , LPM570065 ), also known as 4-methylbenzoate desvenlafaxine hydrochloride , is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) which is under development by Luye Pharma Group for the treatment of major depressive disorder (MDD).[ 1] [ 2] [ 3] [ 4] It is described as an SNDRI and prodrug to desvenlafaxine .[ 2] However, unlike desvenlafaxine, which has in vitro IC50 Tooltip half-maximal inhibitory concentration values of 53 nM and 538 nM for inhibition of serotonin and norepinephrine reuptake , respectively, ansofaxine has respective in vitro IC50 values of 723 nM, 763 nM, and 491 nM for serotonin, norepinephrine, and dopamine reuptake inhibition.[ 2] As of July 2018, the drug is in preregistration for MDD in the United States , the European Union , Japan , and China .[ 1]
See also
References
^ a b http://adisinsight.springer.com/drugs/800039935
^ a b c Zhang R, Li X, Shi Y, Shao Y, Sun K, Wang A, Sun F, Liu W, Wang D, Jin J, Li Y (2014). "The effects of LPM570065, a novel triple reuptake inhibitor, on extracellular serotonin, dopamine and norepinephrine levels in rats" . PLOS ONE . 9 (3): e91775. doi :10.1371/journal.pone.0091775 . PMC 3948889 . PMID 24614602 . {{cite journal }}
: CS1 maint: unflagged free DOI (link )
^ Dale, Elena; Bang-Andersen, Benny; Sánchez, Connie (2015). "Emerging mechanisms and treatments for depression beyond SSRIs and SNRIs" . Biochemical Pharmacology . 95 (2): 81–97. doi :10.1016/j.bcp.2015.03.011 . ISSN 0006-2952 . PMID 25813654 .
^ Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.
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