Ansofaxine

Ansofaxine
Clinical data
Routes of; administration	Oral
ATC code	None
Identifiers
	IUPAC name 4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate;
ChemSpider	13114670
Chemical and physical data
Formula	C24H31NO3
Molar mass	381.508 g/mol
3D model (Jmol)	Interactive image
	SMILES Cc1ccc(cc1)C(=O)Oc2ccc(cc2)C(CN(C)C)C3(CCCCC3)O ;
	InChI 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) (former developmental code names LY03005, LPM570065), also known as 4-methylbenzoate desvenlafaxine hydrochloride, is a serotonin-norepinephrine-dopamine reuptake inhibitor that is under development by Luye Pharma Group for the treatment of major depressive disorder.^[1]^[2]^[3] It is described as an SNDRI and prodrug to desvenlafaxine.^[1] However, unlike desvenlafaxine, which has in vitro IC₅₀ 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.^[1] As of March 2015, the drug is in phase I clinical trials.^[3]^[4]

References[edit]

^ ^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.
^ 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.
^ ^a ^b Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.
^ Ansofaxine - AdisInsight

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[pmid24614602-1] 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.

[DaleBang-Andersen2015-2] 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.

[evaluategroup-3] Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.

[4] Ansofaxine - AdisInsight

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[2]

[3]

[4]

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Phenylisobutylamines	Entactogens: 4-CAB 4-MAB Ariadne BDB Butylone EBDB Eutylone MBDB Stimulants: Phenylisobutylamine

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Ansofaxine

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Clinical data

Routes of administration	Oral
ATC code	None
Identifiers
IUPAC name 4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate
ChemSpider	13114670
Chemical and physical data
Formula	C₂₄H₃₁NO₃
Molar mass	381.508 g/mol
3D model (Jmol)	Interactive image
SMILES Cc1ccc(cc1)C(=O)Oc2ccc(cc2)C(CN(C)C)C3(CCCCC3)O
InChI 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