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[1] bioRxiv preprint
Purity: ≥98%
Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC50 of 723, 491 and 763 nM, respectively.
| Targets |
Serotonin (IC50 = 723 nM); dopamine (IC50 = 491 nM); norepinephrine (IC50 = 763 nM)
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|---|---|
| ln Vitro |
Triple reuptake inhibitors (TRIs) are currently being developed as a new class of promising antidepressants that block serotonin (5-HT), dopamine (DA) and norepinephrine (NE) transporters, thereby increasing extracellular monoamine concentrations. The purpose of this study was to investigate the effects of LPM570065, a novel TRI and a desvenlafaxine prodrug, on extracellular 5-HT, DA and NE levels in the rat striatum after acute and chronic administration relative to desvenlafaxine, using High Performance Liquid Chromatography (HPLC) and microdialysis[1].
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| ln Vivo |
Ansofaxine enters the rat striatum quickly, transforms into desvenlafaxine, and shows a greater overall exposure when compared to when desvenlafaxine is administered. The administration of oral suspension of ansofaxine, both acutely and chronically, is associated with higher levels of 5-HT, dopamine, and norepinephrine than is the case with desvenlafaxine administration. Acute intravenous ansofaxine solution administration does not result in the unwanted 90% reduction in extracellular 5-HT levels, in contrast to desvenlafaxine. When combined with WAY-100635, acute ansofaxine administration results in a capped increase in extracellular 5-HT levels. More so than desvenlafaxine administration in comparison, ansofaxine administration, both acute and chronic, shortens the period of immobility[1].
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| Animal Protocol |
Rats: This study uses oral solutions, oral suspensions, and intravenous solutions of ansofaxine and desvenlafaxine to investigate the effects of acute administration on extracellular 5-HT, DA, and NE levels. When 5-HT1A receptors are blocked by pretreatment with WAY-100635, an equal number of animals are used to investigate the acute effects of ansofaxine and desvenlafaxine on extracellular 5-HT levels. Pets are split into three groups at random for the 14-day chronic administration. Every day for 14 days, oral suspensions of desvenlafaxine, ansofaxine, and vehicle are given. The impact of ansofaxine and desvenlafaxine on extracellular 5-HT, DA, and NE levels is investigated on the fourteenth day of chronic administration[1].
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| References | |
| Additional Infomation |
Acute administration was performed by providing rodents with oral solutions (0.06 mmol·kg(-1) p.o.), oral suspensions (0.06 mmol·kg(-1) p.o.) and intravenous solutions (0.04 mmol·kg(-1) i.v.) of LPM570065 and desvenlafaxine. Oral suspensions (0.06 mmol·kg(-1)·day(-1)) of the two drugs were also administered for a 14-day chronic period. HPLC analysis revealed that LPM570065 rapidly penetrated the rat striatum, converted into desvenlafaxine and exhibited larger total exposure compared with the administration of desvenlafaxine. Microdialysis revealed that acute and chronic administration of oral suspension of LPM570065 increased the 5-HT, DA and NE levels more than the relative administration of desvenlafaxine. Unlike desvenlafaxine, acute administration of an intravenous LPM570065 solution did not induce the undesirable 90% decrease in extracellular 5-HT levels. In contrast to the fully dose-dependent elevation of 5-HT induced by desvenlafaxine, the acute administration of LPM570065 showed a capped increase in extracellular 5-HT levels when combined with WAY-100635. Additionally, forced swim test demonstrated that acute and chronic administration of LPM570065 reduced the immobility time more than the relative administration of desvenlafaxine. These data suggest that LPM570065 may have greater efficacy and/or a more rapid onset of antidepressant action than desvenlafaxine and also counterbalance the harmful effects of desvenlafaxine on 5-HT neurotransmission related to 5-HT1A autoreceptors. Thus, this new class of drugs, TRIs has the potential to provide a new therapeutic mechanism for treating depression[1].
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| Molecular Formula |
C₂₄H₃₂CLNO₃
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|---|---|
| Molecular Weight |
417.97
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| Exact Mass |
417.21
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| Elemental Analysis |
C, 68.97; H, 7.72; Cl, 8.48; N, 3.35; O, 11.48
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| CAS # |
916918-84-8
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| Related CAS # |
Ansofaxine; 916918-80-4; 916918-84-8 (HCl); 2137075-66-0 (HCl hydrate)
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| Appearance |
White to off-white solid powder
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| tPSA |
49.8Ų
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| SMILES |
CC1=CC=C(C=C1)C(=O)OC2=CC=C(C=C2)C(CN(C)C)C3(CCCCC3)O.Cl
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| InChi Key |
BVWFJKQJRNSYCR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H31NO3.ClH/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;1H
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| Chemical Name |
[4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl] 4-methylbenzoate;hydrochloride
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| Synonyms |
LY03005; LY-03005; LY 03005; Ansofaxine hydrochloride; Ansofaxine HCl; Toludesvenlafaxine; LPM570065; LPM 570065; LPM-570065
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 31.3~84 mg/mL (74.8~201 mM)
Ethanol: ~42 mg/mL Water: ~3 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3925 mL | 11.9626 mL | 23.9252 mL | |
| 5 mM | 0.4785 mL | 2.3925 mL | 4.7850 mL | |
| 10 mM | 0.2393 mL | 1.1963 mL | 2.3925 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04853407 | Completed | Drug: LY03005 extended-release tablet Drug: Placebo |
Major Depressive Disorder (MDD) |
Luye Pharma Group Ltd. | December 5, 2018 | Phase 3 |
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