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Liafensine

Catalog No. T32737 CAS 1198790-53-2

Synonyms: BMS820836, BMS 820836, DB104, BMS-820836

Liafensine(BMS-820836) is a novel and selective triple monoamine reuptake inhibitor with inhibitory effects on the reuptake of serotonin, norepinephrine, and dopamine for the study of major depressive disorder and central nervous system disorders.

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Liafensine, CAS 1198790-53-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 387.00
5 mg	In stock	$ 923.00
10 mg	In stock	$ 1,260.00
25 mg	In stock	$ 1,870.00
50 mg	In stock	$ 2,520.00

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Purity: 99.46%

ee: 100%

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Description

In vivo

Healthy subjects were assigned to seven BMS-820836 dose panels (0.025, 0.1, 0.5, 1, 2, 3, and 5 mg; n = 8 each), in which subjects were randomly allocated 3:1 to a single BMS-820836 dose or matched placebo. Serial blood samples were collected on Days 1, 2, 3, 4, 7, and 14 to characterize the PK of BMS-820836. Following evaluation of the maximum tolerated dose, SERT occupancy was determined by applying [(11)C]DASB positron emission tomography (PET) after single-dose BMS-820836 (0.5 or 3 mg; n = 3 each) and DAT occupancy by applying [(11)C]PE2I PET after single-dose BMS-820836 (3 mg; n = 6). RESULTS: Single oral doses of BMS-820836 (0.025-3 mg) were generally safe and well tolerated. BMS-820836 had a median T max of 5.0-7.2 h and a mean apparent terminal T 1/2 of 34-57 h. Mean striatal SERT occupancies were 19 ± 9 % and 82 ± 8 % after single doses of 0.5 and 3 mg BMS-820836, respectively. The mean striatal DAT occupancy was 19 ± 9 % after a single 3 mg BMS-820836 dose. CONCLUSIONS: Single doses of BMS-820836 have meaningful SERT and DAT occupancy and demonstrate an acceptable safety and tolerability profile in healthy control subjects.[1]

Synonyms	BMS820836, BMS 820836, DB104, BMS-820836
Molecular Weight	366.46
Formula	C24H22N4
CAS No.	1198790-53-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Risinger R, et al. Evaluation of safety and tolerability, pharmacokinetics, and pharmacodynamics of BMS-820836 in healthy subjects: a placebo-controlled, ascending single-dose study. Psychopharmacology (Berl). 2014 Jun;231(11):2299-310. 2. Zheng M, et al. Safety, pharmacokinetic, and positron emission tomography evaluation of serotonin and dopamine transporter occupancy following multiple-dose administration of the triple monoamine reuptake inhibitor BMS-820836. Psychopharmacology (Berl). 2015 Feb;232(3):529-40. 3. Bhagwagar Z, et al. Assessment of the Efficacy and Safety of BMS-820836 in Patients With Treatment-Resistant Major Depression: Results From 2 Randomized, Double-Blind Studies. J Clin Psychopharmacol. 2015 Aug;35(4):454-9. 4. Zheng M, et al. Comparison of different QT interval correction methods for heart rate and QT beat-to-beat method in a thorough QT study of triple monoamine reuptake inhibitor BMS-820836. J Clin Pharmacol. 2015 Oct;55(10):1137-46.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Liafensine 1198790-53-2 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Norepinephrine BMS820836 BMS 820836 DB104 DB 104 BMS-820836 DB-104 inhibitor inhibit

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