Tesofensine

Синонимы: Tesofensine, (1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane, NS2330, Tesofensine hydrochloride

Tesofensine is a synthetic phenyltropane derivative that acts as a triple monoamine reuptake inhibitor, targeting the serotonin, norepinephrine, and dopamine transporters (SERT, NET, DAT). Its structure features a tropane ring system substituted with a 3,4-dichlorophenyl group and an ethoxymethyl side chain, which confers high lipophilicity and blood-brain barrier permeability. This unique pharmacophore allows tesofensine to modulate monoaminergic neurotransmission without the psychostimulant effects typical of amphetamine-like compounds.

Originally developed for Parkinson’s disease and Alzheimer’s disease, tesofensine was later investigated for obesity treatment due to its appetite-suppressing and energy-expenditure-enhancing properties. It is clinically studied as an oral agent, with phase II trials demonstrating significant weight loss in obese patients. Tesofensine is available as a research chemical and active pharmaceutical ingredient (API) for further development, with strict quality control to ensure purity and consistency.

In the B2B pharmaceutical supply chain, tesofensine is primarily sought for its potential in metabolic disorders and CNS research. Its dual mechanism—inhibiting reuptake of all three monoamines—offers a promising avenue for developing therapies for obesity, addiction, and cognitive impairment. As a result, demand for high-purity tesofensine API has grown among pharmaceutical companies and research institutions.

Chemical Structure & Properties

Tesofensine is a tropane alkaloid analog with a molecular formula of C17H23Cl2N and a molecular weight of 312.28 g/mol. It is typically isolated as the hydrochloride salt, which improves water solubility and stability. The compound is a white to off-white crystalline powder, soluble in water, ethanol, and DMSO. Its logP value of approximately 3.5 indicates moderate lipophilicity, facilitating CNS penetration. Tesofensine exhibits stereochemical specificity, with the (1R,2R,3S,5S) configuration being the active isomer. It is stable under recommended storage conditions but should be protected from light and moisture.

Механизм действия

• Serotonin reuptake inhibition: Blocks SERT, increasing synaptic serotonin levels, which may contribute to mood regulation and appetite suppression.
• Norepinephrine reuptake inhibition: Inhibits NET, enhancing noradrenergic signaling, which can increase energy expenditure and alertness.
• Dopamine reuptake inhibition: Targets DAT, elevating dopamine concentrations, potentially improving motivation and reward pathways.
• Triple monoamine reuptake inhibition: The combined action on SERT, NET, and DAT distinguishes tesofensine from selective reuptake inhibitors, offering a multifaceted approach to metabolic and neurological disorders.

Quality Specifications

Supply & Documentation

• Capacity: Monthly production capacity of 5 kg, scalable upon request.
• Срок выполнения заказа: 3–5 рабочих дней (товары, имеющиеся в наличии)
• Documentation: COA, MSDS, TDS, and additional regulatory support available upon request.
• Packaging: 1 kg, 5 kg, and 25 kg fiber drums with double polyethylene liners to ensure stability during transport.

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