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Tesofensine (NS-2330) is a potent triple monoamine reuptake inhibitor (IC50 ~6.5 nM DAT, 1.7 nM NET, 11 nM SERT) that produces dose-dependent reductions in food intake in rodent models (ED50 ~1.3 mg/kg) via α1-adrenoceptor and D1 receptor pathways with forebrain dopamine normalization, high DAT occupancy (~80%), and a long half-life, originally studied in animal models of Parkinson's and Alzheimer's disease.
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Product Name: Tesofensine
CAS Number: 195875-84-4
Molecular Formula: C₁₇H₂₃Cl₂NO
Molecular Weight: 328.28 g/mol
PubMed ID: 18474731
Tesofensine (NS-2330) is a potent triple monoamine reuptake inhibitor that blocks the presynaptic reuptake of dopamine, norepinephrine, and serotonin. In preclinical rodent models, it produces dose-dependent reductions in food intake (ED50 ~1.3 mg/kg), mediated in part through indirect stimulation of α1-adrenoceptor and dopamine D1 receptor pathways, with associated normalization of lowered forebrain dopamine levels. Pharmacologically, it exhibits high affinity for the monoamine transporters (IC50 values of approximately 6.5 nM for dopamine, 1.7 nM for norepinephrine, and 11 nM for serotonin uptake), with dose-dependent dopamine transporter (DAT) occupancy reaching up to ~80% in imaging studies, and a long elimination half-life. Originally investigated in models of neurodegenerative conditions such as Parkinson’s and Alzheimer’s disease, tesofensine continues to be studied for its effects on monoaminergic neurotransmission in animal systems.
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