Tesofensine (250mcg) / Dihexa (5mg) x 60 Tablets

What is Tesofensine / Dihexa Tablets?

This dual-tablet formulation brings together two compounds with distinct mechanisms suited for preclinical exploration of neurochemical and neurotrophic pathways:

• Tesofensine is a potent triple monoamine reuptake inhibitor that blocks dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters, enhancing synaptic monoamine levels. It was initially investigated for neurological conditions and later shown to suppress appetite and increase energy expenditure in animal studies.
• Dihexa (PNB-0408) is an orally bioavailable oligopeptide derived from angiotensin IV that allosterically enhances hepatocyte growth factor (HGF) signaling at the c-Met receptor. It demonstrates strong blood–brain barrier penetration and promotes synaptogenesis and synaptic plasticity in rodent models.

This combination serves as a research tool to evaluate synergistic effects between enhanced neurotransmitter availability and HGF-mediated neuroplastic signaling.

Chemical Structure of Tesofensine / Dihexa Tablets

• Tesofensine has the molecular formula C₁₇H₂₃Cl₂NO with a molecular weight of approximately 327 Da. Structurally, it is a phenyltropane derivative substituted with dichlorophenyl and ethoxymethyl groups that confer high affinity for DAT, NET, and SERT.
• Dihexa has the molecular formula C₂₇H₄₄N₄O₅, with a mass of 504.7 Da. Its structure consists of a hexanoyl–Tyr–Ile–aminohexanoic acid backbone (N-hexanoic‑Tyr‑Ile‑Ahx‑NH₂), designed to optimize HGF binding, metabolic stability, and blood–brain barrier penetration.

What Are the Effects of Tesofensine / Dihexa Tablets?

• Monoamine Enhancement (Tesofensine): In animal and early human studies, tesofensine significantly increased synaptic levels of dopamine, norepinephrine, and serotonin. This elevation has been linked to reduced appetite, enhanced energy expenditure, mood stabilization, and weight loss.
• Neuroplasticity & Synaptogenesis (Dihexa): Dihexa exhibits femtomolar affinity for HGF, potentiating c-Met activation and promoting dendritic spine formation and functional synapse development. These neuroplastic effects are confirmed by Morris water maze assays and blocked by HGF antagonists.
• Complementary Neurochemical and Structural Effects: This tablet formulation enables exploration of the combined enhancement of neurotransmitter tone and structural neural support. Tesofensine-driven monoamine presence could potentiate Dihexa-mediated synaptic remodeling, offering a multifaceted approach to studying neurobiological enhancement in preclinical models.

Citations

1. NCATS Inxight Drugs – Tesofensine (NS-2330): triple DAT/NET/SERT reuptake inhibitor; investigated in obesity and neurological models. Dual Mechanism Overview: Tesofensine + Dihexa
2. PubChem Compound Summary – Dihexa (CID 57582587): N‑hexanoic‑Tyr‑Ile‑Ahx‑NH₂; molecular formula C₂₇H₄₄N₄O₅; MW 504.7 Da. Dual Mechanism Overview: Tesofensine + Dihexa
3. PeptideWiki – Dihexa binds HGF with femtomolar affinity, promotes c-Met phosphorylation and synaptogenesis; cognitive enhancement blocked by HGF/c-Met antagonist. Dual Mechanism Overview: Tesofensine + Dihexa
4. Journal of Pharmacology and Experimental Therapeutics – Chapman TR, et al. “Facilitation of the brain HGF/c-Met receptor system improves learning and memory in a model of Alzheimer’s disease.” 2013;346(3):528–536. PMID: 23852499. Dual Mechanism Overview: Tesofensine + Dihexa