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mesocaine + thiocolchicoside + amitriptyline + magnesium pidolate

Development stage
Preclinical
Lead developer
Polyclinique de l'Europe
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a fixed-dose combination drug containing four active ingredients: - **Mesocaine (trimecaine):** An amide-type local anesthetic used for local anesthesia and as an antiarrhythmic. It works by blocking sodium channels, reducing nerve membrane permeability, and inhibiting depolarization, which leads to loss of sensation in the area of application[2][4]. - **Thiocolchicoside:** A muscle relaxant with anti-inflammatory and analgesic properties. It acts as a GABA-A receptor agonist and glycine receptor agonist, leading to muscle relaxation. - **Amitriptyline:** A tricyclic antidepressant primarily used for depression but also prescribed for neuropathic pain and certain chronic pain conditions. Its mechanism involves inhibition of serotonin and norepinephrine reuptake in the central nervous system[6][9]. - **Magnesium pidolate:** A chelated form of magnesium with high bioavailability, used as a mineral supplement to correct magnesium deficiency. Magnesium supports neuromuscular function, cardiovascular health, bone health, metabolic regulation, stress relief, and cognitive function[7][10]. This combination is designed to provide multimodal management of musculoskeletal pain or spasticity by combining local anesthesia (mesocaine), muscle relaxation (thiocolchicoside), neuropathic pain modulation (amitriptyline), and mineral supplementation (magnesium pidolate).

02

Targets

SERT (Sodium-dependent serotonin transporter)GABRR (GABA-A receptor subunit rho)NaV (Voltage-gated sodium channels)GLRA1 (Glycine receptor subunit Alpha-1)NET (Norepinephrine Transporter)

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