Maprotiline inhibits cell proliferation and metastasis with anticancer effects. Maprotiline induces apoptosis in cancer cells by targeting ERK signaling pathway and CRABP1. Maprotiline is a highly selective norepinephrine reuptake blocker with potent antidepressant properties. [1][2].

Maprotiline (10 μM) enhances the sensitivity of HCC cells to sorafenib (2 μM) and induces apoptosis [2]. Maprotiline (0, 10, or 20 μM for 72 h) works on ERK pathway and inhibits phosphorylation of SREBP2 in HepG2 and Huh7 cells [2]. Maprotiline may targets CRABP1 and regulate cholesterol biosynthesis in HCC cells [2]. Cell Invasion Assay [2] Cell Line: The human HCC cell lines Huh7 and HepG2 Concentration: 0, 10, 20 μM Incubation Time: 24 hours Result: Restrained HCC cells migration with inhibition of epithelial-mesenchymal transition (EMT). Cell Viability Assay [2] Cell Line: The human HCC cell lines Huh7 and HepG2 Concentration: 0, 10, 20 μM Incubation Time: 0, 24, 48, 72, 96, 120 hours Result: Triggered cell apoptosis and inhibited the cell viability of Huh7 and HepG2 cells in a dose- and time-dependent manner. Western Blot Analysis [2] Cell Line: The human HCC cell lines Huh7 and HepG2 Concentration: 0, 10, 20 μM Incubation Time: 72 hours Result: Inhibited cholesterol biosynthesis in HCC Cells.

Maprotiline (intraperitoneal injection; 3, 10, or 30 mg/kg) combinds with the synthetic cannabinoid WIN 55,212-2 and effectively reduces neuropathic pain [1]. Maprotiline (intraperitoneal injection; 0, 20, or 40 mg/kg; twice a week; 3 weeks) shows low toxicity and side effects on the organs, immune system and hematopoietic function [2]. Maprotiline (intraperitoneal injection; 0, 20, or 40 mg/kg; twice a week; 3 weeks) restrains cholesterol biosynthesis to inhibit growth and metastasis of HCC cells by interacting with CRABP1 [2]. Animal Model: Male Balb-c mice (25–30 g) [1] Dosage: 3, 10, 30 mg/kg Administration: Intraperitoneal injection; evaluation 30 minutes after treatment Result: Attenuated pain-related behaviours in neuropathic mice. Animal Model: Nude mice (BALB/C nu/nu, 4–6 weeks old, female) [2] Dosage: 40 mg/kg Administration: Intraperitoneal injection; twice a week; 3 weeks Result: Decreased the cholesterol levels in serum and tumors and suppressed the growth of Huh7-derived tumor xenografts without obvious toxic effect.