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编 号：F012563
分子式：C20H23N
分子量：277.4
分子式：C20H23N
分子量：277.4
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CAS No: 10262-69-8
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生物活性：
Maprotiline is a highly selective noradrenergic reuptake blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect.
体内研究：
Maprotiline (3, 10, or 30 mg/kg; i.p.) combinds with the synthetic cannabinoid WIN 55,212-2 and effectively reduces neuropathic pain.Maprotiline (0, 20, or 40 mg/kg; i.p.; twice a week; 3 weeks) shows low toxicity and side effects on the organs, immune system and hematopoietic function.Maprotiline (0, 20, or 40 mg/kg; i.p.; twice a week; 3 weeks) restrains cholesterol biosynthesis to inhibit growth and metastasis of HCC cells by interacting with CRABP1.Animal Model:Male Balb-c mice (25–30 g)
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)
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.
体外研究：
Maprotiline (10 μM) enhances the sensitivity of HCC cells to sorafenib (2 μM) and induces apoptosis.Maprotiline (0, 10, or 20 μM for 72 h) works on ERK pathway and inhibits phosphorylation of SREBP2 in HepG2 and Huh7 cells.Maprotiline may target CRABP1 and regulate cholesterol biosynthesis in HCC cells.
Maprotiline is a highly selective noradrenergic reuptake blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect.
体内研究：
Maprotiline (3, 10, or 30 mg/kg; i.p.) combinds with the synthetic cannabinoid WIN 55,212-2 and effectively reduces neuropathic pain.Maprotiline (0, 20, or 40 mg/kg; i.p.; twice a week; 3 weeks) shows low toxicity and side effects on the organs, immune system and hematopoietic function.Maprotiline (0, 20, or 40 mg/kg; i.p.; twice a week; 3 weeks) restrains cholesterol biosynthesis to inhibit growth and metastasis of HCC cells by interacting with CRABP1.Animal Model:Male Balb-c mice (25–30 g)
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)
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.
体外研究：
Maprotiline (10 μM) enhances the sensitivity of HCC cells to sorafenib (2 μM) and induces apoptosis.Maprotiline (0, 10, or 20 μM for 72 h) works on ERK pathway and inhibits phosphorylation of SREBP2 in HepG2 and Huh7 cells.Maprotiline may target CRABP1 and regulate cholesterol biosynthesis in HCC cells.
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