Maprotiline (Hydrochloride), selective NA reuptake inhibitor, a tetracyclic antidepressant with sedative properties, exhibits strong inhibitory effects on norepinephrine uptake across nerve cell membranes but interferes relatively little with serotoninergic mechanisms[3]. Maprotiline bounds to the full-length recombinant sGC (Soluble guanylate cyclase) with a high affinity (KD = 0.307 μM). Moreover, in a monocrotaline rat model of PAH (Pulmonary arterial hypertension), maprotiline (ip, 10 mg/kg once daily) reduced pulmonary hypertension, inhibited the development of right ventricular hypertrophy and pathological changes of the pulmonary vascular remodeling[4].
Maprotiline HCl/盐酸马普替林 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Vero cells
10 or 20 μM
4 h
Maprotiline inhibited acid sphingomyelinase activity and prevented infection with pp-VSV-SARS-CoV-2 spike particles
Cell Rep Med. 2020 Nov 17;1(8):100142
HEK293 cells
1.51 μmol/L
Evaluate the inhibitory activity of Maprotiline on Nav1.7 channels
Acta Pharmacol Sin. 2020 Mar;41(3):293-302
HEK293T cells
10 µM
24 hours
Maprotiline significantly inhibited Tm/Tg-induced CHOP expression and XBP-1 splicing, indicating its restoration of ER homeostasis by inhibiting HRH1-mediated ER Ca2+ release.
Nat Commun. 2022 Nov 10;13(1):6796
Brain-stem neurons
10^-6 M
30 minutes
To study the effect of Maprotiline on norepinephrine uptake, results showed that Maprotiline did not affect 3H-serotonin uptake.
J Cell Biol. 1981 Oct;91(1):142-52
Rabbit isolated hearts
8 μM
To assess the effects of Maprotiline on cardiac rhythm. Results showed that Maprotiline (8 μM) could induce dysrhythmias involving interference with atrio-ventricular synchronization.
Br J Pharmacol. 1977 Apr;59(4):651-60
Rabbit isolated hearts
4.8 μM
15 minutes
To evaluate the effects of Maprotiline on cardiac force and A-V contraction interval. Results showed that Maprotiline (4.8 μM) significantly reduced ventricular force but did not significantly affect atrial force or heart rate.
Br J Pharmacol. 1977 Apr;59(4):651-60
Maprotiline HCl/盐酸马普替林 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Traumatic optic nerve injury model and glaucoma model
Intravitreal injection and intraperitoneal injection
15 mg/kg
Once daily for 14 days
Maprotiline significantly protected RGC somata and axons and preserved visual functions in two mouse optic neuropathy models.
Nat Commun. 2022 Nov 10;13(1):6796
Rats
Intraperitoneal injection
20 mg/kg and 50 mg/kg
Single injection
Maprotiline (20 mg/kg) enhanced NMDAR-EPSC, while a higher dose (50 mg/kg) reduced NMDAR-EPSC.
Biol Psychiatry. 2014 Dec 15;76(12):953-62
Mice
Huntington's disease model
In vitro culture
2 μM
2-3 hours pretreatment
Maprotiline, as a blocker of the mitochondrial permeability transition pore (MPTP), protects YAC128 medium spiny neurons from glutamate-induced apoptosis.
Proc Natl Acad Sci U S A. 2005 Feb 15;102(7):2602-7
New Zealand White rabbits
Conscious or barbiturate-anaesthetized rabbits
Intravenous infusion
25 mg/kg/h
Continuous infusion until death or 5 hours
To assess the relative toxicity of Maprotiline, which showed intermediate lethal doses between amitriptyline and mianserin. In anaesthetized rabbits, it caused dose-dependent reductions in heart rate and blood pressure, ECG changes (prolonged P-R interval and widened QRS complex), and arrhythmias at higher doses than amitriptyline and imipramine but significantly lower than mianserin.
Br J Pharmacol. 1979 Feb;65(2):331-8
Rats
Anesthetized rats
Intravenous injection
0.5 mg/kg
Single dose
To study the effect of Maprotiline on the vasodepressor responses evoked by histamine. Results showed that Maprotiline inhibited the vasodepressor responses to histamine, similar to promethazine.
Br J Pharmacol. 1981 Sep;74(1):143-8
Rats
Pithed rats
Intravenous
0.5 mg/kg
Single administration
To compare the effects of Maprotiline with other drugs on cardiac and vascular adrenoceptors. Results showed that Maprotiline potentiated pressor responses to noradrenaline and inhibited the pressor action of tyramine.
China, Beijing
... 展开 >> The Third Affiliated Hospital of Beijing University of Chinese Medicine
Recruiting
Beijing, Beijing, China, 100029
Contact: Wenjun Sun, MD, PHD +86 18910259376 doctorsunwenjun@126.com 收起 <<
China, Beijing
... 展开 >> The Third Affiliated Hospital of Beijing University of Chinese Medicine
Recruiting
Beijing, Beijing, China, 100029
Contact: Wenjun Sun, MD, PHD +86 18910259376 doctorsunwenjun@126.com 收起 <<
搜索
