产品描述

Maprotiline hydrochloride is a bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.

靶点活性

5-HT,

Adrenergic Receptor,

H1 receptor,

mAChR,

Noradrenaline transporter (Sodium-dependent),

体外活性

Maprotiline inhibits HERG channels expressed in HEK cells with an IC50 of 5.2 μM and HERG channels expressed in oocytes with an IC50 of 24 μM. Maprotiline blocks open channels but has no significant effect on closed channels. [1] Maprotiline is atetracyclic antidepressant, which strongly inhibits the uptake of noradrenaline, though it is notable in its lack of inhibition of serotonergic uptake. Maprotiline also has markedly less pronounced alpha-adrenergic blocking activity than amitriptyline. [2] Maprotiline decreases cell viability in a concentration- and time-dependent manner in Neuro-2a cells. Maprotiline induces apoptosis and increases caspase-3 activation. Maprotiline also induces [Ca(2+)](i) increases which involves the mobilization of intracellular Ca(2+) stored in the endoplasmic reticulum. [3]

体内活性

Maprotiline results in significantly increases GluR1 and GluR2/3 subunit expression in the nucleus accumbens and dorsal striatum of mice as detected by immunohistochemistry; and significantly increases GluR1 and GluR2/3 expression in the hippocampus, as demonstrated by Western blot analysis. [4] Maprotiline has a potent anti-inflammatory effect in rats and this effect is linked to the peripheral and supraspinal actions of the drug. [5] Maprotiline impairs learning when administered before training, but no statistically significant effect is evident when administered after training. [6]

分子量

313.86

分子式

C20H24ClN

CAS

10347-81-6

溶解度

DMSO: 59 mg/mL (188 mM)

Ethanol: 23 mg/mL (73.3 mM)

Water: <1 mg/mL

（ < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.