Home Neuronal Signaling Adrenergic Receptor antagonist Maprotiline HCl

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Maprotiline HCl Adrenergic Receptor antagonist

Cat.No.S2517

Maprotiline HCl is a selective noradrenalin re-uptake inhibitor, used in the treatment of depression.
Maprotiline HCl Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 313.86

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Chemical Information, Storage & Stability

Molecular Weight 313.86 Formula

C20H23N.HCl

 Storage (From the date of receipt)
CAS No. 10347-81-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C24.Cl

Solubility

In vitro
Batch:

DMSO : 62 mg/mL ( (197.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 52 mg/mL

Water : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
Adrenergic Receptor [1]
In vitro

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]
In vivo

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]
References
  • https://pubmed.ncbi.nlm.nih.gov/19091461/
  • https://pubmed.ncbi.nlm.nih.gov/20574769/
  • https://pubmed.ncbi.nlm.nih.gov/10699652/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04200066 Withdrawn
Glioblastoma|Brain Tumor
University of Rochester
 June 1 2022 Phase 1

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