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Tuesday, 02/20/2018 1:51:14 PM

Tuesday, February 20, 2018 1:51:14 PM

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30+ New Antidepressants (2018): Drugs In Clinical Trials
https://mentalhealthdaily.com/2018/02/13/new-antidepressants-2018-drugs-in-clinical-trials/

14. Ganaxolone

Mechanism: GABAA receptor modulator
Status: Phase II
Developer: Marinus Pharmaceuticals
Ganaxolone is a drug being developed by Marinus Pharmaceuticals for the treatment of postpartum depression, as well as several other conditions such as: epilepsy and Fragile X syndrome. Pharmacodynamic assessments indicate that Ganaxolone functions as a selective positive allosteric modulator of the GABAA receptor. When administered to animals, Ganaxolone yields antiepileptic and anxiolytic effects whereby it respectively protects against seizures and reduces anxiety-like behavior.

Its action as a positive allosteric modulator of both synaptic and extrasynaptic GABAA receptors aids in the normalization of over-excited neurons and excitotoxicity. Like other GABAA receptor modulators, Ganaxolone binds to allosteric sites of the GABAA receptor which triggers opening of the chloride ion channel to hyperpolarize the neuron. Hyperpolarization of the neuron yields an inhibitory effect upon neurotransmission whereby likelihood of action potentials is reduced.

Compared to other agents that modulate the GABAA receptor, Ganaxolone may be unique in its ability to act upon extrasynaptic receptor sites. Currently, Ganaxolone is in phase II of clinical trials. The most common side effects associated with Ganaxolone reported thus far include: sleepiness, dizziness, and fatigue – (most of which should be expected with GABAA receptor modulation).

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