Friday, July 12, 2019 9:51:31 AM
Edonerpic maleate is described as "A neural plasticity enhancer"
https://www.biovision.com/edonerpic-maleate.html
The article you site concludes:
“The clinical outcomes of three Phase 2 trials do not provide evidence of clinical proof of concept for edonerpic maleate for patients with mild to moderate Alzheimer disease,” wrote the authors.—Gwyneth Dickey Zakaib
I am not sure that it has been established that edonerpic maleate is a sigma 1 agonist or how it may activate sigma 1?The article you site does say that edonerpic maleate is a sigma 1 activator although other articles mention that "T-817MA reportedly activates sigma receptors." https://www.alzforum.org/therapeutics/edonerpic
"Chemical Name: 1-{3-[2-(1-benzothiophen-5-yl)ethoxy] propyl}-3-azetidinol maleate". https://www.alzforum.org/therapeutics/edonerpic
I have not found anything that discusses edonerpic maleate in terms of sigma 1 activation or how it may do that.
AVXL 2-73 is a completey different chemical. "Chemical Name: Tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride". https://www.alzforum.org/therapeutics/anavex-2-73
"Anavex 2-73 is a small molecule that activates the sigma-1 receptor, which is known to modulate cellular processes relevant to neurodegeneration. "
https://alzheimersnewstoday.com/anavex-2-73/
AVXL 2-73 is also a mixed ligand. "This compound is an agonist of the intracellular sigma-1 chaperone protein. Specifically, it is a mixed ligand for sigma1/muscarinic receptors. Expressed in most tissues and located at focal contacts between mitochondria and the endoplasmic reticulum, the sigma-1 receptor forms heterodimers with many other membrane receptors, and as such influences multiple cellular pathways and physiological processes. Anavex 2-73 reportedly binds the sigma-1 receptor in the high nanomolar and the muscarinic receptor in the low micromolar range." https://www.alzforum.org/therapeutics/anavex-2-73
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