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Tuesday, August 10, 2021 10:51:20 AM
Please, compare and comment regarding the IC50 concentrations.
Thank you for the invitation, but it would be best for someone more competent in the specifics of reaction dynamics to fully elucidate the data presented for the three Anavex molecules.
But it is clear, at the sigma-1 receptor, both Anavex 3-71 and Anavex 1-41 work far more strongly, in far lower concentrations than blarcamesine (Anavex 2-73). The effective, reactive concentrations of the first two are measured in nanomoles (nM), compared to the micromoles (µM) of blarcamesine (Anavex 2-73).
A micromole is one-millionth of a mole. A mole is a standardized unit in chemistry, having 6.02214076×10 to the 23rd) particles, in this case, molecules.
A nanomole is one-billionth of a mole, one one-thousandth the size of a micromole.
To be effective, blarcamesine needs concentrations a thousand times greater than either of the other two Anavex drugs. Is that, then, a problem?
Nope. As both murine and human therapeutic data have shown, blarcamesine works wonderfully, with great safety and efficacy at its much higher concentrations. “Higher” in regard only to the other two Anavex drugs; not in comparison to the concentrations of the other Alzheimer’s drug, Aricept (donepezil). That drug is prescribed in milligram doses much larger than blarcamesine.
What might be the takeaway?
Simply, Anavex 3-71 works in extremely low concentrations. Therefore, it is less likely to cause side effects. And blarcamesine, at it's far larger dosages, has few side effects; none that disqualify it.
For Anavex, across the board, safety and efficacy. (In the central nervous system, even.)
Recent AVXL News
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