Besipirdine – (119257-34-0)

Besipirdine, also known as HP-749, is an indole-substituted analog of 4-aminopyridine, developed as a nootropic drug for the treatment of Alzheimer’s disease (AD). It enhances acetylcholine release by blocking M-channels and voltage-gated K+ channels, increasing neuronal excitation.

Besipirdine also antagonizes the noradrenergic α2 receptor, increasing norepinephrine release and inhibiting its uptake. Initially considered for obsessive-compulsive disorder (OCD), it was later explored for Alzheimer’s due to its effects on the cholinergic and adrenergic systems.

However, it failed in Phase III trials due to severe cardiovascular side effects. Currently, it is under Phase III development for lower urinary tract dysfunctions by UroGene.

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Sources:

https://en.wikipedia.org/wiki/Besipirdine
https://pubchem.ncbi.nlm.nih.gov/compound/60691
https://www.medchemexpress.com/besipirdine.html
https://www.medkoo.com/products/12320
https://www.sciencedirect.com/science/article/abs/pii/S0090429507014628