Ipidacrine

Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K⁺ and Na⁺-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases^{[1][2][3][4][5]}. In Vitro: Ipidacrine showes a concentration-dependent and reversible inhibition of AChE and BuChE activity with IC₅₀ values of 1 μM and 1.9 μM, respectively^[1].
In Vivo: Ipidacrine (1 mg/kg, p.o., repeated and a single dose for 5 days) by repeated administration has more potent antiamnesic effects than by single administration in induced by nucleus basalis of meynert (NBM) induced rats^[1].
Ipidacrine (10 mg/kg p.o., a single dose) significantly decreases spontaneous movements, which is more selective as an antiamnesic than either Tacrine (HY-111338) and E-2020 (HY-B0034) in rats^[1].
Ipidacrine (6.7 mg/kg, intragastrically, daily for 14 days) leads to statistically more efficient evolving of intracavernous pressure (ICPmax)/maxipressure (MAP) compared with control group in Streptozotocin (STZ) (HY-13753)-induced diabetic rats^[3].