Ipidacrine-d9

Ipidacrine-d9 (NIK-247-d9 (free base) ) is the deuterium labeled 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].

NIK-247-d9 (free base)

12352005

Cholinesterase (ChE) ; Isotope-Labeled Compounds; Potassium Channel; Sodium Channel

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Metabolic Disease

[2H]C1(C2=C(C([2H])(C([2H])(C1([2H])[2H])[2H])[2H])N=C3C([2H])(CCC3=C2N)[2H])[2H]

C12H6D10N2

198.33

[1]Kojima J, et al. Ipidacrine (NIK-247) : A Review of Multiple Mechanisms as an Antidementia Agent[J]. CNS Drug Reviews, 1998, 4 (3) : 247-259.|[2]Pulatov S S. Efficacy of ipidacrine in the recovery period of ischaemic stroke[J]. World Bulletin of Public Health, 2022, 7: 28-32.|[3]Bykov V, et al. Ipidacrine (Axamon), A Reversible Cholinesterase Inhibitor, Improves Erectile Function in Male Rats With Diabetes Mellitus-Induced Erectile Dysfunction[J]. Sex Med. 2022 Feb;10 (1) :100477.|[4]Zinovyeva O E, et al. Ipidacrine efficacy in diabetic polyneuropathy complex treatment: A review[J]. Consilium Medicum, 2022, 24 (2) : 123-127.|[5]Samartsev I N, et al. The efficacy and safety of ipidacrine in patients with idiopathic neuropathy of the facial nerve (PELICAN study) [J]. Neurology, Neuropsychiatry, Psychosomatics, 2022, 14 (1) : 60-68.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W027553S1/

Isotope-Labeled Compounds

No Development Reported